Polymers Used in Drug Delivery Systems

Presented By: Dr. Jawad Ahamd Khan

POLYMERS USED IN DRUG DELIVERY SYSTEM
Outlines

Introduction

Polymers
Monomers
Polymerization
History

Characteristics of ideal polymers

General Mechanism Of Drug Release From Polymers

• Diffusion Mechanism
• Degradation Mechanism
• Water Penetration Mechanism
Outlines…
Classification Of Polymers based on

 Sources
 Nature of Polymer
 Composition
 Properties (Thermal properties)
 Structure
 Polymerization
 Crystallinity
 Tacticity
 Degradability
 Outlines…
Application Of Polymers In Different Dosage forms
• In Tablets
• In Capsules
• In Suspension
• In Emulsion
 Introduction
POLYMERS
The word polymer is derived from Greek word
‘Poly ‘ means many
‘mers ‘means unit or parts.
Definition :
Polymer is composed of molecules with large molecular
mass, Composed of repeating structural units or
monomers connected By covalent and other chemical
bonds.
Polymers are macromolecules built up by the linkage
together of large numbers of much smaller molecules .
 Introduction
Polymers are always complex and giant molecules with carbon
usually use as a backbone .
Example : Poly butadiene = (Butadiene+ Butadiene+........)n
Where n is =4,000.
Monomers :
Small Repeating structural unit derived from some simple and
reactive molecules are linked to each other by covalent bond.
The small molecules which combine with each other to form
polymer
Molecules are termed as Monomers.
Examples:
Ethylene , vinyl chloride, Styrene ,Butadiene ,Acryl nitrite.
 Introduction…
Polymerization :
• The process of formation of polymers is known as
polymerization.
• The process of linking the repeating units ( monomers
)is termed as
• Polymerization.
 Simply the Polymers are the Analogue Of Necklace .
Polymers Used in Drug Delivery Systems…
Polymers Used in Drug Delivery Systems…

IDEAL CHARACTERISTICS OF POLYMERS:

Polymers should be:
• Versatile and possess wide range of mechanical , physical and
chemical properties.
• Non toxic , biodegradable and compactable with API (Active
Pharmaceutical Ingredients).
• Strength For easily administration .
• Temperature resistance.
• Inexpensive.
• Good moulding ability
• Low density
 Mechanism Of Drug Release From Polymers

Diffusion Degradation Water Penetration

Mechanism Mechanism (Swelling
Mechanism)

Reservior Matrix
System System
 Mechanism of Drug Release from Polymers

Mostly there are three methods from which the drug released
from polymers

1.Diffusion
2.Degradation
3.Water Penetration (Swelling )

DIFFUSION MECHANISM :
Diffusion : Movement of molecules from high to low concentration.
•It is rate limiting step and is used to control the release
of drug .
•Follow zero Order of kinetics.
•Remain in body for long period of time.
Mechanism of Drug Release from Polymers…

There are two types of Diffusion mechanism .

• 1.Reservier
• 2.Matrix
• 1.Reservoir System :
• Type of Diffusion mechanism.
• In which drug is store or reserve in a core(Centre) and
that core is surrounded by the layer of
polymers.
• Drug is release by diffusion through rate controlling
membrane.
• Example : Poly ( N-vinyl Pyrrolidone ).
Polymers Used in Drug Delivery Systems…

2.Matrix System :
• It is type of Diffusion mechanism.
•It also follow the Zero order of kinetics
•In this type the drug released in controlled manner.
• The drug is distributed internally within core and this
core is covered with Mesh (Network like structure) of
polymers.
•It is most beneficial method of diffusion in which equal
and fixed concentration of drug is released in body.
Polymers Used in Drug Delivery Systems…
Reservior System

Matrix System
Polymers Used in Drug Delivery Systems…
2. Biodegradation( Degradation ) Mechanism :
 The drug molecule which are initially dispersed in the
polymer are release as the polymer start eroding or
degrading .
 It is also known as Bio erodible System.
 This mechanism control the dissolution and diffusion of
the drug .
 First process of dissolution occur then diffusion take
place from membrane of polymers.
Example : Poly( Lactic co glycolic acid).
Polymers Used in Drug Delivery Systems…
3.Water Penetration ( Swelling):
• Initially this swelling process of drug release from polymer is dry.
• When placed with body absorb water, and other fluids and
become swells. After some time the polymers adhere more water
as result the
Membrane become burst and drug rapidly release from polymers.
Example : Ethylene vinyl alcohol

Swelling Mechanism
Classification of Polymer

Based on Nature of Based on

Sources Polymer Composition

Based on Based on Based on

Properties Structure Polymerization

Based on Based on Based on

Crystallinity Tacticity Degradabilities
 Based on Sources

Natural Synthetic Semi – Synthetic

Vulcanized rubber gum
Protein Cotton
Carbohydrate Cellulose
Nucleic acid

Biodegradable Non- biodegradable

Lactides Acrolein (propenal)
Glycolides Epoxypolymer
Polyanhydrides
Natural Polymers
Natural polymer are derived from natural sources and can
be polysaccharides and proteins in chemical natural.

Examples
Collagen
Albumin
Starch
Resin
Silk
Protein
Wool
Natural alginate
rubber etc.
Synthetic Polymer
Synthetic polymer are of artificial polymer/ origin which
consist of fibers.

Examples
Teflon
Dacron
Polystyrene
Synthetic Rubber
Plastic &
PVC.
 Synthetic Polymers are further classified into two main
categories
Biodegradable Polymers

Natural Biodegradable
These polymers are very common in natural bio-degradable
polymer

Examples
Collagen, Albumin, Gelatin hemoglobin etc.
(They have been studied for medical and pharmaceutical
applications)
Synthetic Biodegradable

These type of polymer are preferred rather than NBD polymers due
to their internees and easy and cheap formulation.

Synthetic Biodegradable polymers have following advantages over

natural ones.

 Localized delivery of drugs

 Sustain delivery of drug
 Stabilization of drug
 Reduced side effect etc.

Examples

Poly lactic acid

Polyester (PET)
Semi-Synthetic Polymer
These polymers are derived from natural occurring
polymers by means of chemical modification.

Examples

Vulcanized Rubber Gum

Cotton
Cellulose diacetate
HPMC polyethylene
GPA
LPA
Polyhydoxy butyrate
Polyanhydride
 Nature of Polymer (Polarity)

Water Soluble (Polar ) Water insoluble (Non polar)

Polar Polymer are more Typical non-hygroscopic
soluble/ permeable to water don’t absorb water but can
than non-polar polymers. pickup moisture on the
granule surface in high
humidity atmosphere,
Example:- Example:-
High polarity 1) Ethyl cellulose
1) Polyethylene terephthalate (PET) 2) Polydimethyl siloxane
2) Epoxy
3) Poly Carbonate
4) Poly Chloroprene
5) Cellulose derivative
6) Xanthane gum
7) Chitosa
 Based on Composition

Homopolymer Co-polymer/Heteropolymer

Alternating Random Block

co-polymer co-polymer co- polymer
1) Homopolymer:-
polymers formed from one kind of monomer are called
Homopolymer
like:- A-A-A-A-A
Example :- Polyethylene, Polystyrene
2) Co-polymer :-
Polymers formed from more than one kind of monomer
unit is called a co-polymer or mixed polymer.
like :- A-B-C-A-B-C -A-B-C
Examples
Silicon containing co-polymer, Ethyl cellulose.
(a) Alternating Co-polymer
Two polymer are arrange in an alternative way.
Like :- A – B – A – B – A – B

(b) Random Co-polymer

Monomers are arrange in any orders
Like :- A- A- B – A – A – B – A – A
(c) Block Co-polymer
Some time each monomer can join with the same
type of monomer and than the two blocks of
homopolymer join
Like:- A – A – A – B – B – B
 Based on properties
(Thermal Response) OR (Molecular Force)

 Can not be reused/recycle

1) Thermoset Polymers:- These polymer’s are cross or branched
molecules .
 On heating under go extensive cross linking in mould to form an
insoluble, infusible network.
 Temperature above 200oC (392oF)
 Also called thermosetting plastic.
Example:- Bakelite, urea-formaldehyde resins,
2) Thermoplast Polymers :- These consist of linear or branched chain
molecule
 Soften when heated.
 Their hardness is temporary
 They can be reshaped
 Also called as thermoplasting / Thermo softening plastic
Example:- PVC, nylons etc
3) Elastomers:- These are the linear or slightly branched
chain molecules.
Capable of repeatedly softening on heating and hardening in
cooling.
Example:- Polythene, Polystyrene etc.
 Based on Structure

Linear polymers Branched Chain polymer Cross linked polymer

The Smallest repeating unit Contain linear chain having Formed from Bi functional,
arrange in straight line path some branches Tri functional monomers contain
strong covalent bond

Linear Branched Chain Cross linked

Example Example Example
PVC Low-density/ Backlite

High-density polythane melamine

Polythane
Linear Polymer
The Smallest repeating unit arrange in straight line path
Example:- PVC , High-density or Polythane
Branched Polymer
Contain linear chain having some branches
Example:-Low-density or polythane
Cross linked
Formed from Bi functional, Tri functional monomers
and contain strong covalent
Example:- Backlite, melamine
Based on Polymerization OR Mode of formation

Addition polymer Condensation polymers

When unsaturated carbon (organic) When Bi functional molecules react to
Molecules react to form a long chain form a long chain polymer molecule.
molecule.
And no small molecule or atoms are Small molecule such as water are
eliminated during the reaction eliminated during the reaction.
Eg:- Ethylene Polyethylene Eg:- terylene
n(CH2 = CH2 CH2 - CH2)
 Based on Polymer Crystallinity

Crystalline polymer Amorphous polymer

Lamellar chain/ crystalline form in Amorphous form in which
which chain fold and make lamellar chain arranged in the
Structure arrange in the regular manner. irregular manner.
Transparent Opaque/ Translucent
Hard Soft
Good chemical resistance Poor chemical resistance
 Based on Tacticity

Isotactic Atactic Syndistactic

Polymer Polymer Polymer
Side group of the Side Group are Side group of polymer
monomer lie on the arranged in an are arrange in an
same side of the irregular or random alternative manner
chain . manner around the Main chain

CH3 CH3 CH3 CH3 CH3 CH3 CH3 CH3 CH3

-C - C - C - C- -C- C -C -C-C–C- -C- C -C -C-

CH3 CH3 CH3

 Based on Degradability
Biodegradable Polymer
Those which can be degraded in body fluids e.g

PLA&

Polycaprolactone

No-biodegradable
Those which cannot be degrade in body fluids e.g

Ethyl cellulose &

Cellulose acetate
APPLICATION OF POLYMERS IN DIFFERENT DRUG PRODUCTS
Polymers are widely used in various formulations and major role
in pharmaceutical technology.

 The major aim of polymer production is to ‘ formulate new

drugs which must be safe ,effective with best quality .

 Polymers are also use to improve the organoleptic properties,

increase patient compliance by decreasing the frequency of
dosing.

Polymers in DDS:
In modified drug delivery system
In Controlled drug Delivery System
In immediate drug Delivery System
Polymers Used in Drug Delivery Systems…
In Tablets:
Binder : M.C (Methyl Cellulose)H.E.C (Hydroxy Ethyl Cellulose )
Disintegrating Agent: H.M.C(Hydroxy Methyl Cellulose).

In Capsules :
Gelatin is natural polymer mostly used in capsules .

In Suspension :
Suspending Agent : Acacia , tragacanth , Cellulose derivatives .

In Emulsion:
Emulsifying Agent : Tragacanth ,Spans , Tween s .
Thank You