5 Biodegradable Polymer

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BIODEGRADABLE POLYMERS

• Biodegradable polymers are the polymers that get decomposed


under aerobic or anaerobic conditions due to the action of
microorganisms or enzymes are called biodegradable polymers

• They are broken down into biologically acceptable molecules that


are metabolized and removed from the body via normal
metabolic pathways.

• They slowly disappear from the site of


administration in response to a chemical reaction
such as hydrolysis.
• Based on biodegradability polymers are
classified as:
1.Biodegradable polymers
eg: collagen, poly glycolic acid etc.,
2.Non biodegradable polymers
eg: poly vinyl chloride, polyethylene etc.,
Ideal characteristics of Biodegradable polymer
They should be biocompatible-(shape, surface, and
leachable)

They should be bio absorbable-(degradability profile,


reabsorption of degradation products.)

They should be bi functional-(physical, mechanical and


biological).

They should be stable-(processing, sterilization and


storage).
Requirement of Biodegradation

i.) Subratrate
ii.) Micro- organism
iii.) Environment- Temperature, pressure, moisture, oxygen.

Decomposition of Biodegradable Polymers

Biodegradable Polymer

Dimmer, Monomer

CO2, H2O CH4/H2S,CO2,H2O


Mechanism Of Biodegradable
Polymers
BIODEGRADATIO
N

ENZYMATIC
DEGRADATIO HYDROLYSIS COMBINATIO
N N

BULK EROSION SURFACE EROSION


Types of bioerosion
1) Bulk erosion
• Degradation takes place
throughout the whole of the
sample.
• Ingress of water is faster
than the rate of degradation
Eg : Polylactic acid (PLA)
Polyglycolic acid (PGA)
2) Surface erosion
– Sample is eroded from the
surface.
– Mass loss is faster than
the
ingress of water into the bulk ,
Eg:Polyanhydride
s
ENZYMATIC OR CHEMICAL DEGRADATION
• Chemical or enzymatic degradation – It is mediated by water,
enzymes, microorganisms.

TRANSFORMATION OF SIDE CHAINS

CLEAVAGE OF CROSSLINKS

CLEAVAGE OF BACKBONE
Classification of biodegradable polymers based on the
source
1) Synthetic biodegradable polymers:
Poly β-hydroxybutyrate – co-β-hydroxy valerate (PHBV)
Nylon 2–Nylon 6
Polyhydroxybutyrate (PHB)
Aliphatic poly(esters)
Polyanhydrides
Polyphosphazenes
Polyaminoacids

2) Natural biodegradable
polymers:
eg: Albumin, Collagen
Pectin, starch
Dextran etc.,
Gelatin
Most attractive class of polymers.

Biocompatible and versatile in


terms of physical, chemical and
biological properties.

 Stability
of the polymer can be
increased as they are chemically
synthesized.
The use of natural biodegradable polymers to deliver drugs
continues to be an area of active research despite the advent
of synthetic biodegradable polymers.

Natural polymers remain attractive primarily because,


 They are derived from natural sources.
 They are easily available.
 They are relatively cheap.
 They qualify for a number of chemical modifications.
 They can be a protein or a polysaccharide in chemical

origin.
Poly β-hydroxybutyrate-co-β-hydroxy valerate
(PHBV)

 It is derived by combining 3-hydroxy butanoic acid


and 3-hydroxy pentanoic acid,

in which monomers are cross-linked by an ester


linkage.

 It decomposes to form carbon dioxide and water.

 It is brittle in nature, and it can be used in the


production of drugs and the manufacturing of bottles.
Poly β-hydroxybutyrate-co-β-hydroxy valerate (PHBV)
Nylon 2–Nylon 6
It is a polyamide copolymerization of
glycine (H2N−CH2−COOH) and
aminocaproic acid (H2N−(CH2)5−COOH).

Polyhydroxybutyrate (PHB): It is formed


by the condensation of hydroxybutyric acid
(3-hydroxy butanoic acid) molecules.
Synthetic biodegradable polymers

1) Aliphatic poly(esters)
• These are prepared by ring opening and polymerization
of
cyclic ester.
• Aliphatic polyesters include:
a) POLY (GLYCOLIC ACID)

b) POLY (LACTIC
ACID)

c)POLY (CAPROLACTONE)
---(--O—C-CH2---)n
POLY (GLYCOLIC ACID)
POLY (LACTIC ACID) --(--O---C—CH---)
Ring-opening polymerization of glycolide can
be catalyzed using different catalysts, including antimony
 compounds, such as antimony trioxide or, zinc compounds
(zinc lactate) and tin compounds like stannous octoate
Stannous octoate is the most commonly used initiator, since it is
approved by the FDA (Food and drug Administration)as a food
stabilizer.
a) POLYGLYCOLIC ACID
• Polyglycolide or Polyglycolic acid (PGA) is a
biodegradable,
thermoplastic polymer and the simplest linear, aliphatic polyester.
• It is a tough fibre-forming polymer.
• insolubility in water.
• polyglycolide is degraded by hydrolysis, and broken down by certain
enzymes.
– Applications
– Used to deliver drugs in the form of microspheres, implants etc.,
– Examples of drugs delivered include steroid hormones, antibiotics, anti
cancer agents etc.,
b) POLYLACTIC ACID
• Polylactic acid or polylactide (PLA) is a thermoplastic aliphatic
polyester derived from renewable resources, such as corn starch,
tapioca products (roots, chips or starch) or sugarcane.

• It can biodegrade under certain conditions, such as the presence of


oxygen, and is difficult to recycle.

• Highly crystalline, high melting point, low solubility.

• Bacterial fermentation is used to produce lactic acid from corn starch


or cane sugar.

 APPLICATIONS
• PLA is used in the preparation of sutures or orthopaedic devices.
Polyesters
c) POLYCAPROLACTONE( TONE POLYMER)

• Polycaprolactone (PCL) is a biodegradable polyester.

• slower degradation rate than PLA.

• Good resistant towards oil, water & chemical solvents.

• It remains active as long as a year for drug delivery.

 Applications:

Drug delivery applications of PCL includes:


- Cyclosporin in the form of nanoparticles

- Ciprofloxacin in the form of dental implants


2) Poly anhydrides
– Highly reactive and hydrolytically unstable.

– Aliphatic (CH2 in backbone and side chains)


polyanhydrides degrade within days.

– Aromatic (benzene ring as the side chain) polyanhydrides degrade


over several years.

– Suitable for short term drug delivery.


– Used for vaccination and localized tumor therapy.
3) polyphosphazenes

• Its hydrolytic stability/instability is determined by change in


side
group attached to macromolecular backbone.

• Used in the construction of soft tissue prosthesis, tissue like coatings,


as material for blood vessel prosthesis.

• Used for immobilization of antigen or enzyme.

• Use for drug delivery under investigation


4) Polyaminoacids
– Aminoacid side-chains offer sites for drug attachment.
– .
– Investigated as suture materials.

– Artificial skin subtitutes .

– Polymers containing more than three or more amino acids may


trigger antigenic response.
Natural biodegradable polymers
• Natural polymers are an attractive class of biodegradable polymers
as they are:
– Derived from natural sources
– Easily available
– Relatively cheap

eg:
Albumin
Collagen
Dextran
Gelatin
Pectin,
1) Collagen
• Collagen is the most widely found protein in mammals and is the
major provider of strength to tissue.

• It is not only has been explored for use in various types of surgery,
cosmetics, and drug delivery, but also in bioprosthetic implants
and tissue engineering of multiple organs as well.

• It is used as sutures ,Dressings,


etc
Applications:
• Majorly used in ocular drug
delivery system
2) Albumin
It is a major plasma protein component.

It accounts for more than 55% of total protein in human plasma.

It is used to design particulate drug delivery systems.

Applications:
• Albumin micro-spheres are used to deliver drugs like
Insulin, Sulphadiazene Prednisolone etc.
• It is mainly used in chemotherapy, to achieve high local
drug concentration for relatively longer time.
3) Dextran

• Dextran is a complex branched polysaccharide made of many


glucose
molecules joined into chains of varying lengths.
• Applications:

• Used for colonic delivery of drug in the form of gels.

4) GELATIN
• Gelatin is a mixture of peptides and proteins produced by partial hydrolysis
of collagen, extracted from the boiled bones, connective tissues, organs and
some intestines of animals. Gelatin is an irreversible hydrolyzed form of
collagen,

 Applications:
 Employed as coating material.
 Gelatin micropellets are used for oral controlled delivery of drugs.
Factors that influence the overall rate
of degradation,
 pH and copolymer composition

 Polymer degradation is accelerated by

More hydrophilic backbone.


More hydrophilic end groups.
More reactive hydrolytic groups in the backbone.
Less crystallinity.

More porosity

 lower average molecular weight,

 Smaller device size


ADVANTAGES OF
BIODEGRADABLE POLYMERS
• Localized delivery of drug

• Sustained delivery of drug

• Stabilization of drug

• Decrease in dosing frequency

• Reduce side effects

• Improved patient compliance

• Controllable degradation rate


APPLICATIONS OF BIODEGRADABLE
POLYMERS
• Polymer system for gene therapy.

• Biodegradable polymer for ocular, tissue engineering,


vascular,
orthopedic, skin adhesive & surgical glues.

• Bio degradable drug system for therapeutic agents such as


antitumor, antipsychotic agent, anti-inflammatory agent.

• Polymeric materials are used in and on soil to improve aeration,


and promote plant growth and health.

• Many biomaterials, especially heart valve replacements and blood


vessels, are made of polymers like Dacron, Teflon and polyurethane.
Medical Applications of Biodegradable Polymers

Wound management Dental applications


 Sutures  Guided tissue
 Staples regeneration Membrane
 Clips  Void filler following tooth
 Adhesives extraction
 Surgical meshes
Cardiovascular applications
Orthopedic devices  Stents
 Pins
 Rods
 Screws Intestinal applications
 Tacks  Anastomosis rings
 Ligaments
Drug delivery system

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