Technology Evaluation

Eudragit
: a technology
evaluation
Seema Thakral, Naveen K Thakral & Dipak K Majumdar†
†
1. Introduction University of Delhi, Delhi Institute of Pharmaceutical Sciences and Research (Formerly College of
Pharmacy), Department of Pharmaceutics, New Delhi, India
2. Types of Eudragit
3. Background and Introduction: Eudragit is the brand name for a diverse range of polymethacry-
characterization late-based copolymers. It includes anionic, cationic, and neutral copolymers
4. Coating methodologies used based on methacrylic acid and methacrylic/acrylic esters or their derivatives.
for Eudragit Areas covered: In this review, the physicochemical characteristics and appli-
cations of different grades of Eudragit in colon-specific/enteric-coated/
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12

5. Registered products
sustained release drug delivery and taste masking have been addressed.
containing Eudragit
Expert opinion: Eudragits are amorphous polymers having glass transition
6. Safety profile of Eudragit
temperatures between 9 to > 150oC. Eudragits are non-biodegradable, non-
7. Applications of Eudragit in absorbable, and nontoxic. Anionic Eudragit L dissolves at pH > 6 and is used
colon-specific/enteric-coated for enteric coating, while Eudragit S, soluble at pH > 7 is used for colon targe-
delivery system ting. Studies in human volunteers have confirmed that pH drops from 7.0 at
8. Application of Eudragit in terminal ileum to 6.0 at ascending colon, and Eudragit S based systems some-
sustained release delivery times fail to release the drug. To overcome the shortcoming, combination of
system Eudragit S and Eudragit L which ensures drug release at pH < 7 has been advo-
9. Applications of Eudragit in cated. Eudragit RL and RS, having quaternary ammonium groups, are water
For personal use only.

taste masking and protective insoluble, but swellable/permeable polymers which are suitable for the
system sustained release film coating applications. Cationic Eudragit E, insoluble at
10. Incompatibilities associated pH ‡ 5, can prevent drug release in saliva and finds application in
with Eudragit taste masking.
11. Conclusions
Keywords: colon targeting, enteric coating, Eudragit, polymethacrylates, sustained release
12. Expert opinion
delivery, taste masking

Expert Opin. Drug Deliv. (2013) 10(1):131-149

1. Introduction

Eudragit is the brand name for a diverse range of copolymers based on polymetha-
crylates principally marketed by Evonik Industries, Germany. Eudragit was first
introduced by Rohm & Hass GmbH, Darmstadt in 1953 as an alkaline soluble
drug coating material resistant to stomach acid. The brand has gradually diversified
to include anionic, cationic as well as neutral copolymers based on methacrylic acid
and methacrylic or acrylic esters or their derivatives in varying proportions, and
these copolymers exhibit varying degree of pH dependent/independent solubility
profiles. In addition to being extensively used for functional pharmaceutical
coatings, Eudragits are applied as matrix formers in common granulation
techniques as well as in direct compression.

2. Types of Eudragit

Eudragits are synthetic polymers obtained by polymerization of acrylic acid (prop-

2-enoic acid; CH2=CHCOOH) and methacrylic acids or their esters like butyl ester
or dimethylaminoethyl ester. Being synthetic polymers, Eudragits are supplied in
extensively reproducible forms, in comparison to cellulosic derivatives, whose
physicochemical properties may vary depending on the source of raw material.
Methacrylate copolymers are synthesized via free-radical polymerization, wherein

10.1517/17425247.2013.736962 © 2013 Informa UK, Ltd. ISSN 1742-5247, e-ISSN 1744-7593 131
All rights reserved: reproduction in whole or in part not permitted
 S. Thakral et al.

CH3 CH3 CH3 CH3

I CH2 C. + C = CH2 Exothermic I CH2 C CH2 C

C=O C=O C=O C=O

OR OR OR OR

Figure 1. Free radical polymerization started by initiator I [2].

R1 R3 R1 R3
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12

C CH2 C CH2 C CH2 C CH2

C=O C=O C=O C=O

OR2 OR4 OR2 OR4 n

Eudragit R1 R2 R3 R4
Grade
E CH3 CH2CH2N(CH3)2 CH3 CH3, C4H9
L and S CH3 H CH3 CH3
RL and RS H, CH3 CH3, C2H5 CH3 CH2CH2N(CH3)3+Cl-
NE 30D H, CH3 CH3, C2H5 H, CH3, C2H5
For personal use only.

CH3
L 30 D-55 and H, CH3 H H CH3, C2H5
L 100-55 CH3

Figure 2. Basic chemical structure of Eudragit and different grades.

various acrylate and methacrylate derivatives are incorporated
into the polymer by chain grow reactions [1]. (Figure 1) The
polymerization reaction can be performed in solvent, bulk,
suspension, or emulsion. Variations in chain length are
obtained via various termination and transfer reactions. The
functional properties of methacrylate copolymers and the
final polymer can be adjusted by selecting from a variety of
monomers. The non-functional co-monomers are responsible
for steering the polymer properties, and the functional
co-monomer for adjusting the solution profile [2].
The basic chemical structure of Eudragit and its different
grades is presented in Figure 2. Different grades of Eudragit
are commercially available and these are supplied in various
forms such as dry powder, granules, aqueous dispersion, or
organic solution. A (60:40) mixture of acetone and isopropa-
nol is most commonly used as the organic solvent [3]. The
chemical nature, characteristic features, and applications of
different types of Eudragit have been compiled in Table 1.
The table shows that four broad classes of Eudragit are avail-
able: cationic Eudragit E (soluble below pH 5.5) has applica-
tion in taste masking; anionic Eudragit L and S (soluble above
pH 6 and 7, respectively) are used in colon targeting/enteric
coating; neutral types Eudragit RL and RS (pH-independent
solubility) as well as Eudragit NE and NM (swellable and
permeable) are used in sustained release drug delivery.
In addition to all these popular grades, some lesser known
grades of Eudragit include Eudragit P4135, a methacrylic
acid, methyl acrylate, and methyl methacrylate copolymer
(ratio of the functional groups 25:10:65), though its aqueous
dispersion is used as Eudragit FS 30 D. Eudragit RD 100,
which is comprised of 91% Eudragit RL PO and 9% carboxy
methyl cellulose (the inclusion of latter increasing its perme-
ability), is used as pH-independent coating material for fast
disintegrating films.
3. Background and characterization
3.1 Chemistry of Eudragit
Methacrylic acid copolymers: Copolymers of methyl methac-
rylate (MMA) and ethyl acrylate (EA) as ester components
with methacrylic acid (MA) are used for enteric coatings.
Their enteric effect is attributed to the presence of carboxylic
groups that are transformed to carboxylate in the pH range of
5 -- 7 by salt formation with alkali or amines. In pure water
and dilute acids they form a water-insoluble film which is
resistant to gastric juice. Further, due to their low permeabi-
lity to water vapor, an effective isolating layer is formed.
The dissolution pH of the copolymer depends primarily on
the content of carboxylic groups; poly (MA-MMA) 1:1
(Eudragit L) dissolves at > pH 6, poly (MA-MMA)

132 Expert Opin. Drug Deliv. (2013) 10(1)


1:2 (Eudragit S) dissolves at pH above 7. When the ester com-
ponent is replaced with ethyl acrylate (poly (MA-EA) 1:1;
Eudragit L 100-55), the resulting film dissolves above pH 5.5.
Methacrylate ester copolymers: Methacrylate ester copoly-
mers are neutral or weakly cationic polymers and are insoluble
in pure water, dilute acids, buffer solutions, or digestive fluids
over the entire physiological pH range. Eudragit E is a
cationic polymer based on dimethylaminoethyl methacrylate,
butyl methacrylate, and methyl methacrylate. It is soluble in
gastric fluid as well as in weakly acidic buffer solution (up to
pH ~ 5) [2]. The films prepared from poly (EA-MMA)
2:1 (Eudragit NE 30 D) swell in water, show medium degree
of permeability, which is not dependent upon pH. The film
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
formed at room temperature is also soft and flexible. Intro-
duction of hydrophilic quaternary ammonium groups by
copolymerization with trimethylamminoethyl methacrylate
chloride (TMACl) modifies permeability of the methacrylate
ester copolymers. Films of poly (EA-MMA-TAMCl)
1:2:0.2 (Eudragit RL) are more permeable and poly (EA-
MMA-TAMCl) 1:2:0.1 (Eudragit RS) are less permeable
than Eudragit NE 30 D. The quaternary ammonium groups
can be titrated electrometrically in water after addition of
mercuric acetate [4,5].
For personal use only.
3.2 Characterization of Eudragit polymers
X-ray powder diffractogram of Eudragit L 100, S 100, RL and
RS are presented in Figure 3. As evident from the figure, the
diffractograms of all these Eudragit grades demonstrate a
halo indicating amorphous nature of the polymers. Differen-
tial thermal analysis of these polymers shows a single thermal
event as glass transition temperature, which is characteristic
for the different grades of Eudragit (Table 2). FTIR spectrum
of Eudragit L 100, S 100, RS and RL (Figure 4) shows
carbonyl vibrations of ester group in the range of
1734 -- 1728 cm--1 [6,7].
3.3 Physical properties of different Eudragit grades
One among the significant factors in describing the physical
properties of polymeric films is the glass transition tempera-
ture (Tg), which is a function of molecular mobility of the
polymer chain segments. Tg has far reaching consequences,
for example, for film formation, melt processing, and storage
of finished formulation. As evident from Table 2, the Tg of
Eudragit grades NE is ~ 9
C, Eudragit E ~ 48
C, of enteric
polymers (Eudragit L or S) is > 150
C, and insoluble
polymethacrylates is ~ 55
C. A plasticizer in a film coating
formulation lowers the Tg of polymer by reducing the inter-
molecular interaction between polymer chains and increases
the flexibility of the resulting film. For obtaining proper
degree of suppleness, 10% plasticizer is recommended
for the insoluble grades and 40% plasticizer is needed for
enteric grade, while no plasticizer is required for gastrosoluble
methacrylate polymers [8]. Citrate esters, polyethylene
glycol 6000 or polypropylene glycol have been reported to
effectively plasticize polymethacrylate polymer films [9,10].
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit
: a technology evaluation
In addition to the above, another important polymer prop-
erty playing decisive role in special applications is water vapor
transmission rate (WVTR), which influences the storage stabi-
lity of moisture sensitive formulations. In comparison to
hydroxyl propyl methyl cellulose (showing WVTR 900 g/m2.
day), polymethacrylate polymers demonstrate effective mois-
ture barrier property (WVTR ~ 100 -- 350 g/m2.day) as
presented in Table 2 [2].
4. Coating methodologies used for Eudragit
Eudragit polymers are widely used as coating materials in
order to achieve either modification of drug release behavior
or taste masking. For the purpose of coating, polymeric films
are generally applied to the solid dosage forms using the spray
atomization technique. Traditionally, the polymethacrylate
polymers are generally dissolved in organic solvents like
isopropanol and acetone. The organic coating dispersions
are generally turbid and disturb the coating process. Addition
of small amount of water is advised to improve the appearance
of the organic coating dispersion [8]. In addition, ready-to-use
aqueous dispersions of many Eudragit grades are also com-
mercially available. The solid core materials are often pre-
heated in the coating equipment prior to the coating
process. To reduce the stickiness and minimize agglomeration
of the coated substrates, anti-adherent compounds are gener-
ally included in the coating formulations and talc is one of
the most common anti-adherent. Studies have shown that
talc may cause increase in drug dissolution, presumably by
forming cracks in the coating [11].
While organic solvent film-coating technology suffers from
toxicological, environmental, cost, and safety-related disad-
vantages [12], the aqueous-based coating technology is associ-
ated with the limitations of slow drying rate of coating, high
energy input, possibility of microbial contamination, and
stability issues with water-sensitive drugs [13]. Recently, vari-
ous dry coating techniques for pharmaceutical products have
been widely investigated as an alternative to liquid-based
coating and these techniques have been applied for coating
with Eudragit polymers also.
. Compression coating: Mixture of Eudragit RS PO and S
100 was applied as seal coat on tablets to achieve con-
stant rate-regulated release. Polymer coating was shown
to be porous, allowing diffusion medium to enter the
core tablets and NMR analysis revealed diffusion of
water into compression coated tablets [14].
. Modified fluidized bed Wurster process: Used to coat
pellets with different formulations of Eudragit RS, ethyl
cellulose, and shellac so as to achieve sustained and
delayed release [15]. The process, however, is based
upon utilization of small amount of liquid plasticizer
of polymer solution to facilitate film formation.
. Dry powder coating: Applied to coat tablets with Eudragit
polymers, for example, Eudragit E PO [16], Eudragit
133
 Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
For personal use only.

Table 1. Different Eudragit grades, their chemical composition and properties with applications [2,3].

134
S. no Eudragit grade Chemical composition Available as/ polymer Solubility Applications
dry content
S. Thakral et al.

Cationic (Aminoalkyl methacrylate copolymers)

1 Eudragit E 100 Poly(butyl methacrylate, Granules/98% Soluble in gastric fluid Film coating
(2-dimethyl aminoethyl) to pH 5
methacrylate, methyl
methacrylate) 1:2:1
2 Eudragit E 12.5 Poly(butyl methacrylate, Organic solution/12.5% Soluble in gastric fluid Film coating
(2-dimethyl aminoethyl) to pH 5
methacrylate, methyl
methacrylate) 1:2:1
Anionic (Methacrylic copolymers)
1 Eudragit L 100 Poly(methacrylic acid, methyl Powder/95% Soluble in intestinal Enteric coating
methacrylate) 1:1 fluid from pH 6
2 Eudragit L 12.5 Poly(methacrylic acid, methyl Organic solution/12.5% Soluble in intestinal Enteric coating
methacrylate) 1:1 (without plasticizer) fluid from pH 6
3 Eudragit L 12.5 P Poly(methacrylic acid, methyl Organic solution/12.5% Soluble in intestinal Enteric coating
methacrylate) 1:1 (with1.25% dibutyl fluid from pH 6
phthalate as plasticizer)
4 Eudragit L 100-55 Poly(methacrylic acid, ethyl Powder/95% Soluble in intestinal Enteric coating
acrylate) 1:1 fluid from pH 5.5
5 Eudragit L Poly(methacrylic acid, ethyl Aqueous dispersion/30% Soluble in intestinal Enteric coating
30 D-55 (formerly acrylate) 1:1 fluid from pH 5.5
Eudragit L 30 D)
6 Eudragit S 100 Poly(methacrylic acid, methyl Powder/95% Soluble in intestinal Enteric coating
methacrylate) 1:2 fluid from pH 7

Expert Opin. Drug Deliv. (2013) 10(1)

7 Eudragit S 12.5 Poly(methacrylic acid, methyl Organic solution/12.5% Soluble in intestinal Enteric coating
methacrylate) 1:2 (without plasticizer) fluid from pH 7
8 Eudragit S 12.5 P Poly(methacrylic acid, methyl Organic solution/12.5% Soluble in intestinal Enteric coating
methacrylate) 1:2 (with1.25% dibutyl fluid from pH 7
phthalate as plasticizer)
9 Eudragit FS 30 D Methyl acrylate, methyl Aqueous dispersion/30% Soluble above pH 6.8 Enteric coating
methacrylate and methacrylic
acid
Neutral (Ammonioalkyl methyacrlate copolymers)
1 Eudragit RL Poly(ethyl acrylate, methyl Granules/97% High permeability Sustained release
100 (Type A) methacrylate, trimethyl
aminoethyl methacrylate
chloride) 1:2:0.2
2 Eudragit RL PO Poly(ethyl acrylate, methyl Powder/97% High permeability Sustained release
methacrylate, trimethyl
aminoethyl methacrylate
chloride) 1:2:0.2

Table 1. Different Eudragit grades, their chemical composition and properties with applications [2,3] (continued).
S. no Eudragit grade
3 Eudragit RL 30 D
4 Eudragit RS
100 (Type B)
5 Eudragit RS PO
6 Eudragit RS 30 D
Neutral (Methacrylate copolymer)
Expert Opin. Drug Deliv. (2013) 10(1)
1 Eudragit NE 30 D
(formerly Eudragit
E 30 D)
2 Eudragit NE 40 D
3 Eudragit NM 30 D
135
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
For personal use only.
Chemical composition Available as/ polymer Solubility Applications
dry content
Poly(ethyl acrylate, methyl Aqueous dispersion/30% High permeability Sustained release
methacrylate, trimethyl
aminoethyl methacrylate
chloride) 1:2:0.2
Poly(ethyl acrylate, methyl Granules/97% Low permeability Sustained release
methacrylate, trimethyl
aminoethyl methacrylate
chloride) 1:2:0.1
Poly(ethyl acrylate, methyl Powder/97% Low permeability Sustained release
methacrylate, trimethyl
aminoethyl methacrylate
chloride) 1:2:0.1
Poly(ethyl acrylate, methyl Aqueous dispersion/30% Low permeability Sustained release
methacrylate, trimethyl
aminoethyl methacrylate
chloride) 1:2:0.1
Poly(ethyl acrylate, methyl Aqueous dispersion/30% Swellable, permeable Sustained release
methacrylate) 2:1 with
nonoxynol (1.5%)
Poly(ethyl acrylate, methyl Aqueous dispersion/40% Swellable, permeable Sustained release
methacrylate) 2:1 with
nonoxynol (1.5%)
Poly(ethyl acrylate, methyl Aqueous dispersion/30% Swellable, permeable Sustained release
methacrylate) 2:1 with PEG
stearyl ether (0.7%)
Eudragit
: a technology evaluation
 S. Thakral et al.

Eudragit L 100

Eudragit S 100

Eudragit RL
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12

Eudragit RS
For personal use only.

10 20 30 40
Position (º2theta)

Figure 3. X-ray diffractogram of various Eudragit polymers, Eudragit L 100, S 100, Eudragit RL, and Eudragit RS.

Table 2. Physical properties of different grades of Eudragit [2].

S. No. Eudragit grade Density (g/cm3) Glass transition Minimum film forming Water vapor transmission
temperature (
C) temperature (
C) rate (WVTR) (g/m2.day)

1 Eudragit E 0.811 -- 0.821 ~ 48 - ~ 350 (organic)

2 Eudragit L 100, S 100 0.831 -- 0.852 --* > 85z ~ 150 (redispersed)
3 Eudragit L 30 D-55 1.062 -- 1.072 ~ 110 ~ 25 ~ 100 (10% TEC)
4 Eudragit L 100-55 0.821 -- 0.841 ~ 110
5 Eudragit RL PO 0.816 -- 0.836 ~ 70 ~ 40z ~ 450 (RL 100- organic)
6 Eudragit RS PO 0.816 -- 0.836 ~ 65 ~ 45z ~ 250(RS 100- organic)
7 Eudragit NE 30 D 1.037 -- 1.047 ~9 ~ 5 ~ 300
8 Eudragit FS 30 D 1.058 -- 1.068 ~ 48 ~ 27 ~ 100 (3% TEC)

*Not possible to determine Tg value for Eudragit S 100 and L 100, because of overlapping with the damage of the functional groups at temperatures of more
than 150
C.
z
Includes the minimum film forming temperature of aqueous dispersion.
TEC: Triethyl citrate.

136 Expert Opin. Drug Deliv. (2013) 10(1)

 Eudragit
: a technology evaluation

Eudragit L 100

Eudragit S 100
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12

Eudragit RL
For personal use only.

Eudragit RS

Figure 4. FTIR spectra of different Eudragit polymers. Eudragit L 100, S 100, Eudragit RL and RS.

RS/RL [17], and Eudragit L 100-55 [18]. In these processes,
some polymers with higher glass transition temperature
(Tg) like Eudragit RS, Eudragit L and Eudragit L
100-55 were pre-plasticized with liquid plasticizer using
hot-melt extrusion prior to coating in order to lower
down Tg so as to generate binding force at certain opera-
ting temperature. Powder adhesion to the tablet is
improved by a partially melted polymer that generates
binding force between particles and tablet surface.
. Electrostatic spray powder coating: Used with Eudragit
polymers, namely Eudragit RS and Eudragit E, as
claimed in several US patents by Phoqus Ltd. The coating
powder was obtained by wet granulation followed by
fluid bed drying and micronization using fluid energy
mill. Both the sides of tablets were coated separately using
specialized equipments. Polymer particle fusion was com-
pleted by curing with IR radiation [19]. The said process
has been later shown to exhibit difficulties in coating
tablets with well-defined edges [20].
. A modified coating process based on creation of electri-
cal field by an electrostatic charging gun and grounded
substrate to assist deposition of charged powder particles
has also been reported for coating tablets with Eudragit
RS and RL [21].
These solvent free coating processes, however, need to be
modified to obtain optimized coating [13].
5. Registered products containing Eudragit
A number of formulations employing Eudragit as coating
polymer are being marketed as registered products and these
have been compiled in Table 3.
6. Safety profile of Eudragit
Eudragits, owing to their stability in the presence of digestive
enzymes and body fluids, are known as non-biodegradable

Expert Opin. Drug Deliv. (2013) 10(1) 137

 S. Thakral et al.

Table 3. Marketed products based on Eudragit as coating polymer.

S.No. Active ingredient Trade name Manufactured by Coating polymer Dissolution pH

1 Sulfasalazine Colo-pleon Sanofi-Aventis Eudragit L 100-55 5.5

2 Mesalazine Claversal GlaxoSmthkline Eudragit L 100 > 6.0
Asacol Warnner Chilcott Eudragit S 100 > 7.0
Asacol HD Warnner Chilcott Outer coat combination of >7
Eudragit L 100 and S 100; inner
coat of Eudragit S 100
Salofalk Dr. Falk Pharma Eudragit L 100 > 6.0
Mesasal GSK Australia Eudragit L 100 > 6.0
Calitofalk Dr. Falk Pharma Eudragit L 100 > 6.0
Lialda (USA) Cosmo Pharmaceuticals Eudragit S 100 >7
Mesavant (Europe) Cosmo Pharmaceuticals Eudragit S 100 >7
Mesren MR Teva Pharmaceutical Eudragit S 100 >7
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12

Ipocol Sandoz Eudragit S 100 >7

Apriso Salix Pharmaceuticals Eudragit L 100 > 6.0
3 Budesonide Entocort Prometheus Lab. Drug pellets in ethyl cellulose coated 5.5
with Eudragit L 100-50
Budenofalk Dr. Falk Pharma Eudragit L 100 & Eudragit S 100 6 -- 7
4 Beclomethasone Clipper Chiesi Pharmaceuticals Eudragit L 100/55 5.5
dipropionate

polymers. Eudragit E, basic methacrylate polymer, has been 7.Applications of Eudragit in colon-specific/
demonstrated to be non-toxic and its properties moderated enteric-coated delivery system
For personal use only.

greatly by its lack of absorption as a result of the large effective

molecular weight [22]. Detailed studies of toxicokinetics, acute
and subchronic oral toxicity, genotoxicity, and reproductive
toxicity of Eudragit E confirm absence of significant toxicity
by external and oral routes of exposure. Based on these
reports, it has been proposed that Eudragit E is GRAS
(Generally Regarded As Safe) on the basis of scientific proce-
dures, as discussed at 21 CFR, Section 170.30, with regard to
its use as direct and indirect food ingredients [22]. Similarly,
the median lethal dose (LD50) of anionic methacrylate copo-
lymer (Eudragit FS 30 D) in male and female Sprague-
Dawley rats of CD(SD)BR strain was found to be in excess
of 2,000 mg/kg body weight [23]. No-Observed-Adverse-
Effect-Level (NOAEL) was found to be 400 mg/kg body
weight/day in short term toxicity study conducted for
28 days on male and female Beagle dogs [24], while the same
has been reported as 1,500 mg/kg body weight/day in sub-
chronic oral toxicity study conducted for 26 weeks on male
and female Sprague-Dawley rats [25]. The in vitro cell
mutation assay has demonstrated non-mutagenicity of the
polymer [26].
Methacrylate copolymers are listed in the German Rote
Liste and are being used in pharmaceutical preparations.
In USA, various grades of Eudragit are approved and listed
in US FDA’s “Inactive Ingredients for Approved Drug
Products” list with the maximum potency of these grades
specified with respect to the particular use [27]. Maximum
potency of different Eudragit grades for some of the impor-
tant applications is compiled as Table 4. The polymetha-
crylates are included in nonparentral medicines licensed in
the UK [3].
Eudragits are extensively employed as pH-dependent coating
polymers in order to attain either enteric effect or colon
targeting of drugs. The pH-dependent systems are conven-
tionally designed on the generally accepted view that pH of
the human gastrointestinal tract increases progressively from
stomach (2.0 -- 3.0) to small intestine (6.5 -- 7.0) to colon
(7.0 -- 8.0) [28] (though it has been reported that pH drops
slightly in colon and is highest in ileocecal junction [29]).
Thus, it is expected that the polymer used as coating material
for colon targeting should be able to withstand lower pH
value of upper gastrointestinal tract and disintegrate at neutral
or slightly alkaline pH of terminal ileum, preferentially
ileocecal junction.
Eudragit with its ensemble of polymer grades available
which exhibit a range of dissolution pH profile offer an ingen-
uous method to avoid drug release in upper part of gastroin-
testinal tract. The most commonly employed Eudragit
grades include Eudragit L 100 and S 100. Eudragit L dissolves
at pH > 6 and is used for enteric coating, whereas Eudragit S,
which dissolves at pH > 7 (attributed to the presence of higher
amount of esterified groups in relation to carboxylic groups) is
used for colon targeting. Replacement of the methyl acrylate
with ethyl acrylate in Eudragit L led to introduction of Eudra-
git L 100-55, which dissociates above pH 5.5. On the other
hand, increasing the proportion of esterified group in the
polymer from 50% in Eudragit L to 90% led to introduction
of Eudragit FS 30 D, which is available as aqueous dispersion
and shows dissolution at pH about 6.8 [2,30].
The use of Eudragit S was first described by Dew et al. for
the targeted delivery of drug, for example, 5-amino salicylic

138 Expert Opin. Drug Deliv. (2013) 10(1)


Table 4. Maximum potency for different Eudragit grades for important applications [27].
S.No Grade of Eudragit
1 Eudragit L 100-55
2 Eudragit 30 D
3 Eudragit NE 40 D
4 Eudragit RL 100
5 Eudragit RL 12.5
6 Eudragit RL 30 D
7 Eudragit RS 100
8 Eudragit RS 30 D
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
9 Eudragit RS 12.5
*Maximum potency specifies the maximum amount of inactive ingredient for each route/dosage form for containing that ingredient.
acid (5-ASA) in colitic patients, wherein dosage form disinte-
gration and drug release was observed in distal gut [31,32]. The
results from these studies provided the basis for the develop-
ment and eventual commercialization of a number of modi-
fied release products (Table 3). The colon-targeted drug
For personal use only.
delivery systems using Eudragit have been described for a
number of drugs like insulin [33,34], prednisolone [35], campto-
thecin [36], naproxen [37] and cyclosporine [38]. However, some
in vivo reports revealed that the use of Eudragit S (which dis-
solves at pH > 7) alone is not suitable for colonic delivery [39].
In order to overcome the problem, it was shown that a proper
combination of polymer Eudragit S 100 and Eudragit L
100 ensures that the release of drug from formulation will
occur even when the pH value of the gastrointestinal tract
does not reach more than 6.8 [40]. The combination of these
two polymers ensures that the coating begins to dissolve on
entering small intestine, although thickness of coating pre-
vents complete dissolution of the film and breakdown of the
capsule until further down the gut. Scintigraphic evaluation
of the system in healthy volunteers has demonstrated colon
targeting success rate of 90% [39].
It was shown through in vitro release studies that these
polymers (used alone or in combination) exhibit excellent
protection in gastric pH followed by gradual or sudden
release in alkaline environment in different pH conditions
(6.0 -- 7.4). Some coated formulations, based on Eudragit
FS 30 D, have shown to resist disintegration/dissolution in
upper gastrointestinal tract but have been reported to disinte-
grate after colonic arrival [41-43]. However, studies in human
volunteers have confirmed that since pH drops from 7.0 at
terminal ileum to 6.0 in ascending colon, such systems some-
times fail to release the drug [44]. The use of polymers that
release the drug at higher pH values (> 7.0) may fail to give
reproducible results, since pH in the lower gastrointestinal
lumen (ileum and colon) may fail to exceed the dissolution
pH of the polymer in some patients, for example, in the
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit
: a technology evaluation
Dosage form Maximum potency*
Enteric-coated tablets 17 mg
Enteric-coated pellets 28 mg
Enteric-coated particles 27.9 mg
Capsules 33.8 mg
Sustained action tablets 10 mg
Controlled release tablets --
Sustained release capsules 25.59 mg
Sustained release tablets 25 mg
Sustained release capsules 4.706 mg
Controlled release tablets --
Sustained release capsules 91.88 mg
Sustained release tablets 81.6 mg
Controlled release tablets 14 mg
Controlled release tablets 35.24 mg
case of inflammatory bowel disease [45]. Therefore, coated
systems, in general, may suffer from the drawback of non-
reproducible release in vivo. Extensive studies carried out by
some research groups in the recent past have shown that
tablets coated with Eudragit polymers sometimes demon-
strated erratic performance in vivo, and tablets may fail to
disintegrate inside the human body [46,47]. This has been
previously attributed to the narrow pH gradient between the
small and large intestine, intersubject variability in gastroin-
testinal pH, residence time of dosage form at ileocecal junc-
tion, pH changes, that occur in diseased conditions and
fasted or fed states resulting in variable performance of these
systems [48].
In view of the aforesaid facts, it has been gradually appreci-
ated that the conventional colonic delivery system based only
on Eudragits may not be reliable in vivo because of the inher-
ent variability of pH and emptying times from gastrointesti-
nal tract. The combination of pH- dependent polymers with
polymers exhibiting time-based release has been proposed as
one of the means for achieving controlled release of drug
from the coated system [49]. Further, Eudragits in combina-
tion with biodegradable guar gum [41] and starch [50] have
also been attempted and proven as triggers by microbial deg-
radation for colon-specific release. Thus the focus has recently
shifted to development of suitable targeted formulation based
on Eudragits in combination with other polymeric system.
Some of the significant latest observations in the use of
Eudragits based enteric/colon-targeted systems [33,34,42,47,50-68]
have been summarized in Table 5.
A retrofit study of the Table shows that different methods
for imparting enteric/colon-targeted action have been
exploited. While some of the systems represent Eudragit
coated conventional unit dosage forms like tablets or cap-
sules [47,51,52,54,56,58], recent trends indicate shift toward use
of Eudragit-coated multiparticulate systems which include
microspheres [57,59-63], pellets [50,55,64] or non-pariel seeds
139

Table 5. Compilation of some recent observations of studies conducted using Eudragit as enteric polymer/for colon targeting.
140
Eudragit grade used
Different grades of Eudragit used alone
Eudragit S 100
Eudragit L 100
Eudragit S (ethanolic),
Eudragit S (aqueous
dispersion) or Eudragit FS
30 D
Eudragit L 30 D-55 or
Eudragit FS 30 D
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit S 100
Eudragit S 100 or L 100
Eudragit S (ethanolic),
Eudragit S
(aq dispersion) or E FS
30 D
Eudragit grades used in combination
Eudragit L 100 and S 100
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
Mechanism employed
Drug entrapped microspheres
prepared by double emulsion
solvent evaporation
Drug entrapped microspheres
prepared by double emulsion
solvent evaporation
Drug tablets coated with
Eudragit dispersions (5% w/w),
tablets radiolabelled with 90mTc
HPMC capsules coated with
either of the two polymers;
different coating thickness
employed
Drug tablets coated with
different amounts of polymer;
different other polymers also
employed
Drug binder suspension sprayed
on non-pareil seeds, then
coated with either grade of
Eudragit
Drug tablets coated with
Eudragit dispersions (5% w/w)
For personal use only.
Model drug Type of drug release Results obtained Ref.
study conducted
S. Thakral et al.
Insulin In vivo (rabbit; blood Prominent hypoglycemic effect; [33]
glucose level)
Insulin In vitro Retard release at low pH, fast release [34]
at pH 7.4
Prednisolone In vivo (human volunteers Disintegration of Eudragit S (aq) [47]
by gamma scintigraphy) coated tablets in proximal to mid small
intestinal regions
Disintegration of Eudragit S (organic)
coated tablets: inconsistent, in
ileocecal junction or ascending colon
Disintegration of Eudragit FS 30 D
coated tablets: consistent in ileocecal
junction or ascending colon
Paracetamol In vitro pH gradient 1.2 Eudragit L 30 D-55, rapid drug release [51]
(2 h), 6.8(1 h), 7.4(2 h) at pH 6.8
In vivo (human Eudragit FS 30 D rapid drug release at
volunteers) pH 7.4
Eudragit L 30 D-55: Complete capsule
disintegration in small intestine
Eudragit FS 30 D complete capsule
disintegration in proximal colon, avg
time 6.9 h post dose
Indomethacin In vitro Increasing coat thickness showed [52]
reduced dissolution rate of drug
Indomethacin In vitro pH gradient, No drug release at pH 1.2 and 6.5, [53]
1.2 (2 h), 6.5(1 h), 6.8 slow release at pH 6.8, and fast at pH
(2 h), and 7.2(1 h) 7.2
Prednisolone In vitro Drug release rapid and equivalent from [54]
tablets coated with Eudragit S and
Eudragit FS in PBS pH 7.4
Discriminating in Sorenson buffer (pH
7.0) as Eudragit S (aq) > Eudragit
FS > Eudragit S (organic)
5-ASA In vitro [55]

Table 5. Compilation of some recent observations of studies conducted using Eudragit as enteric polymer/for colon targeting (continued).
Eudragit grade used
Combination of Eudragit as coating material with other polymers
Eudragit FS 30 D
Eudragit as coating material with polymeric cores
Eudragit FS 30 D
Eudragit S 100
Eudragit L 100 and S 100
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit L 100
Eudragit S 100
Eudragit S 100
141
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
Mechanism employed
Pellets coated with different
ratios of Eudragit
pH and enzyme system obtained
by coating guar gum and
Eudragit FS 30 D sequentially
onto drug loaded pellets in
fluidized bed dryer
Drug-binder (HPMC)-beta-
cyclodextrine as solubilizer
solution layered on non-
pariel seeds and then coated
with Eudragit (15% w/w)
Pectin matrix tablets coated
with Eudragit (total weight gain
27%)
Glutaraldehyde cross-
linked chitosan microspheres
coated with Eudragit
Drug tablets prepared with
matrix of different
polysaccharides in combination
with methacrylic acid-guar gum
graft polymer (MAA-g-GG).
Tablets coated with Eudragit L
100
Pectin microspheres of drug
coated with Eudragit
Sodium alginate microspheres
coated with Eudragit S 100
For personal use only.
Model drug Type of drug release Results obtained Ref.
study conducted
Effect of combination ratios, coating
thickness and pH dependent drug
release
Indomethacin In vitro; pH gradient Only 5% drug release in pH medium [50]
(1.2 (2 h), 6.8 (2 h), 7.4 after 2 h showing retarding effect
7.4 (1h) and, 6.5 (15 h) of guar gum, enzyme
In vivo (beagle dogs) (galactomannase) dependent drug
release found at pH 6.4
Prolonged drug plasma peak
concentration time and absorption lag
time
Meloxicam In vitro pH dependent drug release with [42]
In vivo sufficient gastric resistance
(beagle dogs) Delayed onset of drug absorption
reduced AUC (0 -- 96 hr)
Theophylline In vitro (pH Identification of high methoxylated [56]
gradient: 1.1 (2 h), pectin as the most suitable candidate
6.8 (2 h), 7.4 (10 h) for colon delivery
Metronidazole In vitro No drug release in acidic pH, presence [57]
of fecal rat contents led to higher drug
release
Metronidazole In vitro (simulated colon Tablets prepared with guar gum and [58]
fluid containing 40% MAA-g-GG showed 70% drug release,
fecal rat content) which was reduced to 18-20% upon
enteric coating
5-Fluorouracil In vitro No drug release at pH 1.2 and 4.5 but [59]
Organ distribution study fast at pH 7.4
in rats Coated microspheres showed
negligible drug in stomach or small
intestine and ~ 100% drug in colon
5-Fluorouracil In vivo (rats) No drug release in stomach and small [60]
intestine; Reduced side effects of drug
observed
Eudragit
: a technology evaluation
 Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
For personal use only.

142
S. Thakral et al.

Table 5. Compilation of some recent observations of studies conducted using Eudragit as enteric polymer/for colon targeting (continued).

Eudragit grade used Mechanism employed Model drug Type of drug release Results obtained Ref.
study conducted

Eudragit S 100 Chitosan microspheres coated Aceclofenac In vitro ~ 96% drug released in simulated [61]
with Eudragit S In vivo (rats) colonic fluid (enzyme induced)
Prolonged effect of drug and
significant anti-inflammatory response
observed
Eudragit S 100 Calcium pectinate microspheres Curcumin In vitro Significantly increased drug release in [62]
coated with Eudragit S the presence of 1% rat cecal contents,
Eudragit S 100 Core of chitosan (as Valdecoxib In vitro, pH gradient: No drug release at lower pH. Release [63]
mucoadhesive polymers), coated 2(2 h), 5.5 (2 h), of drug content only at pH 7
with Eudragit 6.8 (2 h), 7.4 (8 h)
Eudragit FS 30 D Pellet cores of chitosan and Caffeine In vivo (human Time of appearance of drug in [64]
microcrystalline cellulose volunteers) saliva (considered as lag time)
prepared by extrusion and then 6.95 ± 1.12 hrs
coated with Eudragit FS 30 D
(TWG ~ 29%)
Eudragit as core matrix in combination with other polymers
Eudragit L 100 and S 100 Incorporated Eudragit in matrix Indomethacin In vitro Drug release reduced in acidic and [65]
composed of polycarbophil and In vivo (human by gamma weakly acidic medium but improved in
carbopol scintigraphy) alkaline medium

Expert Opin. Drug Deliv. (2013) 10(1)

Mean colonic residence time 15 -- 19 h
Eudragit S 100 Nanocapsules of drug prepared Prednisolone In vitro Lag time of 4 -- 5 h [66]
with Eudragit S 100 using In vivo (rats) Lag time 3 h corresponding to arrival
nanoprecipitation method of contents in colon
Eudragit S 100 Microspheres of ethyl cellulose Mesalamine In vitro Drug release only at higher pH [67]
and Eudragit S containing drug
prepared; formulation variables
optimized
Eudragit L 100 and S Drug containing Eudragit Indomethacin In vivo, (rabbit by gamma System releases drug in the lower part [68]
100 (1:2) multiparticulates filled in hard scintigraphy) of gastrointestinal tract only after a
gelatine capsules and sealed programmed lag time, employing
with hydrogel plugs employing different hydrogel plugs
different polymers

containing drug [42,53]. Alternatively, colon-targeted formula-
tion may be presented as Eudragit-based multiparticulate
system, presented in the form of microcapsules prepared using
techniques like double emulsion solvent evaporation, extru-
sion spheronization, spray drying [33,34,68], as nanocapsules
prepared by nanoprecipitation [66], and as matrix [65] or
microspheres [67] in combination with other suitable poly-
mers. In addition to above, Eudragit S 100 based tablets
have been prepared by hot-melt extrusion to target drug deli-
very to the colon and the drug release profiles of the extruded
tablets were found to fit both the diffusion and surface erosion
models [70]. Recently, a double coating enteric system com-
prising of inner coat (partially neutralized Eudragit L
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
30 D-55 and an organic acid) and an outer coat (standard
Eudragit L 30 D-55) has been shown to achieve rapid drug
release in proximal small intestine. The improved dissolution
of the system, attributed to increased ionic strength and
buffer capacity of its inner layer, has been demonstrated for
in vitro studies, while in vivo study showed a more consistent
disintegration in proximal small intestine for the double-
layered system as compared to conventional single enteric
coating [71,72].
8. Application of Eudragit in sustained
For personal use only.
release delivery system
By employing Eudragits as release-manipulating excipients, it
is possible to achieve modified drug release either through
polymeric coating on the drug reservoir core, or through the
use of polymeric matrix incorporating the drug itself.
8.1 Through sustained release coating
The grades of Eudragit which are water insoluble, but
swellable over the range of physiological pH are suitable for
the sustained release film coating applications and include
Eudragit RL (highly permeable), Eudragit RS (low perme-
able), Eudragit NE (permeable), and Eudragit NM (perme-
able) [73]. Eudragit RL and RS have quaternary ammonium
groups in the chloride salt form, and the dissociation of these
groups in aqueous media is responsible for the swellability and
permeability of the polymers [74]. Eudragit RL includes a
greater concentration of the quaternary ammonium groups
and the coatings made from this polymer are more permeable
than those which are made from Eudragit RS. The sustained
release Eudragit polymer can be used as coating materials
for tablets [75], pellets and microspheres or capsules [74]. Often,
Eudragit RS and (or) RL are used as coating materials to
create sustained release drug forms from such active sub-
stances like ibuprofen, indomethacin, nitrendipine, diltiazem,
and others [74].
The mechanism of drug release from dosage forms coated
with Eudragit RS and RL mixtures has been proposed to be
through control of fluid permeation into the core and subse-
quent dissolution and outward diffusion of the active
substance [76]. The pores in the film have been shown to be
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit
: a technology evaluation
larger and the diffusion of the drug through these pores is
higher in Eudragit RL films than in Eudragit RS films.
Drug diffusion has been shown to be dependent upon the
size of drug and steric effects [77] and also on ionic strength
and buffer species of the dissolution medium [78,79]. Further,
the drug release from dosage forms formulated with Eudragit
RS and RL films has been shown to be pH independent
attributed to ionization of quaternary ammonium groups at
all pH levels occurring in the gastrointestinal tract.
The drug release from dosage forms coated by these poly-
mers may be modified by addition of a wide range of other
excipients. To increase the permeability of film, various
water-soluble substances like sucrose, lactose and other
saccharides, starch, micronized cellulose, soluble cellulose
ethers, poly(vinylpyrrolidone), polyethylene glycol or its
derivatives, and fumed or precipitated silica can be added.
For instance, the coating permeability from low permeable
Eudragit RS has been shown to increase with the addition of
inulin to the film [49]. Eudragit RL and RS, which are miscible
in all proportions, have been used to adjust the drug release in
different sustained release coating applications [73]. Addition
of 200% talc to Eudragit RS/RL 30 D 95:5 plasticized with
triethyl citrate provided sustained release of drug and the dos-
age form has been shown to be non-agglomerating, physically
stable, and without significant change in drug release after
storage for a period of 3 months [80].
Eudragit RL and RS may also be combined with other
Eudragit polymers to achieve the desirable dissolution profile.
Eudragit RL 30 D and RS 30 D in combination with
Eudragit FS 30 D were used as coating materials to produce
sustained release pellets of 5-ASA for the colon targeting [74].
Different ratios of Eudragit NE 30 D and Eudragit L
30 D-55 were tested as the coating materials for drug-layered
beads using verapamil-hydrochloride as the model drug. The
lag time observed with two suitable ratios of polymers, that
is, 75:25 and 80:20, was found to be 3 h and 6 h, respectively.
Generally, the lag time increased and drug release decreased
with increasing amount of Eudragit NE 30 D in the polymer
blend [81].
The neutral Eudragit NE and NM polymer, commercially
available as aqueous dispersion, could also be employed as
coating material to develop water-insoluble, permeable (pH-
independent) formulation. The main difference between both
these dispersions is in the nature and content of emulsifier
(Eudragit NE 30 D contains nonoxynol 100 (1.5% w/v) and
Eudragit NM 30 D contains polyethylene glycol stearyl ether
(0.7%)). The films formed by these polymers are highly flexible
and do not need addition of a plasticizer. These films are insol-
uble in gastrointestinal tract, show very low permeability and a
pH-independent swelling. For coating, anti-tacking agents are
used to reduce the stickiness of the polymeric dispersion.
Drug pellets sub-coated with ethyl cellulose and outer coated
with Eudragit NE 30 D (containing small amount of drug)
have demonstrated initial immediate-release of the drug
dispersed in the outer coat and subsequently the desired
143
 S. Thakral et al.
sustained release of the drug from the pellets [82]. Stability
problems have been reported with the nonoxynol 100, in the
form of crystallization of the surfactant upon storage at room
temperature leading to increase in drug release rate [83].
8.2 Through swellable matrix
Eudragits are attractive matrix forming materials, due to their
high chemical stability, good compatibility properties, and
large variety of available grades with different physicochemical
characteristics. Eudragit polymers are known to form a
swellable matrix, wherein drug release is controlled by conti-
nuously changing dimension of the diffusive barrier. This
barrier is the layer thickness externally formed on the matrix
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
that controls active substance transport through it. The
swellable matrices are examples of typical moving boundary
release systems. Matrix tablets containing Eudragit polymer
can be manufactured by direct compression [84], wet
granulation [85] or melt extrusion [86].
Direct compression has been extensively utilized as a
method for the preparation of Eudragit-based matrix tablets.
Ceballos and co-workers prepared extended-release theophyl-
line matrix tablets by a direct compression of drug and differ-
ent pH-dependent (Eudragit L 100, S 100 and L 100-55) and
time-dependent (Eudragit RL PO and RS PO) polymer
For personal use only.
combinations. Matrix tablets based on L 100/RL PO and L
100/RS PO mixtures gave the best results, displaying the
highest percentage of theophylline release and the matrix for-
mulation allowed to obtain the more regular release profiles.
This was achieved by the combination of the good erodible
properties of L 100 with the swelling properties of RL PO
and RS PO polymers [87]. Colo and co-workers reported
that compressed matrix tablets based on a pH-sensitive poly
(ethylene oxide) and Eudragit L 100 compounds ensured a
complete release of the active substance during the transit
from stomach to jejunum, unaffected by gastric pH fluctua-
tions. Release in the gastric fluid was controlled by matrix
swelling and/or drug dissolution, whereas matrix dissolution
controlled release in simulated jejunum fluid [88]. Inert matrix
tablets of carteolol hydrochloride can be prepared from
Eudragit RS as a supporting material with different fillers
and wetting liquids, which include mannitol, polyethylene
glycol 6000, and Emcompress as fillers and Eudragit L
12.5 as a wetting liquid. The two-phase release profile has
been accounted for as the release of a drug on the surface of
a tablet and the particles of the drug which are not completely
surrounded by the Eudragit, during the first phase and the
release of drug contained in the inert matrix during the second
phase [89].
Melt extrusion as a method for producing the sustained
release pellets of poly (meth) acrylates is practicable since Eudra-
gits are thermoplastic polymers, their physiochemical properties
such as melt viscosity, glass transition temperature, and temper-
ature stability are ideal for use in melt extrusion [90-93]. Further,
melt extruded matrix systems provide a strong controlled release
effect due to very dense structure and molecular dispersion of
144 Expert Opin. Drug Deliv. (2013) 10(1)
the drug in polymer [94]. Based on low glass transition temper-
ature of Eudragit RL and RS, these polymers can be processed
without plasticizer. However, to enable even lower melt extru-
sion temperature or less shear stress, plasticizer such as triethyl
citrate, triacetin, dibutyl sebacate, or polyethylene glycol
6000 can be used. As solid state plasticizer, citric acid was iden-
tified for Eudragit RS as effective plasticizer [95]. In sustained
release applications, the influence of plasticizer type and con-
centration on dissolution properties needs to be ensured. For
solubility enhancing formulations, hydrophobic plasticizer
may actually cause decrease in dissolution, whereas surfactant
can additionally improve solubility enhancing effect.
9.Applications of Eudragit in taste masking
and protective system
Eudragit polymers have been investigated for their possible
applications in taste masking formulations and as protective
formulation. Particularly cationic Eudragit E is well suited
for taste masking applications formulated as fast dissolving
tablets. Due to presence of tertiary amino group as functional
unit, it forms films that are swellable and permeable, yet insol-
uble, at pH 5 or higher, but dissolves rapidly by forming salts
at acidic pH values lower than 5. This polymer can prevent
the release of the delivered drug in saliva (pH 6.8 -- 7.4) and
readily dissolves in gastric fluid (pH 1.0 -- 1.5) [96]. Alterna-
tively anionic Eudragit LD 30 D-55 and cationic RL/RS
30 D also have taste masking properties. Since these polymers
have other specific functionalities (gastro-resistance or retar-
dation) the polymer application is advised to be used as low
as possible [2]. Small particles such as crystals, granules, and
pellets were coated with aqueous dispersions of methacrylic
acid and methacrylic ester copolymers (Eudragit RL 30 D,
RS 30 D, L 30 D-55, and NE 30 D) for taste masking and
compressed into fast dissolving tablets [97]. The fast dissolving
tablets, containing the taste-masked granules of pirenzepine
HCl or oxybutynin HCl, were prepared by coating the drugs
with Eudragit E 100 using the extrusion method. Drug release
from these Eudragit E based granules was shown to be negli-
gible even after 8 h at pH 6.8 and none of the six volunteers
reported any bitter taste upon administration of the fast
dissolving tablet [96]. Taste-masked immediate release micro-
matrix powders were formed by spray drying the drug and
cationic copolymer with the drug: polymer ratio 1:4, prefera-
bly 1:6 [98]. Drug release was shown to be < 5% in medium
representing pH of saliva when linezolid was presented as
microcapsules prepared by coacervation and subsequent
membrane coating on the microcapsules with Eudragit L
30 D [99]. Indinavir loaded Eudragit E microparticles were
prepared by double emulsion/solvent evaporation and sensor-
ing test by ten volunteers indicated that systems containing
15% of the drug displayed acceptable taste, though drug
loading as high as 90% was possible [100].
Further, Eudragit E coatings are also characterized by low
water permeability and this polymer has been demonstrated

to be an effective moisture protective film coating [101]. Bley
and co-workers determined glass transition relative humidity
for different polymers including Eudragit E through a combi-
nation of differential scanning calorimetry and dynamic vapor
sorption techniques and showed that this polymer remains in
glassy state in the moisture protective film coatings [102]. Cao
and co-workers reported effective moisture protection of silica
particles when coated with the novel Eudragit E aqueous
dispersion [103]. However, some of the studies have questioned
the effectiveness of low permeable Eudragit E barrier film
in the actual prevention of moisture-related deterioration of
drugs using aspirin as model drug [104].
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
10. Incompatibilities associated with Eudragit
Though Eudragit polymers are regarded as chemically stable,
incompatibilities of Eudragit polymers with few active ingre-
dients have been documented in literature. As an example,
incompatibility of Eudragit RS and RL with diflunisal, flurbi-
profen, and piroxicam has been reported. It has been shown
that, except for mechanical dispersion, these drugs interacted
with Eudragit matrices by virtue of electrostatic interactions
with the ammonium groups present in the polymer [105,106].
Physical and chemical interaction with the carboxylic group
For personal use only.
of ibuprofen has been reported to occur because of electro-
static interactions and/or hydrogen bonding with the quater-
nary ammonium groups in Eudragit RL. This probably
inhibits uniform dispersion of the drug in the polymer
network and ultimately affects the drug loading and release
profile in vitro and in vivo [107]. Through diffuse reflectance
infrared Fourier transform spectroscopy, mild interaction,
such as hydrogen bonding, has been suggested between
protonated tertiary amine group of the ranitidine and a
functional group on the Eudragit E 100 polymer [108].
Incompatibilities can also occur with certain polymethacry-
late dispersions depending upon ionic and physical properties
of the polymer and solvent. For example, coagulation may be
caused by soluble electrolytes, pH changes, some organic
solvents, and extremes of temperatures. Dispersion of Eudra-
git L 30 D, RL 30 D, L 100-55 and RS 30 D are incompat-
ible with magnesium stearate (thickening or coagulation),
though magnesium stearate contained in tablets does not
affect film properties [3,109]. Solid polymethacrylates and
organic solution are generally more compatible than
aqueous dispersions.
11. Conclusions
The present review shows that Eudragit represents a group of
synthetic polymethacrylate copolymers, used as functional
excipient in various pharmaceutical dosage forms. Eudragit
polymers, commercially available as granules, powder, organic
solution, or aqueous dispersions, have been widely used as
coating materials in order to achieve either modification of
drug release behavior or taste masking. The incompatibilities
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit
: a technology evaluation
between Eudragit polymers (mostly aqueous dispersions)
and active ingredients are few and defined. The safety associ-
ated with use of Eudragits makes them attractive candidates
for optimizing the existing dosage forms and developing the
new ones.
12. Expert opinion
Polymers have played indispensable role in pharmaceutical
development and manufacturing by facilitating development
of robust medicinal products which deliver the drug at desired
site of action in optimum therapeutic concentration. While
natural polymers (like pectin, shellac, starch) are biocompati-
ble, some are expensive to produce and refine and also suffer
from batch to batch variability in terms of physicochemical
properties, based on source of raw materials. On the other
hand, synthetic polymers have excellent reproducibility and
hence have clear advantage over natural polymers. Eudragits
represent group of polymethacrylate based polymers, con-
taining methacrylic acid and methacrylic or acrylic esters or
their derivatives in varying proportions. Being a synthetic
polymer, Eudragits display good reproducibility and other
advantages associated with synthetic polymers. Further, these
are regarded as non-biodegradable, non-absorbable, and
non- toxic functional excipients, thus circumventing issues
accompanying synthetic polymers.
Anionic Eudragits, represented by Eudragit L and
Eudragit S, have been extensively employed as coating mate-
rial to evade drug release in stomach and facilitate the release
in small intestine or in the colonic regions. A number of
products based on Eudragit S alone or on a combination of
Eudragit L and S are already in the market. The products
have been launched based on success stories demonstrating
dosage form disintegration and drug release in distal gut.
However, some recent studies have highlighted variability in
the performance of some marketed preparations and in few
cases, failure of dosage form to release the drug, which among
other factors, have been attributed to pH being less than 7 in
the ascending colon. Various strategies have been proposed to
overcome this limitation, which includes the use of Eudragit
FS rather than Eudragit S (threshold dissolution pH of former
being 6.8 rather than 7), use of combination of Eudragit L
and Eudragit S to facilitate drug release in intestinal environ-
ment of pH less than 7, combination of Eudragit based
pH-mediated release with either pre-programmed time-based
or microflora-based release mechanisms utilizing suitable
polymers. Further, with the recent trend toward shifting
from single-unit to the multiple-unit design, many more
success stories employing Eudragit for colon targeting are
expected in the coming future.
Neutral Eudragit polymers RL and RS are considered to be
important functional excipients to achieve sustained drug
release. These two polymers demonstrate contrastingly
distinct release profiles and can be mixed in any proportions
to adapt permeability of coating to technological and
145
 S. Thakral et al.
pharmacokinetic requirements. However, processing of these
polymers is known to be associated with tackiness, which
is frequently circumvented using talc. Use of talc in coating
formulations is known to be associated with processing
limitations, like clogging of spray nozzles, incompatibility
with certain drugs. Agglomeration and sticking of pellets
have been demonstrated with the use of high curing tempera-
ture used in the coating. This ultimately led to the damage
to film coating and faster drug release. These processing
difficulties need to be optimized before use of polymer in
sustained release formulation transforms into industrial
application.
Cationic Eudragit E finds applications for taste masking
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
of bitter drugs in the formulation of fast dissolving tablets.
The polymer prevents release of the delivered drug in the
near neutral saliva and readily dissolves in the acidic gastric
Bibliography
Papers of special note have been highlighted as
either of interest () or of considerable interest
() to readers.
1. Elias HG. Makromolecukule. Volume 1
Chemische struktur und syntheses. 9.
6th edition. P 303ff Wiley-VCH;
For personal use only.
Weinheim: 1999
2. Evonik: Eudragit Application Guidelines
11th editoin, 09/2009. Available from:
http://www.pharma-polymers.com/
pharmapolymers/en/downloads
3. Rowe RC, Sheskey PJ, Weller PJ.
10.
Handbook of pharmaceutical excipients.
4th edition. The Pharmaceutical Press;
London: 2003
4. Dittgen M, Durrani M, Lehmann K.
Acrylic polymers: a review of
pharmaceutical applications. .
STP Pharm Sci 1997;7(6):403-37
5. Sauer D. An investigation of formulation 11.
factors and processing parameters for the
powder-coating of tablets. The University
of Texas; Austin: 2008
6. Sharma M, Sharma V, Panda AK,
Majumdar DK. Development of enteric
submicron particle formulation for oral 12.
delivery of papain. Int J Nanomedicine
2011;6:2097-111
7. Lin SH, Yu HL. Microscopic fourier
transform infrared/differential scanning
13.
calorimetry system used to study the
different thermal behaviours of
polymethacrylate copolymers of Eudragit
RS, RL, E 30D or E. J Appl Polym Sci
14.
2000;78:829-35
8. Tu J, Shen Y, Mahalingam R, et al.
Polymers in oral modified release
systems. Chapter 5. In: Wen H, Park K,
146
environment. For the purpose, it needs to be ensured that
the dosage form is entirely coated and that the coating’s layer
thickness is quite sufficient to prevent drug dissolution in
saliva and mask the taste.
To summarize, Eudragits are nontoxic synthetic polymers
providing adequate scope for manipulating release profile
through the use of different grades in combination. Certain
processing difficulties and few incompatibilities with active
ingredients need to be taken care of before utilizing them as
functional excipient in the formulation of modified release
dosage form.
Declaration of interest
The authors state no conflict of interest and have received no
payment in preparation of this manuscript.
editiors Oral controlled release regulated release system.
formulation design and drug delivery: J Control Release 1998;51:179-84
theory to practice. John Wiley and Sons; 15. Pearnchob N, Bodmeier R. Dry powder
New Jersey: 2010. p. 71-87 coating of pellets with micronized
O’Donnel PB, McGinity JW. Eudragit RS for extended drug release.
Mechanical properties of polymeric films Pharm Res 2003;20:1970-6
prepared from aqueous polymeric
16. Cerea M, Zheng W, Young CR,
dispersions. In: McGinity JW, editior McGinity JW. A novel powder coating
Aqueous polymeric coatings for process for attaining taste masking and
pharmaceutical dosage forms. 2nd moisture protective films applied to
ednition. Marcel Dekker Inc; New York: tablets. Int J Pharm 2004;279:127-39
1993. p. 517-48
17. Zheng W, Cerea M, Sauer D,
Lin SY, Chen KS, Run-Chu L. Organic McGinity JW. Properties of theophylline
esters of plasticizers affecting the water tablets powder-coated with methacrylate
absorption, adhesive property, glass ester copolymers. J Drug Deliv
transition temperature and plasticizer Sci Technol 2004;14:319-25
permanence of Eudragit acrylic films.
18. Sauer D, Zheng W, Coots LB,
J Control Release 2000;68:343-50
McGinity JW. Influence of processing
Reports effect of plasticizers on the
parameters and formulation factors on
physical properties of Eudragit film
the drug release from tablets
Chang RK, Hsiao C. Eudragit RL and powder-coated with Eudragit L 100-55.
RS pseudolatices: properties and Eur J Pharm Biopharm 2007;67:464-75
peformance in pharmaceutical coating as
19. Whiteman M, Hallett MD, Feather DH,
a controlled release mechanism for
et al. Electrostatic application of powder
theophylline pellets. Drug Dev
material to solid dosage forms.
Ind Pharm 1989;15:187-96
WO061841; 2003
Cole G, Hogan J, Aulton M.
20. Hallett MD. Method and apparatus for
Pharmaceutical coating technology.
applying powder in a pattern to a
Taylor and Francis; London:
substrate. US20060099350; 2006
1995. p. 1-5
21. Qiao M, Luo Y, Zhang L, et al.
Bose S, Bogner RH. Solvent less
Sustained release coating of tablets with
pharmaceutical coating processes:
Eudragit RS/RL using a novel
a review. Pharm Dev Technol
electrostatic dry powder coating process.
2007;12:115-31
Int J Pharm 2010;399:37-43
Fahie BJ, Nangia A, Chopra SK, et al.
22. Eisele J, Haynes G, Rosamilia T.
Use of NMR imaging in the
Characterisation and toxicological
optimization of a compression-coated
behaviour of Basic Methacrylate
Expert Opin. Drug Deliv. (2013) 10(1)

Copolymer for GRAS evaluation.
Regul Toxicol Pharmacol 2011;61:32-43
23. Nunziata A. Praparat 12991/1 (F) aus
Plex 4110: Acute oral toxicity study in
the rat (Study number 5090, Research
Toxicology Centre SpA, Via Tito Speri
12, 00040 Pomezia (RM), Italy) (1995)
24. Eileraas M. Eudragit FS 30 D: 4 week
oral toxicity study in dogs (Study 8101,
Research Toxicity Centre SpA,
00040 Pomezia (RM) (2004)
25. Venturella S. Eudragit FS 30D Freeze
Dried: 26 week oral toxicity study in the
rat followed by 4 week recovery period
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
(Report 7250/T/346/2000, Research
Toxicology Centre SpA, 00040, Pomezia
(RM), Italy (2000)
26. Wollny HE. Cell mutation assay at the
thymidine kinase locus (TK+/-) in mouse
lymphoma L5178Y cells with Eudragit
FS 30 D freeze dried (Study 689302,
RCC Cytotest Cell Research GmbH,
64389 Robdorf, Germany) (2001)
27. FDA, Centre for Drug Evaluation and
Research, Inactive Ingredients for
For personal use only.
Approved Drug Products. Available
from: http://www.accessdata.fda.gov/
scripts/cder/iig/index.cfm [Accessed
15 September 2012]
28. Davenport HW. Physiology of the
digestive tract. 3rd edition. Year Book
Medical Publishers; New York: 1971
29. Evans DF, Pye G, Bramley R, et al.
Measurement of gastrointestinal pH
profiles in normal ambulant human
subject. Gut 1988;29:1035-41
30. Basit AW. Advances in colonic drug
delivery. Drugs 2005;65:1991-2007
31. Dew MJ, Hughes PJ, Lee MG, et al. An
oral preparation to release drugs in
human colon. Br J Clin Pharmacol
1982;14:163-9
32. Dew MJ, Ryder REJ, Evans N,
Rhodes J. Colonic release of
5-aminosalicylic acid from oral
preparation in active ulcerative colitis.
Br J Clin Pharmacol 1983;16:185-7
.. Pioneer report on the successful use of
Eudragit S 100 as coating material to
achieve colon targeting.
33. Jain D, Panda AK, Majumdar DK,
Eudragit S. 100 entrapped Insulin
microspheres for oral delivery.
AAPS Pharm Sci Tech 2005;06:E100-7
34. Jain D, Panda AK, Majumdar DK.
Insulin loaded Eudragit
L100 microspheres for oral delivery:
preliminary in vitro studies.
J Biomater Appl 2006;21(2):195-211
. Protection of therapeutic protein
against proteolytic degradation in
small intestine and delivering the drug
to colon for hypoglycemic activity
35. Thomas P, Richards D, Richards A.
Absorption of delayed release
prednisolone in ulcerative colitis and
Crohn’s disease. J Pharm Pharmacol
1985;37:757-8
36. Thakral NK, Ray AR, Bar-Shalom D,
et al. Soluplus-solubilized citrated
camptothecin-a potential drug delivery
strategy in colon cancer.
AAPS PharmSciTech 2012;13(1):59-66
37. Hardy JG, Evans DF, Zaki I, et al.
Evaluation of an enteric coated naproxen
tablet using gamma scintigraphy and pH
monitoring. Int J Pharm 1987;37:245-50
38. Kim CK, Shin HJ, Yang SG, et al. Once
a day oral dosing regimen of cyclosporine
A: combined therapy of cyclosporine a
premicroemulsion concentrate and
enteric coated solid-state
premicroemulsion concentrates.
Pharm Res 2001;18:454-9
39. Watts PJ, Illum L. Colonic drug
delivery. Drug Dev Ind Pharm
1997;23:893-913
40. Khan MZ, Prebeg Z, Kurjakovic N.
A pH dependent colon targeted oral drug
delivery system using methacrylic acid
copolymers. I manipulation of drug
release using Eudragit L 100-55 and
Eudragit S100 combinations.
J Control Release 1999;58:215-22
. Demonstrated effect of coating
thickness, pH of dissolution medium
to manipulate drug release for
Eudragits in combination
41. Ji C, Xu H, Wu W. In vitro evaluation
and pharmacokinetics in dogs of guar
gum and Eudragit FS 30-D
coated-colon-targeted pellets of
indomethacin. J Drug Target
2007;15:123-31
42. Gao C, Huang J, Jiao Y, et al. In vitro
release and in vivo absorption in beagle
dogs of meloxicam from Eudragit FS
30 D-coated pellets. Int J Pharm
2006;322:104-12
43. Li Y, Li HJ, Yang GR, et al.
Colon-specific delivery tablets of sodium
4-amino salicylic acid. Yao Xue Xue Bao
2006;41:927-32
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit
: a technology evaluation
44. Chu JS. Advances in colon specific drug
delivery system employing CODESTH,
The Drug Delivery Companies Report,
Autumn/Winter Pharmaventure Ltd
(2003)
45. Nugent SG, Kumar D, Rampton DS,
et al. Intestinal luminal pH in
inflammatory bowel disease: possible
determinants and implications for
therapy with aminosalicylates and other
drugs. Gut 2001;48:571-7
46. Safdi AV. Determination of 5-ASA in
whole or partial mesalamine
delayed-release tablets recovered from
fecal samples of healthy volunteers.
Am J Gastroenterol 2005;100:S159
.. Reported probable failure of
disintegration of Eudragit S
100 coated tablet in some cases
47. Ibekwe VC, Lui F, Fadda HM, et al. An
investigation into the in vivo
performance variability of pH responsive
polymers for ileo-colonic drug delivery
using gamma scintigraphy in human.
J Pharm Sci 2006;95:2760-6
48. Friend DR. Colon-specific drug delivery.
Adv Drug Deliv Rev 1991;7:149-99
49. Akhgari A, Farahmand F, Afrasiabi GH,
et al. Permeability and swelling studies
on free films containing inulin in
combination with different
polymethacrylates aimed for colonic drug
delivery. Eur J Pharm Sci
2006;28:307-14
50. Ibekwe VC, Khela MK, Evans DF,
Basit AW. A new concept in colonic
drug targeting: a combination of pH
responsive and bacterially triggered drug
delivery technology.
Aliment Pharmacol Ther 2008;28:911-16
51. Cole ET, Scott RA, Connor AL, et al.
Enteric coated HPMC capsules designed
to achieve intestinal targeting.
Int J Pharm 2002;231:83-95
52. Sinha VR, Kumria R. Coating polymers
for colon specific drug delivery:
a comprehensive 1 in vitro evaluation.
Acta Pharm 2003;53:41-7
53. Akhgari A, Garekani HA, Sadeghi F,
Azimaie M. Statistical optimization of
indomethacin pellets coated with pH
dependent methacrylic polymers for
possible colonic drug delivery.
Int J Pharm 2005;305:22-30
54. Ibekwe VC, Fadda HM, Parsons GE,
Basit AW. A comparative in vitro
assessment of the drug release
147
 S. Thakral et al.
performance of pH-responsive polymers
for ileo-colonic delivery. Int J Pharm
2006;308:52-60
55. Cheng G, An F, Zou MJ, et al. Time
and pH-dependent colon specific drug
delivery for orally administered
diclofenac sodium and 5-aminosalicylic
acid. World J Gastroenterol
2004;10:1769-74
56. Mura P, Marstrelli F, Cirri M, et al.
Development of enteric coated pectin
based matrix tablets for colonic delivery
of theophylline. J Drug Traget
2003;11:365-71
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
57. Chourasia MK, Jain SK. Design and
development of mutiparticulate system
for targeted drug delivery to colon.
Drug Deliv 2004;11:201-7
58. Mundargi RC, Patil SA, Agnihotri SA,
Aminabhavi TM. Development of
polysaccharide based colon targeted drug
delivery systems for the treatment of
amoebiasis. Drug Dev Ind Pharm
2007;33:255-64
59. Paharia A, Yadav AK, Rai G, et al.
For personal use only.
Eudragit-coated pectin microspheres of
5-fluorouracil for colon targeting.
AAPS PharmSciTech 2007;8:E87-93
60. Rahman Z, Kohli K, Khar RK, et al.
Characterization of 5-fluorouracil
microspheres for colonic delivery.
AAPS PharmSciTech 2006;7:E1-9
61. Umadevi SK, Thiruganesh R, Suresh S,
Reddy KB. Formulation and evaluation
of chitosan microspheres of aceclofenac
for colon-targeted drug delivery.
Biopharm Drug Dispos 2010;31:407-27
62. Zhang L, Cao F, Ding B, et al. Eudragit
S 100 coated calcium pectinate
microspheres of curcumin for colon
targeting. J Microencapsul
2011;28:659-67
63. Thakral NK, Ray AR, Majumdar DK.
Eudragit S-100 Entrapped chitosan
microspheres of valdecoxib for colon
cancer. J Mater Sci Mater Med
2010;21:2691-9
64. Zimova L, Vetchy D, Muselik J,
Stembirek J. The development and
in vivo evaluation of a colon drug
delivery system using human volunteers.
Drug Deliv 2012;19:81-9
65. Asghar LF, Chandran S. Design and
evaluation of matrices of Eudragit with
polycarbophil and carbopol for
colon-specific delivery. J Drug Target
2008;16:741-57
148
66. Kshirsagar SJ, Bhalekar MR, Patel JN,
et al. Preparation and characterisation of
nanocapsules for colon-targeted drug
delivery system. Pharm Dev Technol
2012;17(5):607-13
67. El-Bary AA, Aboelwafa AA,
Al Sharabi IM. Influence of some
formulation variables on the optimization
of pH-dependent, colon-targeted,
sustained-release mesalamine
microspheres. AAPS PharmSciTech
2012;13:75-84
68. Amrutkar JR, Gattani SG. A novel
hydrogel plug of Sterculia urens for
pulsatile delivery: in vitro and in vivo
evaluation. J Microencapsul
2012;29:72-82
69. Obeidat WM, Price JC. Preparation and
evaluation of Eudragit S
100 microspheres as pH sensitive release
preparations for piroxicam and
theophylline using emulsion solvent
evaporation method. J Micoencapsul
2006;23:195-202
70. Bruce LD, Shah NH, Malick AW, et al.
Properties of hot melt extruded tablet
formulations for the colonic delivery of
5-amino salicylic acid. Eur J Biopharm
2005;59:85-97
71. Liu F, Lizio R, Meier C, et al. A novel
concept in enterc coating:
a double-coating system providing rapid
release in the proximal small intestine.
J Control Release 2009;133:119-24
72. Lui F, Basit AW. A paradigm shift in
enteric coating: achieving rapid release in
the proximal small intestine of man.
J Control Release 2010;147:242-5
73. McGinity JW, Felton LA. Aqueous
polymeric coatings for pharmaceutical
dosage forms. 3rd edition. Informa
Healthcare; New York: 2008
74. Miller DA, McGinity JW. Aqueous
polymeric film coating. In:
Augsburger LL, Hoag SW, editors.
Pharmaceutical dosage forms: tablets.
Volume 1 3rd edition. Unit operations
and mechanical properties. Informa
Healthcare; New York: 2008
75. Fan TY, Wei SL, Yan WW, et al. An
investigation of pulsatile release tablets
with ethyl cellulose and Eudragit L as
film coating materials and cross-linked
polyvinylpyrrolidone in the core tablets.
J Control Release 2001;77:245-51
76. Steward PA, Hearn J, Wilkinson MC.
Studies on permeation through polymer
Expert Opin. Drug Deliv. (2013) 10(1)
latex films. I Film coating containing no
or low levels of additives. Polym Int
1995;38:1-12
77. Lehmann K. Chemistry and application
properties of polymethacrylate coating
system. In: McGinity JW, editor.
Aqueous polymeric coating for
pharmaceutical dosage forms. Marcel
Dekker Inc; New York: 1997
78. Bodmeier R, Guo X, Sarabia RE,
Skultety PF. The influence of buffer
species and strength on diltiazam HCl
released from beads coated with aqueous
cationic polymer dispersion Eudragit RS
30 D. Pharm Res 1996;13:52-6
79. Wagner KG, McGinity JW. Influence of
chloride in exchange on permeability and
drug release from Eudragit RS 30D
films. J Control Release 2002;82:385-97
80. Maejima T, McGinity JW. Influence of
film additives on stabilizing drug release
rates from pellets coated with acrylic
polymers. Pharm Dev Technol
2001;6:211-21
. Studied effect of addition of talc to
Eudragit RS/RL 30D 95:5 plasticised
with triethyl citrate and showed no
significant change in drug release after
storage for a period of 3 months
81. El-Malah Y, Nazzal S. Novel use of
Eudragit NE 30. D/Eudragit
L
30D-55 blends as functional coating
materials in time-delayed drug release
applications. Int J Pharm
2008;357:219-27
82. Li G, Han D, Guan T, et al. Isosorbide-
5- mononitrate (5-ISMN) sustained
release pellets prepared by double layer
coating for reducing 5-ISMN migration
and sublimation. Int J Pharm
2010;400:134-44
83. Lin AY, Muhammad NA, Pope D,
Augsburger LL. Study of crystallization
of endogenous surfactant in Eudragit
NE30D-free films and its influence on
drug release properties of
controlled-release diphenhydramine HCl
pellets coated with Eudragit NE30D.
AAPS PharmSci 2001;3:E14
84. Agabeyoglu I. Studies on sustained
release I, the biopharmaceutical design
and preparation of an inert matrix type
sulfamethazole tablet employing
polymethacrylate. Drug Dev Ind Pharm
1985;11:2021-41
85. Oth MP, Moes AJ. Sustained release
solid dispersion of indomethacin with

eudragit RS and RL. Int J Pharm
1989;55:155-64
86. Abhaspour MR, Sadeghi F, Garekaw A.
Preparation and characterization of
ibuprofen pellets based on Eudragit RS
PO and RL PO or their combination.
Int J Pharm 2005;303:88-94
87. Ceballos A, Cirri M, Maestrelli F, et al.
Influence of formulation and process
variables on in vitro release of
theophylline from directly-compressed
Eudragit matrix tablets. Il Farmaco
2005;60:913-18
88. Colo DG, Falchi S, Zambito Z. In vitro
Expert Opin. Drug Deliv. Downloaded from informahealthcare.com by McGill University on 12/20/12
evaluation of a system for pH-controlled
peroral delivery of metformin.
J Control Release 2002;80:119-28
89. Arevalo MF, Villafuerte MAH,
Dorado JMG, Alvarez AMR. Effects of
different fillers and wetting liquids on
the dissolution of carteolol hydrochloride
controlled release inert matrix tablets.
Int J Pharm 1993;95:117-25
90. Aitken-Nichol C, Zhang F,
McGinity JW. Hot melt extrusion of
For personal use only.
acrylic films. Pharm Res 1996;13:804-8
91. Follonier N, Doelker E, Cole ET.
Evaluation of hot-melt extrusion as a
new technique for the production of
polymer-based pellets for sustained
release capsules containing high loading
of freely soluble drugs. Drug Dev
Ind Pharm 1994;20:1323-39
92. Zhu Y, Shah NH, Malick AW, et al.
Solid state plasticization of an arylic
polymer with chlorpheniramine maleate
and triethyl citrate. Int J Pharm
2002;241:301-10
93. Crowley MM, Zhang F, Repka MA,
et al. Pharmaceutical applications of hot
melt extrusion. Part I. Drug Dev
Ind Pharm 2007;33:909-26
94. Douroumis D. Hot melt extrusion:
pharmaceutical applications. John Wiley
and Sons; Chichester, UK 2012
95. Zhu Y, Mehta KA, McGinity JW.
Influence of plasticizer level in the drug
release from sustained release film coated
and hot melt extruded dosage forms.
Pharm Dev Technol 2006;11:285-94
96. Ishikawa T, Watanabe Y, Utoguchi N,
Matsumoto M. Preparation and
evaluation of tablets rapidly
disintegrating in saliva containing
bitter-taste-masked granules by the
compression method. Chem Pharm Bull
1999;47(10):1451-4
97. Lehmann K, Petereit H-U, Dreher D.
Fast disintegrating controlled release
tablets from coated particles.
Drug Made Germany 1994;37(2):53-60
98. Cumming KI, Harris E. Taste-masked
formulations. US6153220; 2000
99. Percel PJ, Venkatesh GM,
Vishnupad KS. Functional coating of
linezolid microcapsules for taste-masking
and associated formulation for oral
administration. WO0152848; 2001
100. Chiappetta DA, Carcaboso AM,
Bregni C, et al. Indinavir-loaded
pH-sensitive microparticles for taste
masking: toward extemporaneous
paediatric anti-HIV/AIDS liquid
formulations with improved patient
compliance. AAPS PharmSciTech
2009;10:1-6
101. Thoennes CJ, McCurdy VE. Evaluation
of a rapidly disintegrating, moisture
resistant lacquer film coating. Drug Dev
Ind Pharm 1989;15:165-85
102. Bley O, Siepmann J, Bodomeier R.
Characterization of moisture-protective
polymer coatings using differential
scanning calorimetry and dynamic vapor
sorption. J Pharm Sci 2009;98:651-64
103. Cao X, Gao Q, Gao P, et al. Preparation
and characterization of novel aqueous
dispersion of Eudragit E for coating.
Asian J Pharm Sci 2007;2:29-37
104. Mwesigwa E, Basit AW, Buckton G.
Moisture sorption and permeability
characteristics of polymer films:
implications for their use as barrier
coatings for solid dosage forms
containing hydrolysable drug substances.
J Pharm Sci 2008;97:4433-45
Expert Opin. Drug Deliv. (2013) 10(1)
Eudragit
: a technology evaluation
105. Pignatello R, Ferro M, Guidi GD, et al.
Preparation, characterisation and
photosensitivity studies of solid
dispersions of diflunisal and Eudragit
RS100 and RL100. Int J Pharm
2001;218:27-42
106. Pignatello R, Ferro M, Puglisi G.
Preparation of solid dispersions of
nonsteroidal anti-inflammatory drugs
with acrylic polymers and studies on
mechanisms of drug-polymer
interactions. AAPS PharmSciTech
2002;3:1-11
107. Pignatello R, Spadaro D, Vandelli MA,
et al. Characterization of the mechanism
of interaction in Ibuprofen - Eudragit
RL100 coevaporates. Drug Dev
Ind Pharm 2004;30:277-88
108. Sarisuta N, Lawanprasert P,
Puttipipatkhachorn S, Srikummoon K.
The influence of drug-excipient and
drug-polymer interactions on adhesive
strength of Ranitidine Hydrochloride
film-coated tablets. Drug Dev Ind Pharm
2006;32:463-71
109. Yuksel N, Baykara T. Preparation of
polymeric microspheres by the solvent
evaporation method using sucrose
stearate as a droplet stabilizer.
J Microencapsul 1997;14:725-33
Affiliation
Seema Thakral1, Naveen K Thakral2 &
Dipak K Majumdar†3
†
Author for correspondence
1
GVM College of Pharmacy,
Sonipat, India
2
University of Minnesota,
Department of Pharmaceutics,
Minneapolis, MN 55455, USA
3
University of Delhi,
Delhi Institute of Pharmaceutical Sciences and
Research (Formerly College of Pharmacy),
Department of Pharmaceutics,
Pushp Vihar, Sector III,
New Delhi 110017, India
Tel: +91 9871343968;
E-mail: dkmajumdaar@yahoo.com;
dkmajumdar@gmail.com
149