Role of polymers in *

drug delivery

PREPARED BY :1.MOATH ALSARARI

MOATH AL-AGHBARI.2
MOATH RAJEH.3
MOFID AL-AMARI.4
SUPERVISED BY :DR. ABDULWALI ALSHARGABI
 Contents *
.Introduction of polymers-
.Biodegradable polymers-
.classification of biodegradable polymers-
.Polymer degradation mechanism-
.a)Bioerosion mechanism
.b)Enzymatic or chemical degradation
.Synthetic biodegradable-
.Natural biodegradable polymers-
Factors affecting biodegradation of-
.polymers
.Applications of biodegradable polymers-
.Conclusion-
.References-
 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
Biodegradable
polymer
polymer

Natural
Natural ’‘
’‘ Synthetic
Synthetic

Extracted
Extracted Produced
Produced Aliphatic
Aliphatic
directly
directly from
from directly
directly from
from polyester
polyester e.g
e.g Polyvinyl
Polyvinyl
::biomass
biomass natural
natural organism
organism PLA,PGA,PHA
PLA,PGA,PHA alcohol
alcohol and
and
Polysaccharide,p
Polysaccharide,p e.g
e.g and
and their
their polyvinyl
polyvinyl acetate
acetate
rotein
rotein lipid
lipid PLA,PGA,PHA
PLA,PGA,PHA copolymer
copolymer
 List of biodegradable polymer used in *
drug delivery
Natural polymer

Protein- based polymer

Polysaccharides

Synthetic polymer Collagen ,albumin,gelatin

Polyester Agarose,alginate,carrageenan,hyaluronic
Polyanhydrides acid,dextran,chitotsan,cyclodextrins
Polyamides
Phosphorous based polymers
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
 Polymeric DDS devices*
Particulate system -
Nanoparticles -
Nanocapsules -
Nanospheres -
Microparticles -
Microshperes -
Microcapsules -
 Polymer
)Natural\Synthetic(
Drug

Preparation of polymeric
nanoparticles by various methods

Nanocapsule Nanosphere
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