Introduction

• Polymer
Large molecules composed of a number of sub-units

• How can they help in DDS?

 Protection of therapeutic compound during through body as
encapsulant or carrier.
 Mediator or activator of controlled release
Characteristics of ideal polymer
 Should be inert and compatible with environment.
 Non toxic and easily administered
 Easy and inexpensive to fabricate
 Should have good mechanicals strength

Criteria in Polymer selection :

 Soluble and easy to synthesize
 Provide drug attachment and release site for drug polymer
linkage
 Should be biodegradable or be eliminated after its function is
over
General mechanism of drug release from polymer

Three primary mechanism:

1. Diffusion
2. Water penetration (swelling)
3. Degradation
Any of these mechanism can occur in a given release system
 Drug release from polymer by diffusion
• Rate limiting steps is
diffusion of drug through
inert water insoluble
membrane barrier

• There are two types;

A. Matrix
B. Reservoir
Reservoir diffusion system
• In membrane controlled reservoir device ,the drug contained
in a core ,which is surrounded be a polymer membrane and it
is released by diffusion this rate controlling membrane
E.g poly (ethylene –co-vinyl acetate )
 Matrix diffusion system
In these devices ,the drug is released either by passing through
the pores or between polymer chains,and these are the processes
that control the release rate as polyethylene and polyvinylacetate
Water penetration (swelling)
This type of systems are initially dry when placed in the body
absorb water or other fluid it swells .
Swelling increase aq solvent within the formulation as well as the
polymer mesh size enabling the drug to diffuse through the
swollen network into external environment
 Biodegradable polymers
It defined as polymers that are degradable in vivo,either
enzymatically or nonenzymatically ,to produce biocombatable or
nontoxic by-product .these polymer can be metabolized and
excreted through physiological pathway .
Specific physical properties that contribute to the rate of
:polymer degradation are as follows

 Water permeability and water solubility

 Crystallinity of the polymer; only the amorphous phase of the
polymers accessible to permeants (i.e., water, drug) and to
enzymatic attack
 Glass-transition temperature
 Physical dimensions (e.g., size and surface-to-volume ratio
:Advantage of biodegradable polymers
1. It provides a drug at a constant controlled rate owes a prescribed period of
time.
2. The polymer carrier would degrade into nontoxic, absorbable subunits
which would be subsequently metabolized.
3. The system would be biocompatible would not exhibit dose dumping at any
time and polymer would retain its characteristics untill after depletion of the
drug.
4. Degradable system eliminates the necessity for surgical removal of
implanted device following depletion of a drug.
5. They are broken down into biologically acceptable molecules that are
metabolized and removed from the body via normal metabolic pathways.
Disadvantage:
 Sometimes the degradable polymers exhibit substantial dose
dumping at some point following implantations.
 A “burst effect” or high initial drug release soon after
administration is typical of most system.
 Degradable systems which are administered by injection of
aparticulate form are non-retrievable.
 Classification of biodegradable polymer

Biodegradable
polymer

Natural Synthetic

Extracted directly
:from biomass Produced directly Aliphatic polyester
Polyvinyl alcohol and
from natural organism e.g PLA,PGA,PHA
Polysaccharide,protei polyvinyl acetate
e.g PLA,PGA,PHA and their copolymer
n lipid
List of biodegradable polymer used in drug delivery
Natural polymer
 Protein- based polymer
 Polysaccharides
Synthetic polymer
 Polyester
 Polyanhydrides
 Polyamides
 Phosphorous based polymers
Collagen ,albumin,gelatin
Agarose,alginate,carrageenan,hyaluronic
acid,dextran,chitotsan,cyclodextrins
Polylactic acid,polyglycolic acid
Polysebacic acid ,polyadibic acid
Polyiminocarbonate
Polyphosphates,polyphosphonate
Natural biodegradable polymers
Application Polymer
Used in bioprosthetic implants and tissue Collagen
engineering of multiple organ but majorly
used in ocular drug delivery system
Used to deliver drug like insulin Albumin
,prenisolone as albumin micro-spheres
Used for colonic delivery of drug In the Dextran
form of gels.
Employed as coating material Gelatin
Gelatin micropellets are used for oral
controlled DDS
 Synthetic biodegradable polymer
Application Polymer
Used to deliver drugs in the form of Poly glycolic acid
microspheres,implants etc.
Examples of drugs delivered include
steroid hormone,antibiotic,anticancer
agent.
It is used in the preparation of sutures or Poly lactic acid
orthopaedic devices .
Includig ; Polycaprolactone
-cyclosporin in the form of nanoparticles
-ciprofloxacin in the form of dental
implants.
-Sitable for short term drug delivery Poly anhydrides (drug prepared by
-Used for vaccination and localized tumor compression molding or
therapy. microencapsulation
-Used in the construction of soft tissue Polyphoshazenes
prosthesis, tissue like coatings, as material
for BV prosthesis.
-Used for immobilization of antigen or
enzyme
 Mechanism of drug release from
biodegradable polymer

Biodegradation

Enzymatic Hydrolysis Combination

Bulk erosion Surface erosion

Hydrolytic degardation

Break down of polymer by water by cleaving long chain into

monomeric acid this done by two ways:
 Eroding polymers:
e.g polylactic acid , polyglycolic acid

 Surface eroding polymers:

e.g polyanhydrides
Types of bioerosion

1. Bulk erosion
• Degradation of sample take place
through the whole of sample
• Ingress of water is faster than the
rate of degradation
E.g: polylactic acid (PLA)
polyglycolic acid(PGA)

2.Surface eroding polymers

• Sample is erodided from the
surface
• Mass loss is faster than the
ingress into the bul E.g :
polyanhydrides,
polyorthoester
Need of biodegradable polymer

1) Achieving controlled drug delivery

2) No need for a second surgery for removal of polymer

what are biopolymer?

Any
Biodegradable •
bio related Biomaterial •
polymeric Bio renewable •
material
Enzymatic or chemical
degradation
• Mechanism I
Cleavage of crosslinks

• Mechanism II
transformation of site

• Mechanism III
Cleavage of backbone
Factor effecting biodegradation of polymer
 Morphological factor
• Size & shape
• Variation of diffusion coefficient and mechanical stress
 Chemical factors
• Chemical structure & composition
• Presence of ionic group of and configuration structure
• Molecular weight and presence of low molecular weight compound
 Physical factors
• Processing condition
• Sterilization process
 Advantage of biodegradable polymer

• Localized delivery of drug

• Sustained delivery of drug
• Stabilization of drug
• Decrease in dosing frequency
• Reduce side effects
• Improved patient compliance
• Controllable degradation rate
Application of polymer in formulation of controlled DDS

Oral DDS

Osmotic pressure Gel diffusion Muco-adhesive GI

controlled GI DS controlled DS delivery system
Osmotic pressure controlled GI delivery system
It controlled release oral drug delivery system as tablet .the tablet
has rigid water permeable jacket. As the tablet posses through the
body, the osmotic pressure of water entering the tablet pushes the
active drug through semi-permeable membrane.in this system
semi-permeable membrane is made from biocompatible polymer
e.g cellulose acetate
 Muco-adhesive GI delivery system
It interact with the mucus layer covering the mucosal epithelial
surface ,mucin molecules & increase the residence time of the
dosage from the dosage format the site of absorption.in this,a
polymer is required to produce adhesion interaction with a
biological membrane e.g carbopol
 Gel diffusion controlled delivery system
The main feature of this system is that the drug core is enclosed
with a partially soluble membrane
e.g Carboxy methyl cellullose
Transdermal drug delivery system

TDDS is defined as self contained ,self discrete dosage forms,

which when applied to the intact skin delivers the drug at a
controlled rate to the systemic circulation .in this polymer matrix
plays a major role , it release the drug from the device to the skin
Ocular drug delivery system

• It allow prolonged contact of drug with corneal surface of eye.

The example is pilocarpine in the treatment of glaucoma. In
this muco-adhesive polymers are used as barriers to control
the drug release.
e.g polyacrylic acid ,copolymers of acetate vinyl & ethyl
 Applications of polymers in solid dosage form

• In tablet
Polymer like methyl cellulose, hydroxy methyl cellulose are used as binder
Carboxy methyl cellulose sodium is used as disintegration
Polymer like cellulose acetate phthalate used as enteric coating material
• In capsules
Gelatin a natural polymer which is the major ingredient in the manufacturing
of capsules
In liquid dosage form
• In Suspension
Polymer like Acacia ,Tragacanth are used as suspending
agent.They should be selected based on their characters like PH,
Solubility & concentration .They enhance the dispersion of solids
in liquids.
• In Emulsions
Polymer like Tragacanth ,Spans,Tween are used as emulsifying
agents
 Conclusion
Polymer‐based pharmaceuticals are starting to be seen as key elements to treat
many lethal diseases that affect a great number of individuals such as cancer
or hepatitis .Although excipients have traditionally been included in
formulations as inert substances to mainly make up volume and assist in the
manufacturing process, they are increasingly included in dosage forms to
fulfill specialized functions for improved drug delivery because many new
drugs have unfavorable physicochemical and pharmacokinetic properties. The
synthetic polymers can be designed or modified as per requirement of the
formulation by altering polymer characteristics and on the other hand natural
pharmaceutical excipients are biocompatible, non toxic, environment friendly
and economical. Several polymers have been successfully used and others are
being investigated as excipients in the design of dosage forms for effective
drug delivery.
References
 Drug delivery system book
 Researchgate site
 Slideshare site
 polymer in pharmaceutical drug delivery
system : kjg16@rediffmail.com