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Micro-Encapsulation: by Sandeep Mollidain Roll No:04 M.Pharmacy (Pharmaceutical Technology) Shift-Ii
Micro-Encapsulation: by Sandeep Mollidain Roll No:04 M.Pharmacy (Pharmaceutical Technology) Shift-Ii
By
SANDEEP MOLLIDAIN
Roll no:04
M.Pharmacy (pharmaceutical technology)
SHIFT- II
1
CONTENTS:
INTRODUCTION
FUNDAMENTAL CONSIDERATIONS
CORE MATERIAL
COATING MATERIAL
RELEASE MECHANISMS
METHODS OF PREPARATION
APPLICATIONS OF MICROENCAPSULATION
PHYSICOCHEMICAL EVALUATION
ADVANTAGES
CONCLUSION 2
INTRODUCTION
Definition :
substances.
3
4
A well designed controlled drug delivery system
5
To obtain maximum therapeutic efficacy, drug is to be
delivered :
6
One such approach is using microspheres as carriers for drugs.
biodegradable in nature
7
Microspheres:
8
Formulated Microsphere
9
Red one’s are R.B.C
Purple one’s are microspheres
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REASONS FOR MICROENCAPSULATION
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isolating a reactive core from chemical attack.
12
FUNDAMENTAL CONSIDERATIONS
13
CORE MATERIAL
coated.
material.
. 14
The solid core can be single solid substance or mixture of
15
COATING MATERIAL
The selection of coating material decides the physical and
- stabilization
- reduced volatility
- release characteristics
SYNTHETIC
NATURAL
Classification of polymers
17
The polymer should be capable of forming a film that is
core material.
- strength
-flexibility,
-impermeability,
examples :
-Gelatin
- polyvinyl alcohol
- ethyl cellulose
on:
clusters of particles.
20
After isolation from the liquid manufacturing vehicle
-compressed tablets
21
Morphology of Microcapsules
The morphology of microcapsules depends mainly on the core
material and the deposition process of the shell.
1- Mononuclear (core-shell) microcapsules contain the shell around
the core.
2- Polynuclear capsules have many cores enclosed within the shell.
3- Matrix encapsulation in which the core material is distributed
homogeneously into the shell material.
- In addition to these three basic morphologies, microcapsules can
also be mononuclear with multiple shells, or they may form clusters
of
microcapsules.
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23
RELEASE MECHANISMS
the isolation of the core from its surrounding, the wall must
microcapsules :
24
by pressure or shear stress.
25
by solvent action
26
METHODS OF PREPARATION
Preparation of microspheres should satisfy certain
criteria:
The ability to incorporate reasonably high concentrations of
the drug.
27
Controlled particle size and dispersability in aqueous
time scale.
28
MICROENCAPSULATION METHODS
Air suspension
Multiorifice-centrifugal process
Pan coating
29
Solvent evaporation techniques
Electrostatic deposition
Vaccum deposition
Polymerization
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AIR SUSPENSION:
air stream.
particles.
34
The design of the chamber and its operating parameters
During each pass through the coating zone, the core material
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The cyclic process is repeated, perhaps several hundred times
The supporting air stream also serves to dry the product while it
is being encapsulated.
38
Schematics of a fluid-bed coater.
(a) Top spray;
(b) bottom spray;
(c) tangential spray
39
Drying rates are directly related to the volume temperature of
40
COACERVATION PHASE SEPARATION
41
The term originated from the Latin ›acervus‹ , meaning
“heap”.
42
The mechanism of microcapsule formation for both
43
The process consists of three steps:
solvent.
material.
polymer.
state is formed by
vitamin encapsulation ,
45
(iii) addition of nonsolvent, e.g. addition of isopropyl ether to
core material.
connected molecules.
47
The vulcanization of rubber using elemental sulfur is an
48
Schematic representation of the coacervation process.
(a) Core material dispersion in solution of shell polymer;
(b) separation of coacervate from solution;
(c) coating of core material by microdroplets of coacervate;
(d) coalescence of coacervate to form continuous shell around core particles.
49
50
Polymer Encapsulation by Rapid Expansion of Supercritical Fluids
51
Supercritical CO2 is widely used because of following
advantages:
-nontoxic,
-readily available,
-highly pure
-cost-effective.
52
The most widely used methods are as follows:
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Rapid expansion of supercritical solution
Supercritical fluid containing the active ingredient and the
54
The disadvantage of this process is that both the active
supercritical fluids.
55
The solubility of polymers can be enhanced by using
co-solvents.
In some cases nonsolvents are used; this increases the solubility
atmospheric pressure.
56
Microencapsulation by rapid expansion of supercritical solutions
(RESS).
57
Gas anti-solvent (GAS) process
The solute must be soluble in the liquid solvent, but should not
59
Upon releasing the pressure, the shell material is allowed to
In this process, the core and shell materials may not be soluble in
60
The liquid solvent must be miscible with the supercritical
fluid.
supercritical fluids.
this method.
61
MULTIORIFICE-CENTRIFUGAL PROCESS
method.
62
Processing variables include:
material.
63
The multiorifice-centrifugal process is capable for
- dry powder.
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PAN COATING
release beads.
65
Medicaments are usually coated onto various spherical
66
Usually, to remove the coating solvent, warm air is passed
drying oven.
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68
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CO EXTRUSION
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Schematic presentation of the Co-
extrusion process
71
Co-extrusion Process
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SPRAY DRYING AND SPRAY CONGEALING
material.
dissolved.
accomplished by
evaporation techniques.
75
Microencapsulation by spray-drying is a low-cost commercial
process.
a hot chamber.
The shell material solidifies onto the core particles as the solvent
or matrix type.
76
Chitosan microspheres cross-linked with three different cross-
-tripolyphosphate (TPP),
-formaldehyde (FA)
technique.
77
The particle size and encapsulation efficiencies of thus
78
Spray dried chitosan microspheres cross-linked with TPP exhibited
from 1 to 2%w/w.
79
Release rate of the drug from spray dried chitosan
80
Release of the drug from chitosan-TPP, chitosan-FA and
81
Spray congealing can be done by spray drying equipment where
coating solution.
82
Waxes, fatty acids, and alcohols, polymers which are solids at
83
Schematic illustrating the process of micro-encapsulation by spray-drying.
84
85
Spinning Disk
Suspensions of core particles in liquid shell material are
poured into a rotating disc.
Due to the spinning action of the disc, the core particles
become coated with the shell material.
The coated particles are then cast from the edge of the disc
by centrifugal force.
After that the shell material is solidified by external means
(usually cooling).
This technology is rapid, cost-effective, relatively simple and
has high production efficiencies.
86
Microencapsulation by spinning disc
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SOLVENT EVAPORATION
size microcapsules.
89
Several methods can be used to achieve dispersion
90
Important factors that must be considered in solvent
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The core materials may be either water soluble or water
insoluble materials.
92
ELECTROSTATIC DEPOSITION
high voltage.
93
Coating material is charged in solution when it leaves the
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VACCUM DEPOSITION
is present.
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POLYMERIZATION
A relatively new microencapsulation method utilizes
is dispersed.
96
Interfacial polymerization ( IFP)
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The multifunctional monomer dissolved in liquid core
material
agent.
mixture.
with amine,
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In situ polymerization
polymerization of monomers.
In this process no reactive agents are added to the core material.
100
Initially a low molecular weight prepolymer will be formed,
101
APPLICATIONS OF MICROENCAPSULATION
Nitrofurantoin etc.
102
Sustained release Aspirin preparations have been reported to
preparations.
103
Hygroscopic properties of core materials may be reduced by
104
Separation of incompatible substance has been achieved by
encapsulation.
105
PHYSICOCHEMICAL EVALUATION
CHARACTERIZATION:
the carrier.
106
SIEVE ANALYSIS
A series of five standard stainless steel sieves (20, 30, 45, 60 and
most sieve.
The sieves are shaken for a period of about 10 min, and then the
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ATOMIC FORCE MICROSCOPY
(AFM)
the microspheres.
110
Atomic Force Microscope
111
PARTICLE SIZE
Particle size determination:
ultrasound.
at 60 ml/ s.
115
VISCOSITY OF THE POLYMER SOLUTIONS
116
viscometer
117
DENSITY DETERMINATION
The density of the microspheres can be measured by using
118
Two consecutive readings of reduction in pressure at different
119
multi volume pychnometer.
120
BULK DENSITY
The microspheres fabricated are weighed and transferred to a
stabilised.
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122
CAPTURE EFFICIENCY
lyse.
hydrophilicity or hydrophobicity.
124
The angle of contact is measured at the solid/air/water
interface.
inverted microscope.
125
IN VITRO METHODS
membrane to be determined.
127
BEAKER METHOD
129
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ADVANTAGES
specificity.
131
Microspheres received much attention for targeting of
particles in vivo.
residing intracellularly.
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CONCLUSION
opportunities such as
Protection.
Masking.
facilitation of handling.
or tissue.
6.P.Venkatesan, C.Muralidharan,
R.Manavalan and K.Valliappan. Selection
of better method for the preparation of
microspheres by applying Analytic
Hierarchy Process. J. Pharm. Sci. & Res.
Vol.1(3), 2009, 64-78.
138
Thank you
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