Polymer

By
ADITHIYAN. D
M.Pharm
Pharmaceutics
INTRODUCTION
The application of the polymeric materials for medical purposes is growing fast
Polymers have found applications in diverse biomedical fields such as drug delivery systems,
developing scaffolds in tissue engineering, implantation of medical devices and artificial
organs, prosthesis, ophthalmology, dentistry, bone repair, and many other medical fields.
Polymers have been used as a main tool to control the drug release rate from the
formulations. Extensive applications of polymers in drug delivery have been realized because
polymers offer unique properties which have not been attained by any other materials.
Advances in polymer science have led to the development of several novel drug delivery
systems. A proper consideration of surface and bulk properties can aid in the designing of
polymers for various drug delivery applications. These newer technological development
include drug modification by chemical means carrier based drug delivery and drug
entrapment in polymeric matrices or within pumps that are placed in desired compartments
These technical development in drug delivery/targeting approaches improve the efficacy of
drug therapy thereby improve human health. Polymer chemists and chemical engineers,
pharmaceutical scientists are engaged in bringing out design predictable, controlled delivery
of bioactive agents.
Extensive Biodegradable polymers have been widely used in biomedical applications
because of their known biocompatibility and biodegradability. In the biomedical area
polymers are generally used as Implants and are expected to perform long term service.
These improvements contribute to make medical treatment more efficient and to minimize
side effects and other types of inconveniences for patients. The pharmaceutical applications
of polymers range from their use as binders in tablets to viscosity and flow controlling agents
in liquids, suspensions and emulsions. Polymers can be used as film coatings to
disguise/mask the unpleasant taste of a drug, to enhance drug stability and to modify drug
release characteristics Pharmaceutical polymers are widely used to achieve taste masking,
controlled release targeted release enhanced stability and improved bioavailability.
The word ‘polymer’ comes from the Greek words poly (meaning ‘many’) and meros
(meaning ‘parts’). A polymer is a large molecule made up of many small repeating units. In
the early days of polymer synthesis, little was known about the chemical structures of
polymers. Hermann Staudinger, who received the Nobel Prize in Chemistry in 1953. coined
the term "macromolecule" in 1922 and used it in reference to polymers. The difference
between the two is that polymers are made of repeating units, whereas the term
macromolecule refers to any large molecule. not necessarily just those made of repeating
units. So, polymers are considered to be a subset of macromolecules.
Thus Polymers are very large molecules made when hundreds of monomers join
together to form long chains. From the structural prospective, monomers are generally
classified as olefinic (containing double bond) and functional (containing reactive functional
groups) for which different polymerization methods are utilized. If two, three, four or five
monomers are attached to each other, the product is known as a dimer, trimer, tetramer, or
pentamer, respectively. An oligomer contains from 30 to 100 monomeric units. Products
containing more than 200 monomers are simply called a polymer. From a thermodynamic
perspective, polymers cannot exist in the gaseous state because of their high molecular
weight. They exist only as liquids or high solid materials.
CLASSIFICATION OF POLYMERS
 BASED ON THE SOURCE
o NATURAL Occurs in nature and known as biopolymers. Ex- natural rubber,
natural silk and cellulose.
o SEMI-SYNTHETIC Chemically modified natural polymers. Ex- methyl
cellulose, cellulose nitrate and cellulosic.
o SYNTHETIC Synthesized in the laboratory known as manmade polymer. Ex-
polyvinyl alcohol, polyethylene and polysulfone.
 BASED ON THE TYPES OF POLYMERISATION
o ADDITION POLYMER They formed from simple addition of monomer
molecules to each other in a quick succession by a chain mechanism. Ex-
polyethylene, polystyrene and polypropylene.
o CONDENSATION POLYMER They are formed from intermolecular
reactions between bifunctional or polyfunctional monomer molecule having
reactive functional groups, such as –OH, -COOH, -NH2. Ex- polyesters and
polyurethane.
 BASED ON THE DEGRADABILITY
o BIODEGRADABLE They degrade naturally in the body. Ex- PLA, PGA,
polycaprolactone (PCL).
o NONBIODEGRADABLE They are not degraded naturally in the body. Ex-
polyethylene vinyl acetate (PVA), ethyl cellulose (EC), cellulose acetate (CA).
 BASED ON THE POLYMER WATER INTERACTION
o HYDROPHOBIC POLYMER They contain non-polar functional groups,
making them water insoluble. Ex- ethyl cellulose, polydimethyl siloxane.
o HYDROPHILLIC POLYMER They contain polar or charged functiional
groups, making them water soluble. Ex- sodium alginate, chitosan and HPMC.
o HYDROGEL POLYMER They swell but do not dissolve when brought in
contact with water. Ex- polyhydroxy ethyl methyl acrylate, polyvinyl alcohol
(PVA), PVP.
 BASED ON THE STRUCTURE OF POLYMER
o LINEAR POLYMER In this polymer monomers are linked with each other
and form a long straight chain, these chains do not have any side chains. Ex-
polyethene, PVC and polyesters.
o BRANCHED CHAIN POLYMER They have a straight long chain with
different side chains. Ex- polypropylene, amylopectin and glycogen.
o CROSS-LINKED POLYMER In this polymer two liner chains are joined
together by covalent bonds and it have three dimensional. Ex- bakelite,
vulcanised rubber and formaldehyde resins.
 BASED ON THE TYPES OF MONOMER
o HOMOPOLYMER A polymer containing a single type of repeat unit. Ex-
Polystyrene.
 o HETEROPOLYMER (COPOLYMER) If a polymer is made up two different
monomers then it is called copolymer. Ex- Butadiene – styrene rubber.

 BASED ON THE MOLECULAR FORCES

o ELASTOMERS These are rubber-like solids with elastic properties. The
polymer chain chains are held together by the weakest intermolecular forces,
which permits the polymer to be stretched. Ex- buna-S and neoprene.
o FIBERS Fibres are the thread forming solids which posses high tensile
strength and modulus, which can be attributed to the strong intermolecular
forces like hydrogen bonding. Ex- polyamides (nylon 6, 6), polyesters, etc.
o THERMOPLASTIC POLYMERS These polymers having intermolecular
forces between elastomers and fibres, they can be softened on heating and
hardened on cooling and can be recycled many times. Ex- polythene,
polystyrene, PVC.
o THERMOSETTING POLYMERS These polymers are hard and infusible on
heating they are not remoulded also they are non-recyclable. Ex- bakelite,
urea-formaldehyde resins, etc.

PROPERTIES OF POLYMER 
In the field of pharmaceuticals mechanical and viscous properties of polymer are
majorly considered. It has been explained detailed with other general properties of
pharmaceutical polymers.
Mechanical Properties of the polymer will depend upon their structure, molecular
weight, and inter molecular forces. polymers resist differently when they are stressed. They
can resist against stretching (tensile strength). compression (compressive strength). bending
(flexural strength). sudden stress (impact strength). and dynamic load ing (fatigue). With
increasing molecular weight and hence the level of intermolecular forces, polymers display
superior properties under an applied stress. As far as structure is concerned, a flexible
polymer can perform better under stretch ing whereas a rigid polymer is better under
compression. This properties has been considered during selection of polymer for transdermal
drug delivery.

Viscous of the substance will greatly influence the flow property of the substance.
Where polymer will show an viscous properties which is used in liquid pharmaceutical
preparations. As molecular weight increases, polymer chains are more likely entangled into
each other at certain molecular weights. This results in poor polymer flow either in solid state
(as a melt) or in solution state (as a solution). For many applications, there is a working range
of molecular weights that a given polymer in solid or solution state can successfully be
processed.
The varied structure and chemistry of polymer provide an ample opportunity for
complex.
APPLICATION OF POLYMER IN PHARMACEUTICALS
Where polymer are used in dosage form to enhance product performance and also
they where used as drug carrier which has been discussed below,
Immediate release dosage forms
Tablets
Polymers have been used for many years as excipients in conventional immediate-
release oral dosage forms, either to aid in the manufacturing process or to protect the drug
from degradation upon storage. Microcrystalline cellulose is often used as an alternative to
carbohydrates as diluents in tablet formulations of highly potent low-dose drugs. Starch and
cellulose are used as disintegrant in tablet formulations, which swell on contact with water,
resulting in the tablet "bursting," increasing the exposed surface area of the drug and
improving the dissolution characteristics of a formulation. Polymers including polyvinyl-
pyrrolidone and hydroxypropyl methylcellulose (HPMC) also find uses as binders that aid the
formation of granules that improve the flow and compaction properties of tablet formulations
prior to tableting.
Occasionally, dosage forms must be coated with a "non functional" polymeric film
coating in order to protect a drug from degradation, mask the taste of an unpalatable drug or
excipients, or improve the visual elegance of the formulation without affecting the drug
release rate.
Capsules
Capsules are used as an alternative to tablets, for poorly compressible materials, to
mask the bitter taste of certain drugs, or sometimes to increase bioavailability. Many of the
polymeric excipients used to "bulk out" capsule fills are the same as those used in immediate-
release tablets. Gelatine has been used almost exclusively as a shell material for hard (two-
piece) and soft (one-piece) capsules. HPMC has recently been developed and accepted as an
alternative material for the manufacture of hard (two-piece) capsules.

Modified-release dosage forms

It is now generally accepted that for many therapeutic agents drug delivery using
immediate release dosage forms results in suboptimal therapy and/or systemic side effects.
Pharmaceutical scientists have attempted to overcome the limitations of conventional oral
dosage forms by developing modified release dosage forms.
Extended release dosage forms
The therapeutic effect of drugs that have a short biological half-life may be enhanced
by formulating them as extended or sustained release dosage forms. Extended and sustained
release dosage forms prolong the time that systemic drug levels are within the therapeutic
range and thus reduce the number of doses the patient must take to maintain a therapeutic
effect thereby increasing compliance. The most commonly used water-insoluble polymers for
extended-release applications are the ammonium methacrylate copolymer (Eudragit RS and
RL), cellulose derivatives ethylcellulose, cellulose acetate, and polyvinyl derivative,
polyvinyl acetate. Eudragit RS and RL differ in the proportion of quaternary ammonium
groups, rendering Eudragit RS less permeable to water, whereas ethylcellulose is available in
a number of different grades of different viscosity, with higher-viscosity grades forming
stronger and more durable films.
Gastroretentive Dosage Forms
Gastroretentive dosage forms offer an alternative strategy for achieving extended
release profile, in which the formulation will remain in the stomach for prolonged periods,
releasing the drug in situ, which will then dissolve in the liquid contents and slowly pass into
the small intestine. Unlike a conventional extended release dosage form, which gradually
releases the drug during transit along the gastrointestinal tract, such a delivery system would
overcome the problems of drugs that are absorbed preferentially from specific sites within the
gastrointestinal tract (for example, many drugs are absorbed poorly from the distal gut, where
an extended release dosage form may spend the majority of its time), producing nonuniform
plasma time profile delivery systems do not relay on polymers present, to achieve
gastroretentive mucoadhesive"and polymers have been evaluated, with little success so far,
for their ability to extend gastric residence time by bonding to the mucus lining of the
stomach and floating on top of the gastric contents respectively.
Poly (lactic-co-glycolic acid) Microspheres
The term microsphere refers to a small sphere with a porous inner matrix and variable
surface from smooth and porous to irregular and nonporous. The drug when encapsulated is
dispersed throughout the inner matrix. The size range of microspheres is typically 1 to 500
um in diameter. Poly (lactic-co-glycolic acid) microspheres have increasingly become the
focus of research efforts in the scientific community and pharmaceutical industry. Their
application as drug delivery vehicles has risen in line with the expanding biotechnology
sector and the promise of new drugs discovered in the wake of the human genome project and
proteomics.

Polymeric Nanoparticles as Drug Carriers

Certain chemical entities are either rapidly degraded and/or metabolized after
administration (peptides, proteins, and nucleic acids). This is the reason the idea that
nanotechnologies may be employed to modify or even to control the drug distribution at the
tissue, cellular, or sub cellular level has emerged. Among the technologies utilized for drug
targeting are polymer based nanoparticles, which have been developed since the early 1980s,
when progress in polymer chemistry allowed the design of biodegradable and biocompatible
materials. Nanoparticles may be defined as being submicron (<1 um) colloidal systems
generally composed of polymers. Thus, nanoparticles are colloidal systems with a size 7 to 70
times smaller than the red cells. They may be administered intravenously without any risk of
embolization. Depending on the method used in the preparation of nanoparticles, either
nanospheres or nanocapsules can be obtained. Nanospheres are matrix systems in which the
drug is dispersed within the polymer throughout the particle. On the contrary, nanocapsules
are vesicular systems, which are formed by a drug containing liquid core (aqueous or
lipophilic) surrounded by a single polymeric membrane.

Polymeric Micelles as Pharmaceutical Carriers

Polymeric micelles demonstrate many attractive properties as pharmaceutical carriers.
They are stable both in vitro and in vivo, can be loaded with a wide variety of poorly soluble
pharmaceutical agents, effectively accumulate in pathological body areas with compromised
vasculature targeted by attaching various specific ligands to their surface. Both therapeutic
and diagnostic micelles can be easily produced in substantial quantities. It appears that
micellar carriers have a promising future.
Polymeric Vesicles
Polymeric vesicles may be fabricated from a variety of macromolecular amphiphile
architectures, which include:block copolymers, random graft copolymers, and polymers
bearing hydrophobic low-molecular-weight pendant or terminal groups. These tough
particles, which reside in the nanometre and micrometer size domains, may be used for drug
targeting, the preparation of responsive release systems, and other drug delivery applications.