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Polymers

Chapter polymers
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51 views16 pages

Polymers

Chapter polymers
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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INTRODUCTION

• Polymers are complex and giant molecules usually with carbons building the backbone. They are different from
low molecular weight compounds.
• The small individual repeating units/molecules are known as monomers (means single part).
• A polymer with two different monomers is known as a copolymer. While a polymer with one type of monomers
is known as a homopolymer.
Definition:
Polymers are very large molecules made when hundreds of monomers join together to form long chains.
CHARACTERISTICS OF POLYMERS
• Low Density.
• Low coefficient of friction.
• Good corrosion resistance.
• Good mouldability.
• Excellent surface finish can be obtained.
• Can be produced with close dimensional
tolerances.
• Economical.
• Poor tensile strength.
• Low mechanical properties.
• Poor temperature resistance.
• Can be produced transparent
or in different colors
Classification based on source
1. Natural polymers- The definition of a natural polymer is a polymer that results from only raw materials that
are found in nature. Example- Proteins, Cellulose, Starch, Rubber.
2. Semi-synthesis polymers– The polymer can obtained both Natural as well as Synthetic origin is known as
Semisynthetic polymer. Example- Cellulose derivatives- Cellulose acetate (Rayon).
3. Synthesis polymers- The polymer that could be prepared by Laboratory is known as Synthetic Polymer.
Example- Buna-S, Buna-R, Nylon, Polythene, Polyester
Classification based on structure
• 1. Linear polymers- the smallest repeating unit arrange in straight line path is known as Linear polymer. Example- pvc.
• 2. Branched chain polymers- contain linear chains having some branches. Example- low density polymer.
• 3. Cross linked chain polymers- formed from bi-functional and tri-functional monomers and contain strong covalent
bonds. Example- bakelite, melamine.
Classification based on molecular force
➢ Elastomers: The polymers which undergo very long elongation when pulled apart, and return to their original length on
release are called elastomers. Example Natural rubber, Buna-S, etc.
➢ Fibers: These are long, thin and thread like polymers, whose length is at least 100 times their diameter. They do not
undergo stretching and deformation like elastomers. Example jute, wood, silk.
Classification based on polymerization
➢ Addition polymers
• formed by the repeated addition of monomer molecules possessing double or triple bonds.
n(CH2=CH2) Ethylene -(CH2-CH2 )- Polyethylene
• One form of polymer is converted into anther form of polymer with loss of atoms or ions
from molecules.
➢ Condensation polymers
• formed by repeated condensation reaction between two different bi-functional or tri
functional monomeric units. e.g. terylene (dacron), nylon 6, 6, nylon 6.
• One polymer can be converted into anther form of polymer without loss of atoms or ions
from molecules.
GENERAL MECHANISM OF DRUG RELEASE FROM
POLYMERS
• Three primary mechanisms for drug release, namely:
➢ Diffusion
➢ Degradation
➢ Water penetration (Swelling)
• Any of these mechanisms can occur in a given release system.
Drug release from polymer by diffusion
• The rate limiting step is the diffusion of drug through inert water insoluble membrane barrier.
• There are two types:
• a) Reservoir
• b) Matrix
Reservoir diffusion system
• In membrane-controlled reservoir devices, the drug is contained in a core, which is surrounded by a polymer
membrane, and it is released by diffusion through this rate controlling membrane
• e.g. Poly(N-vinyl pyrrolidone),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.
• Such as polyethylene , polyvinylacetate

Degradation
The drug molecules, which are initially dispersed in the polymer, are released as the polymer starts eroding or
degrading.
• The four most commonly used biodegradable polymers in drug delivery systems are poly(lactic acid),
poly(lactic-co-glycolic acid), polyanhydrides, poly(ortho esters), and poly(phosphoesters).
Water penetration (swelling)
• This type of systems are initially dry and when placed in body, absorb water or other fluid and it swells.
• Swelling increases aq. solvent content within the formulation as well as the polymer mesh size, enabling the
drug to diffuse through the swollen network into the external environment.
E.g (N-isopro-pylacrylamide), Ethylene-vinyl alcohol
BIO DEGRADATION OF POLYMERS
• Bio degradation is the chemical changes that alter the molecular weight or solubility of the
polymers.
• Bio erosion may refer to as physical process that result in weight loss of a polymer device.
• The erosion of polymers basically takes place by two methods:
1. Hydrolytic mechanism
2. Enzymatic mechanism
Hydrolytic Mechanism
• Hydrolytic degradation of polymers may be defined as the breaking of chemical bonds in
the polymer backbone by the
attack of water to form oligomers and finally monomers.
• This kind of hydrolysis could not require of specific biological compounds as proteases.
• All biodegradable polymers contain hydrolysable bonds like glycosides, esters, orthoesters,
anhydrides, carbonates, and
amides.
• Rate of hydrolytic degradation is modulated by the hydrophilic characteristics of the
polymers.
Enzymatic mechanism
• Enzymes are biological catalysts.
• They accelerate reaction rates in living organisms without undergoing themselves any
permanent change.
• Hydrolysis reactions may be catalyzed by enzymes known as hydrolases, which include
proteases, esterases, glycosidases, and phos- phatases.
• Enzymatic surface degradation occurs when enzymes cannot penetrate the interior of the
polymer, due to high cross-link density or limited access to cleavage points, forcing the surface
or exterior bonds to cleave first.
SYNTHESIS OF POLYMERS

INITIATION
The first step in chain polymerization- Initiation involves the formation of a free radical. Each
initiating radical has the ability to attack the double bond of a monomer. In this way, the
radical is transferred to the monomer and a monomer radical is produced. Addition can
occur at either end of the monomer.
PROPAGATION
• The monomer radical is also able to attack another monomer and then another
monomer, and so on and so forth. This step is called propagation by which a macro radical
is formed. The entire propagation reaction usually takes place within a fraction of a second.
TERMINATION
• Chain termination is the chemical reaction that ceases the formation of reactive
intermediates in a chain propagation step in the course of polymerization.

APPLICATIONS OF POLYMERS IN FORMULATION OF CONTROLLED DRUG


DELIVERY SYSTEM
1. ORAL DRUG DELIVERY SYSTEM:
• Here, the drug gets released at controlled rate when administered orally. For that several
mechanisms are involved:
• a) Osmotic pressure controlled GI delivery system
• b) Gel diffusion controlled GI delivery system
• c) Muco-adhesive GI delivery system.
2. 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 releases the drug from the device
to the skin.

3. Ocular drug delivery system


• It allows prolonged contact of drug with corneal surface of eye. The example for ODDS 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
Co polymers of acetate vinyl & ethyl
Others:
✓ Drug delivery and the treatment of diabetes
✓ Drug delivery of various contraceptives and hormones
APPLICATIONS OF POLYMERS
✓ 1) DRUG DELIVERY OF VARIOUS CONTRACEPTIVES & HORMONES: E.g. medroxyprogesterone acetate–
vaginal contraceptive ring It consists of a drug reservoir & polymer coating material. Through this layer the drug
releases slowly.
✓ 2) DRUG DELIVERY AND THE TREATMENT OF DIABETES:
• Here the polymer will act as barrier between blood stream & insulin. E.g. polyacrylamide or
N,Ndimethylaminoethylmethacrylate

3) APPLICATIONS OF POLYMERS IN SOLID DOSAGE FORMS:


➢ IN TABLETS
• Polymers like methyl cellulose, hydroxyl ethyl cellulose, hydroxyl ethyl methyl cellulose are
used as binders.
• Polymers like carboxyl methyl cellulose sodium is used as disintegrating agent.
• Polymers like all the cellulose derivative are used as coating materials.
• Polymers like cellulose acetate phthalate, hydroxyl propyl methyl cellulose phthalate,
polyvinyl acetate phthalate are used as enteric coating material.
➢ IN CAPSULES
• Gelatin, a natural polymer which is the major ingredient in the manufacturing of capsules.
4) APPLICATIONS OF POLYMERS IN LIQUID DOSAGE FORMS:
➢ IN SUSPENSIONS
• Polymers like Acacia, Tragacanth, Cellulose derivative, Xanthum gum are used as suspending agents. They
should be selected based on their characters like PH, solubility & concentration. They enhances the dispersion
of solids in liquids.
➢ IN EMULSIONS
• Polymers like Tragacanth, Spans, Tweens are used as emulsifying agents.

5) Polymers can be used as film coatings to mask the unpleasant taste of a drug & to modify drug release
characteristics.
✓ 6) Polyanhydrides are used in DDS because of their unique property of surface erosion.
✓ 7) Hyaluronic acid is used in controlled release ophthalmic preparations.
✓ 8) Wide variety of polymers like natural gums are using as thickening agents. E.g. poly ethylene glycol,
carbomer
✓ 9) Some of the polymers are using as protective colloids to stabilize suspensions & emulsions. E.g .
Sodium alginate
✓ 10) Some polymers can be used as suppository bases E.g. poly ethylene glycol
11) Some polymers are used in uterus therapeutic system E.g. silicone
✓ 12) Copolymers of lactide & glycolide, silicone are using in implantation therapeutic system.
✓ 13) Polyurethanes can be used for elasticity.
✓ 14) Polymethyl methacrylate for physical strength & transparency.
✓ 15) Polyvinyl alcohol for hydrophilicity & strength
✓ 16) In addition to polymers being used as excipients, some drugs themselves are polymers including
insulin, heparin & its antagonist, protamine sulfate, plasma expander like dextran, normal human serum
albumin, bulk laxatives like methyl cellulose & sodium carboxy methyl cellulose.

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