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BIODEGRADABLE POLYMERS
Department of pharmaceutics
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CONTENTS
Definition
Ideal characteristics
Advantages and Disadvantages
Polymers erosion mechanism
Polymers drug release mechanism
Classification of polymers along with their
application
Product based on biodegradable polymers
References
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BIODEGRADABLE
POLYMERS
DEFINITION:
The natural ability of chemical
substance to be broken down into
less complex compounds having
fewer carbon atoms by body fluids
or enzymes or microorganism.
OR
It is defined as the breakdown
of polymer into its components
monomers or oligomers upon
IDEAL CHARACTERISTICS
OF BIODEGRADABLE
POLYMERS
Minimal side effects after
introduction into body.
In vivo degradation at well defined
rate.
Degradation products should be
nontoxic and easily excreted.
Free from any toxic endogenous
impurities or residual chemical.
Should be inert in nature.
Should have relative stability.
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ADVANTAGES OF
BIODEGRADABLE
POLYMERS
Useful for delivery of synthetic drugs as
well as proteins and biotechnological
products .
No need subsequent retrival of the
delivery.
Better drug utilization and improved
patients compliance.
Targeted specific part of body hence
reduce side effect.
Provide controlled rate of drug release.
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DISADVANTEGES OF
BIODEGRADABLE
POLYMERS
Difficult to formulate a biodegradable
system
Carrier must be human friendly.
Some polymers do not have detail
information about its
biodegradability, kinetic, stability
profile.
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POLYMERS EROSION
MECHANISM
Bioerosion : physical process that
result in weight loss of polymer
devices.
Two types of erosion
1.chemical erosion
2.physical erosion
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Chemical erosion
Mechanism 1
Type 1A] Degradation in these
system can occur either at cross links
to form soluble backbone polymeric
chains provide high molecular weight,
Type 2B] At the main chain to form
water soluble fragments. Provide low
molecular weight fragments.
Mechanism 2
water insoluble macromolecule with
side groups converted in water soluble
polymer by ionization, protonation or
hydrolysis of groups.
Mechanism 3
Degradation of insoluble polymers
with labile bonds .hydrolysis of labile
bond causes scisson of polymer
backbone.
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Polymers & their
chemical mechanism of
erosion
Gelatin Type 1
Collagen Type 1 & Type 2
Polyanhydrides Type 3
Polycaprolactone &
it’s copolymer
Poly (ortho esters) Type 3
Poly (lactic acids) Type 3
Poly (glycolic acid) Type 3
Poly (vinyl alcohol)
Type 3
Type 1
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Physical erosion
Heterogeneous erosion
called surface erosion,
polymer erode only at
surface and maintain it’s
physical integrity.
Homogenous erosion
called bulk erosion
hydrolysis occur at even
rate throughout the
polymer matrix.
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DRUG RELEASE MECHANISMS OF
BIODEGRADABLE POLYMERS
In mechanism 1 the drug is
attached to polymer
backbone by labile bond,
shows higher reactivity to
breakdown.
Mechanism 2 drug release
is controlled by
biodegradable membrane
surrounded by core
containing drug .
Mechanism 3
homogeneously dispersed
drug in biodegradable
polymers released by
erosion diffusion or
combination of both.
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CLASSIFICATION OF
BIODEGRADABLE
POLYMERS.
Synthetic Natural
Polyanhydride Gelatin.
Poly-E-Caprolactone. Albumin.
Polyphosphazenes. Starch
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SYNTHETIC BIODEGRADABLE
POLYMERS ALONG WITH THEIR
COPOLYMERS
1)Lactide & glycolides Poly [lactic acid] (PLA)
Poly [glycolic acid] (PGA)
Poly [ lactide-co-glycolic] (PLGA)
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POLYMERS AND THEIR
APPLICATION
Lactide & glycolides
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Local anesthetics [lidocaine,xylocaine]
are formulated with homo and co-
polymers of lactide and glycolides.
In formulation of veterinary products
[melatonin loaded system for sheep for
production of fur.
Bioactive agents like polypeptides
[LHRH,calcitonin] and vaccine [antigen,
antibody] can given with this.
co-polymers used formulate
biotechnology products.
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POLYANHYDRIDE
Better biocompatibility with body tissue
Polycondensation,dehydrochlorination and
dehydrative coupling synthesize this
polymers.
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APPLICATION
CPP-SA used to formulate anticancer agents
[carmustine] –used in treatment of glioblastoma
multiforme,which is a type brain cancer.
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POLYPHOSPHAZENES
Long chain backbone of alternative
nitrogen and phosphorus atom with two
groups attached to each other.
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APPLICATION
Drug containing COOH groups (salicylic acid) could
be linked to this polymer by amide linkage to
prepare controlled release prodrug.
Used as hydrogel:
Intraocular lenses.
Soft tissue prosthesis (artificial replacement
for a missing tissue).
Substrate for enzyme and antigen.
Polymer bound platinum antitumor agent are
available having better therapeutic effect & good
pharmacokinetics properties.
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POLY-E-CAPROLACTONE
Shows heterogeneous degradation by
micro-organism in the environment.
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APPLICATION
Drug like tetracycline, 5-fluoro
Uracil, chlorpromazine, naloxanes
are given with this polymers.
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APPLICATION
Polymer used for antigen delivery
that is for effective vaccination.
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NATURAL POLYMERS
ADVANTAGES
readily available natural
polymers.
relatively inexpensive.
chemical modification is possible
easily.
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COLLAGEN
Unique structural properties therefore it
can fabricated into variety of forms
including films, inserts.
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ALBUMIN
Major plasma constituent in body and
features like reported biodegradation,
lack of toxicity, non- antigenicity and
readily available.
APPLICATION
1. Drugs like doxorubicin,mitomycine,5-
fluorouracil are given because tumor cells
ability to take up albumin.
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STARCH
Most abundant biodegradable polymers
which belong to class of polysaccharide.
It consist of glycopyranose units which
under hydrolysis yields D-glucose.
APPLICATION
starch microspheres used for intranasal
administration of insulin.
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GELATIN
It is protinaceous biodegradable polymers
obtained from partial hydrolysis of collagen
derived from skin, connective tissue and
bones of animal.
Two types
a] Type A : acid treated .
b] Type B : alkali treated.
mostly fabricated into microspheres.
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APPLICATION
Good carrier systems for number of
anticancer agents that is tumors which do
not take albumin redially take up gelatin.
Used as an immunoadjuvant because
gelatin is susceptible to macrophage
recognition. The gelatin containing the
antigen can carry it directly to the
macrophages and antigen is released as
gelatin degrades which leads to enhance
production of antigen specific antibodies.
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Dextran
It is a carbohydrate used to
prepare hydrogel, which is
biodegradable and
biocompatible. Usually available
as microspheres
Application
Acts as a good carrier for a
variety of drugs, proteins.
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OTHER NATURALLY OCCURING
POLYMERS
Hyaluronic acid
Fibrinogen
Deacetylated Chitin: aid weight loss
and cholesterol lowering agents.
Carragenan
Alginate
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SOME PRODUCT BASED ON
BIODEGRADABLE POLYMERS
1. Zoladex (Astra zeneca) :
Is supplied as sterile biodegradable product containing
goserlin acetate equivalent to 3.6 mg of goserlin given as
sub cutaneous injection with continuous release over 28
days. It dispersed in matrix of DL lactic & glycolic acid.
2. Lupron depot :
FDA cleared PLGA product
microsphere formulation based on degradable polymers
of polylactic acid & poly (lactic/glycolic acid).
3 Gliadel wafer.
contain cancer chemotherapeutic drug carmustine
fabricated from poly (caboxyphenoxy propane: sebacic
acid)
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REFERENCES
Biodegradable polymers as Drug delivery
systems Mark chasin, Robert Langer,volume 45.
Indian Journal of pharmaceutical sciences sep-oct 2007.69(5):609-
734. V. B. Kotwal, Maria Saiffee, Nazma
Inamdar and Kiran Bhise, Allana College of
Pharmacy, K. B. Hidayatullah Road, Azam
Campus, Pune - 411 001, India.
Encyclopedia of pharmaceutical Technology
volume 2 : James swarbrick, James.c.Boylan,P-
1
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REFERENCES
Catia Bastioli, Handbook of Biodegradable Polymers,Rapra
Technology Limited,UK,4-18.
Polymers for Controlled for controlled Drug Delivery
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