Polymers in NDDS

Unit 1 (part-2)

Presented by:
Makhan Lal Khaira
(M. Pharm)
Email [email protected]

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Polymers:
• The compounds having high molecular masses and formed by
monomers are termed polymers.
• The term polymer is derived from the Greek words, poly means many
and meros means unit or parts.
• Due to their distinctive nature, polymers are used in pharmaceutical
industries.
• In polymer based drug release system, a new technology has been
adopted that provides possibilities in drug administration.
• Polymers are pharmaceutically used in tablets as binders
• In liquids, suspensions and emulsions as flow controlling agents
• To cover the unpleasant taste of drug as film coating agents
• Also as stabilizers and protective agents.
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Properties of Polymers:
• Many materials are used for controlling the release of drugs and other
active agents.
• Initially the earliest of these polymers were chosen due to their
desirable physical properties. Some examples are:
1) Poly(urethanes) for elasticity,
2) Poly(methyl methacrylate) for physical strength and transparency,
3) Poly(vinyl alcohol) for hydrophilicity and strength,
4) Poly(ethylene) for toughness and lack of swelling, and

An ideal polymer should have the following properties:

1) It should be inert and compatible with the environment,
2) It should be non-toxic,
3) It should be easy to administer,
4) Its fabrication should be easy and inexpensive, and
5) It should have a good mechanical strength. 3
Advantages of Polymers:
Polymers have the following advantages:
1) It delivers drug at a constant rate of controlled release for a
prescribed time period.
2) The carrier of polymer degrades into non-toxic and absorbable sub-
units that get metabolized lately.
3) The system is biocompatible, does not exhibit dose dumping at any
time period, and the polymer retains its properties until after drug
depletion.
4) They breakdown into biologically acceptable molecules which get
metabolised and eliminated from the body via normal metabolic
pathways.

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Advantages of Polymers cont..
The following three advantages are offered by polymeric drug delivery
products are:
1) Localised Drug Delivery: The product can be implanted straight to the
site where drug action is required,
2) Sustained Drug Delivery: The encapsulated drug is released for
prolonged time period, .
3) Stabilisation of the Drug: The polymer can guard the drug from
physiological surrounding, and thus improves in vivo drug stability.

Disadvantages of polymers:
Polymers have the following disadvantages:
1) They cannot tolerate extreme temperature; for example, plastics
immediately melt down on coming in contact with heat.
2) Biodegradable polymers show substantial dose dumping at some points
after implantations. 5
Polymer classification:
Classification of polymers
Based on the
Based upon Based on Based on mode
Based on Nature of
origin of molecular of
structure polymer-water
source forces polymerization
interaction

1. Natural 1. Linear 1. Addition 1. Hydrophobic

1.Elastomers
polymers polymers Polymer polymers

2. Branched 2.
2. Semi- 2. Hydrophilic
chain 2. Fibers Condensation
synthetic polymers
polymers polymers

3. Cross-
3. Synthetic 3.Thermoplast
linked 3. Hydrogels
polymers ics
polymers

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Polymer classification cont..
Classification of polymers based on source
1. Natural polymers:
• These are derived from natural sources and can be polysaccharides and protein
in chemical nature.
• For example: Albumin, Cellulose, Starch, Rubber, Wool.
2. Semi-synthetic polymers:
• These types of polymers are derived from naturally occurring polymers by
means of chemical modifications.
• For e.g. Vulcanized rubber, Gun cotton, Cellulose diacetate, HPMC, etc.
3. Synthetic polymers:
• Synthetic polymers are of artificial origin which consist of fibers.
• This is the polymer, which was prepared by Laboratory is known as Synthetic
Polymer.
• For example: Buna-S, Buna-R, Nylon, Polythene, Polyester.
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Classification Based on Structure
1. Linear polymers:
• The smallest repeating unit arranged in straight line path is known as
Linear polymer.
• For example: PVC.
2. Branched chain polymers:
• Contain linear chains having some branches.
• For example: low density polymer, Polyethylene, HPLD polyethylene.
3. Cross linked chain polymers:
• In this type, all molecules are chemically bonded together, forming a three-
dimensional network.
• Cross-linked polymers are produced from linear and branched polymers or
directly from chemical precursor.
• For e.g. Natural rubber, polyacrylamide gels, epoxies, alkyd resins, etc.
Linear polymers Cross-linked chain polymers Branched chain polymers 8
Classification Based on Polymerization
1. Additional polymers:
• Additional polymers are formed by the repeated addition of monomer
molecules possessing double or triple bonds.
• n(CH2 = CH2) − (CH2 − CH2)−
• Ethylene polyethylene
2. Condensation polymers:
• Condensation polymers formed by repeated condensation reaction
between two different bi-functional or tri- functional monomeric
units. For e.g. terylene (dacron), nylon 6, 6,

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Based on the Nature of Polymer-Water Interaction
1) Hydrophobic Polymers:
• These polymers are water-insoluble due to the presence of non-polar
functional groups.
• Ethyl cellulose and polydimethyl siloxane are the examples of
hydrophobic polymers.
2) Hydrophilic Polymers:
• These polymers are water-soluble due to the presence of polar or
charged functional groups.
• HPMC, NaCMC, chitosan, sodium alginate, etc. are the examples of
hydrophilic polymers.
3) Hydrogels:
• These polymers swell (but do not dissolve) on coming in contact with
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water.
Based on the other Types or types of Monomer
Based on the types of monomers, polymers are classified into the following two
types:
1) Homopolymers: These polymers contain a single type of repeat unit.
Polystyrene is an example of homopolymer.
2) Hetropolymers (Copolymers): These polymers are made up of two different
monomers. Butadiene-styrene rubber is an example of heteropolymer.
Based on the Morphology Based on their morphology, polymers are classified
into the following two types:
1) Crystalline Polymers: These polymers do not always form perfect crystalline
materials, but are semi-crystalline having crystalline as well as amorphous
regions. In such polymers, the crystalline phase is distinguished by their melting
temperature (Tm).
2) Amorphous Polymers: These polymers are distinguished by their glass
transition temperature [Tg, temperature at which they undergo sudden
transformation from glass state (hard) to the rubbery state (soft)]. This transition
resembles to the onset of chain

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Based on the Molecular Forces
The mechanical properties of polymers, such as tensile strength, toughness, and
elasticity, rely on intermolecular forces, such as Van der Waals forces and hydrogen
bonding. Based on these forces, polymers are classified into the following types:
1) Elastomers: These polymers are rubber-like solids having elastic properties.
The polymer chains in elastomers are linked to each other by the weakest
intermolecular forces. Due to these weak forces, the polymer becomes
stretched. Few crosslinks are added between the chains to help the polymer to
retract to its original point after the force is released (as in vulcanised rubber).
Buna-S, buna-N, neoprene, etc. are the examples of elastomers.
2) Fibres: These are thread-forming solids having high tensile strength and
modulus. These properties can be allocated to the strong intermolecular forces
(such as hydrogen bonding), which lead to close packing of chains and impart
crystalline nature. Fibres are used in textile industries. Polyamides (nylon 6,6),
polyesters (terylene), etc. are the examples of fibres.
3) Thermoplastic Polymers: These polymers have intermolecular forces between
elastomers and fibres. They can be softened on heating and toughened on cooling at
room temperature. They are either linear or branched chain polymers. They can be
recycled multiple times. Polythene, polystyrene, PVC, etc. are the examples of
thermoplastic
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4) Thermosetting Polymers: These polymers are hard and become
infusible on heating. They do not soften on heating under pressure
and they cannot be remoulded. They are either cross-linked or
heavily branched molecules. They are not reusable. Bakelite,
Based on the Degradability
Based on the capability to degrade, polymers are classified into the following
two types:
1) Non-Biodegradable Polymers: These polymers do not undergo natural
degradation in the body. Polyethene Vinyl Acetate (PVA), Polyethene Vinyl
Chloride (PVC), Polydimethyl Siloxam (PDS), Polyether Urethane (PEU),
Ethyl Cellulose (EC), Cellulose Acetate (CA), and polyethylene are the
examples of non-biodegradable polymers.
2) Biodegradable Polymers: These polymers undergo natural degradation in
the body. Polycaprolactone (PCL), Polylactic Acid (PLA), Polyglycolic Acid
(PGA), Poly(Lactic-co-Glycolic) Acid (PLGA), etc. are the examples of13
biodegradable polymers.
Based on the Structure of Polymers
Based on the structure, polymers are classified into the following three
types:
1) Linear Polymers on Structure: In these polymers, the monomers
are linked with one another and make a long straight chain.
Polyethene, PVC, nylons, polyesters, etc. are the examples of linear
polymers
2) Branched Chain Polymers: These polymers possess a straight long
chain having different side chains.

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Application of Polymers in Formulation
CRDDS
1) Controlled Release Dosage Forms:
i) Reservoir systems,
ii) Biodegradable systems, vi) Osmotically controlled drug delivery,
iii) Temperature responsive drug release,
iv) pH responsive drug release,
v) Electric current responsive drug release, and
vi) Polymer-drug conjugates.

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Application of Polymers in Formulation
CRDDS cont..
2) Immediate Release Dosage Forms
i) Tablets: Polymers are being used since many years as excipients in
conventional immediate‐release oral dosage forms. They either assist the
manufacturing process or provide protection to the drugs from degradation
upon storage. Microcrystalline cellulose is used as a diluent (as a substitute
to carbohydrates) in tablet formulations of highly potent low‐dose drugs.
Starch and cellulose are used as disintegrants in tablet formulations as they
swell in water and result in tablet bursting, which increases the exposed
surface area of the drug and improves its dissolution. Polyvinyl‐pyrrolidone
and hydroxypropyl methylcellulose polymers are used as binders to aid in the
formation of granules, which improve the flow and compaction properties of
tablet formulations before tableting.
ii) Capsules: Nearly same polymeric excipients are used to bulk out capsule
fills as used in immediate release tablets. Gelatin is used as a shell material
for hard (two‐piece) and soft (one‐piece) capsules. HPMC is used as an
alternative material for manufacturing hard (two‐piece) capsules.
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2) Modified Release Dosage Forms: It is known that many therapeutic drug
delivery using immediate release dosage forms results in sub-optimal therapy
and/or systemic side effects. Pharmaceutical scientists have made efforts to develop
modified release dosage forms so that the limitations of conventional oral dosage
forms can be overcome.
3) Extended Release Dosage Forms: The drugs having short biological halflives
are formulated as extended or sustained release dosage forms in order to enhance
their therapeutic effect. Extended and sustained release dosage forms extend the
time for which systemic drug levels remain within the therapeutic range. This
reduces the number of doses the patient needs to take to exert a therapeutic effect,
and thus increases patient compliance.
Ammonium methacrylate copolymers (Eudragit RS and RL), cellulose derivatives
(ethylcellulose and cellulose acetate), and polyvinyl derivative (polyvinyl acetate)
are the examples of most commonly used water-insoluble polymers for extended
release systems. The proportion of quaternary ammonium groups in Eudragit RS
and RL is different, due to which water permeability of Eudragit RS is 17
comparatively low.
4) Gastroretentive Dosage Forms:
These dosage forms offer an alternative strategy to achieve extended
release profile, in which the formulation remains in the stomach for
prolonged time periods which dissolves in the liquid contents and
slowly passes as into the small intestine.

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