Professional Documents
Culture Documents
Saripilli Rajeswari1*, Teella Prasanthi1, Navya Sudha1, Ranjit Prasad Swain1, Satyajit
Panda2 and Vinusha Goka
1
Department of Pharmaceutical Technology, Maharajah’s College of Pharmacy, Phool
Baugh, Vizianagaram.
2
Department of Pharmaceutics, Institute of Pharmacy and technology, Salepur, Cuttack,
Odisha.
INTRODUCTION[1,2]
A polymer is a large molecule (macromolecules) composed of repeating structural units.
These subunits are typically connected by covalent chemical bonds. Polymers are generally
Natural polymers These polymers are found in nature generally from plants and animals
sources. Such as proteins, cellulose, starch, resins, etc.
Semi-synthetic polymers These polymers are obtained from natural polymers by simple
chemical treatment to change the physical properties of natural polymers like starch,
silicones, etc.
Economic
Natural polymers are cheaper and their production cost is less than synthetic material.
Easy availability
Natural polymers are growing in the form of herbs in many counties being economical than
synthetic polymers and having no side effect and keeping in view their huge application in
many industries, they are produced in large quantity hence their availability is ensured than
synthetic polymers.
Applications
Microcrystalline cellulose is mainly used in the pharmaceutical industry as a diluent/binder in
tablets for both the granulation and direct compression processes. Carboxylated methyl
cellulose is used in drug formulations, as binder for drugs, film-coating agent for drugs,
ointment base etc. Cellulose acetate fibers are used in Wound dressings.
AGAR
Source
Agar or agar-agar consists of dried gelatinous substance obtained from Gelidium amansi
(Gelidaceae) and it is also obtained from several other species of red algae like, gracilaria
(Gracilariaceae) and Pterocladia (Gelidaceae).
Composition
Agar consists of a mixture of agarose and agaropectin. The agarose is a linear polymer which
is made up of the repeating monomeric unit of agarobiose. Whereas, Agarobiose is a
disaccharide made up of D-galactose and 3, 6 - anhydro-L-galactopyranose. Agaropectin is a
heterogeneous mixture of smaller acidic molecules.
Applicatons
Agar is used as Suspending agent, emulsifying agent, gelling agent in suppositories, surgical
lubricant, tablet disintegrants, medium for bacterial culture, laxative. It is also used for the
preparation of jellies, confectionary items, tissue culture studies, and in microbiology study.
STARCHES
Source
Starch is the principal carbohydrate reserved material in green plants and it is mainly present
in seeds and underground organs. Starch occurs in the form of granules (starch grains). A
number of starches are recognized for pharmaceutical use and these include maize (Zea
mays), rice (Oryza sativa), wheat (Triticum aestivum), and potato (Solanum tuberosum).
Composition
Starch or amylum is a carbohydrate consisting of a large number of glucose units joined
together by glycosidic bonds. It consists of two polymers, namely amylose (a non-branching
helical polymer consisting of α-1, 4 linked D-glucose monomers) and amylopectin (a highly
branched polymer consisting of both α-1,4 and α-1,6 linked D-glucose monomers).
Applications
Thermoplastic starch is used in packaging, containers, mulch films, textile sizing agents,
adhesives.
INULIN
Applications
Inulin with a high degree of polymerization was used to prepare biodegradable colon-specific
films in combination with Eudragit® RS that could withstand break down by the gastric and
intestinal fluids.
GUAR GUM
Source
Guar gum is also called guaran, clusterbean, Calcutta lucern, Gum cyamposis, and
Cyamopsis gum, Guarina, Glucotard and Guyarem. Guar gum is the powder of the
endosperm of the seeds of Cyamopsis tetragonolobus Linn. (Leguminosae).
Composition
Chemically, guar gum is natural polysaccharide composed of the sugars galactose and
mannose. It is a galactomannans which is a linear polysaccharide consisting of (1→4)-
diequatorially linked β-D- mannose monomers, some of which are linked to single sugar
sidechains of α-D-galactose attached. Guar gum has a backbone composed of β-1, 4 linked-
D-mannopyranoses to which, on average, every alternate mannose an α-D galactose is linked
1→6.
Applications
Several modifications of guar gum is used for drug delivery system.
Carboxymethyl guar film is used for the formulation of transdermal therapeutic system.
Guar gum is particularly useful for colon delivery because it can be degraded by specific
enzymes in this region of the gastrointestinal tract. The gum protects the drug while in the
stomach and small intestine environment and delivers the drug to the colon where it
undergoes assimilation by specific microorganisms or degraded by the enzymes excreted
by these microorganisms.
Source
Chitin is the polysaccharide derivative containing amino and acetyl groups and are the most
abundant organic constituent in the skeletal material of the invertebrates. It is mainly found in
mollusks, annelids, arthropods. It is also a constituent of the mycelia and spores of many
fungi.
Applications
Chitosan and their derivatives (N-trimethyl chitosan, mono-N-carboxymethyl chitosan)
are safe and effective absorption enhancers to improve mucosal, nasal, peroral drug
delivery of hydrophilic macromolecules such as peptide and protein drugs and heparins.
Chitosan nanoparticles and microparticles are also suitable for controlled drug release.
XANTHAN GUM
Source
Xanthan gum is a high molecular weight extracellular polysaccharide produced by the
fermentation of the gram-negative bacterium Xanthomonas campestris.
Composition
The primary structure of naturally produced cellulose derivative contains a cellulose
backbone ( -D-glucose residues) and a trisaccharide side chain of D-mannose - D gluronic
acid -D-mannose attached with the main chain of alternate glucose residues.
Applications
Xanthan gum is widely used in oral and topical formulations, cosmetics, and in food
industry as a suspending and stabilizing agent.
It has also been used to prepare sustained release matrix tablets.
ALGINATE
Composition
It is composed of 1–4 linked -L-glucuronic and –D - mannuronic acid residues.
Applications
Alginate based mesalazine tablets are used for intestinal drug delivery system.
Alginate is also as encapsulation materials for controlled drug delivery to mucosal tissue.
It is also used to prepare mucoadhesive drug delivery systems.
PSYLLIUM
Source
Psyllium mucilage is obtained from the seed coat of Plantago ovata by milling the outer layer
of the seeds.
Applications
It has tablet binding properties.
Psyllium husk was used in combination with other excipients such as hydroxypropyl
methylcellulose to prepare a novel sustained release, swellable and bioadhesive gastro
retentive drug delivery systems for ofloxacin.
PROTEINS FROM ANIMAL SOURCES(9,10)
COLLAGEN
Source
Collagen is the primary protein component of animal connective tissues. The most abundant
sources of collagen are pig skin, bovine hide and pork and cattle bones.
Composition
There are 27 types of collagen exist and composed of different polypeptides, which contain
mostly glycine, proline, hydroxyproline and lysine. The flexibility of the collagen chain
depends only on the glycine content.
Applications
Collagen films are used in ophthalmology as drug delivery systems for slow release of
incorporated drugs.
It was also used for tissue engineering including skin replacement, bone substitutes, and
artificial blood vessels and valves.
GELATIN
Applications
These widely include emulsifiers, foaming agents, colloid stabilizers, biodegradable film-
forming materials, and microencapsulating agents.
Composition
Wheat gluten contains of two main groups of proteins, gliadin and glutenin. Gliadins are
proteins molecules with disulphide bonds and have low molecular weight and a low level of
amino acids with charged side groups. Glutenins are more sophisticated proteins, with a three
dimensional structure. Their molecular weight is at least ten times higher than that of
gliadins.
Advantages
Wheat gluten materials have the fastest degradation rates.
Gluten is fully biodegradable and the products obtained are non-toxic.
It is readily available in high quantity and at low cost.
Applications
Wheat gluten has been proven to be an excellent film forming agent.
SOY PROTEIN
Source
According to the production method different categories of soy proteins exist: soy protein
isolate, soy protein concentrate and textured soy protein.
Composition
Soy protein isolate is the most refined form of soy protein and contains about 90 percent
protein. Soy protein concentrate is basically soybean without the water soluble carbohydrates.
It contains about 70 percent of protein.
Application
It has been used since 1959 as an ingredient in a variety of foods for its functional properties,
which include emulsification and texturizing. Recently the popularity of soy protein has been
increasing, mainly because of its health benefits. It has been proven that soy protein can help
to prevent heart problems.
Diffusion
Diffusion occurs when a drug or other active agent passes through the polymer that forms the
controlled‐release device. Diffusion occurs when the drug passes from the polymer matrix
into the external environment. As the release continues its rate normally decreases with this
type of system since the active agent has a progressively longer distance to travel and
therefore requires a longer diffusion time to release. In these systems, the combinations of
polymer matrices and bioactive agents choosen must allow for the drug to diffuse through the
pores or macromolecular structure of the polymer upon introduction of the delivery system
into the biological environment without inducing any change in the polymer itself.
Degradation
Biodegradable polymer degrades within the body as a result of natural biological processes,
eliminating the need to remove a drug delivery system after release of the active agent has
been completed. Most biodegradable polymers are designed to degrade as a result of
hydrolysis of the polymer chains into biologically acceptable and progressively smaller
compounds. For some degradable polymers, most notably the polyanhydrides and
polyorthoesters, the degradation occurs only at the surface of the polymer, resulting in a
release rate that is proportional to the surface area of the drug delivery system.
Swelling
They are initially dry, when placed in the body will absorb water or other body fluids and
swell. The swelling increases the aqueous 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.
Capsules: Many of the polymeric excipients used to bulk out capsule fills are the same as
those used in immediate release tablets. Gelatin 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 FORM
To achieve gastro retention, mucoadhesive and low‐density 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.
Zein
Zein an alcohol‐soluble protein contained in the endosperm tissue of Zeamais, occurs as a by‐
product of corn processing. Zein has been employed as an edible coating for foods and
pharmaceuticals for decades. Zein is an inexpensive and most effective substitute for the fast
disintegrating synthetic and semi synthetic film coatings currently used for the formulation of
substrates that allow extrusion coating.
Collagen
Collagen is the most widely found protein in mammals and is the major provider of strength
to tissue. It not only has been explored for use in various types of surgery, cosmetics and drug
delivery, but in bio prosthetic implants and tissue engineering of multiple organs.
Starches
It is the principal form of carbohydrate reserve in green plants and especially present in seeds
and underground organs. Starch occurs in the form of granules (starch grains), the shape and
size of which are characteristic of the species, as is also the ratio of the content of the
principal constituents, amylose and amylopectin. A number of starches are recognized for
pharmaceutical use. These include maize (Zea mays), rice (Oryza sativa), wheat (Triticum
aestivum), and potato (olanum tuberosum). To deliver proteins or peptidic drugs orally,
microcapsules containing a protein and a proteinase inhibitor were prepared. Starch/bovine
serum albumin mixed‐walled microcapsules were prepared using interfacial cross‐linking
with terephthaloyl chloride. The microcapsules were loaded with native or aminoprotected
aprotinin by incorporating protease inhibitors in the aqueous phase during the cross‐linking
process. The protective effect of microcapsules with aprotinin for bovine serum albumin was
revealed in vitro.
Polycaprolactone
Polycaprolactone (PCL) is biodegradable polyester with a low melting point of around 60°C
and a glass transition temperature of about −60°C. PCL is prepared by ring opening
polymerization of ε‐caprolactone using a catalyst such as stannous octanoate. The most
common use of polycaprolactone is in the manufacture of speciality polyurethanes.
Polycaprolactones impart good water, oil, solvent and chlorine resistance to the polyurethane
produced.
Polyorthoesters
These materials have gone through several generations of synthetic improvements to yield
materials that can be polymerized at room temperature without production of condensation
by‐products. These materials are hydrophobic with hydrolytic linkages that are acid sensitive,
but stable to base. They degrade by surface erosion and degradation rates may be controlled
by incorporation of acidic or basic excipients.
Topical delivery: Carrageenans are a family of sulfated polysaccharides extracted from red
marine algae and that are widely utilized in the industry because they can form reasonably
stiff and thermo reversible gels.
Ocular delivery: Chitosan along with an excellent film capability make chitosan suitable for
development of ocular bandage lenses.
Mucosal delivery: Natural polymer gets protonated in acidic solution, so it binds strongly to
negatively charged cell surface making it useful to formulate bioadhesive dosage forms.
Gene Delivery: Natural polymer typically isolated from the shell of shrimp, has the ability to
react with DNA and compact it to produce a nanoparticle. Such nanoparticles are more
readily taken up by cells.
POLYMERS IN PHARMACEUTICAL APPLICATION[3,19]
Water‐Soluble Synthetic Polymers
Poly (acrylic acid) Cosmetic, pharmaceuticals, immobilization of cationic drugs, base for
Carbopol polymers.
Poly (ethylene oxide) Coagulant, flocculent, very high molecular‐weight up to a few
millions, swelling agent.
Poly (ethylene glycol) Mw <10,000; liquid (Mw <1000) and wax (Mw >1000),
plasticizer, base for suppositories.
Poly (vinyl pyrrolidone) used to make betadine (iodine complex of PVP) with less
toxicity than iodine, plasma replacement, tablet granulation.
Poly (vinyl alcohol) water‐soluble packaging, tablet.
Cellulose‐Based Polymers
Ethyl cellulose insoluble but dispersible in water, aqueous coating system for sustained
release applications.
Carboxymethyl cellulose is Super disintegrant, emulsion stabilizer.
Hydroxyethyl and hydroxypropyl celluloses is Soluble in water and in alcohol for tablet
coating.
Hydroxypropyl methyl cellulose is a Binder for tablet matrix and tablet coating, gelatin
alternative as capsule material.
Cellulose acetate phthalate enteric coating.
Hydrocolloids
Alginic acid - oral and topical pharmaceutical products; thickening and suspending agent
in a variety of pastes, creams, and gels, as well as a stabilizing agent for oil‐in‐water
emulsions; binder and disintegrants.
Carrageenan - Modified release, viscosifier.
Chitosan - Cosmetics and controlled drug delivery applications, mucoadhesive dosage
forms, rapid release dosage forms.
CONCLUSION
Natural biodegradable polymers have received much more attention in the last decades due to
their applications in the fields related to environmental protection and the maintenance of
physical health. From the discussion, it can be concluded that by incorporating drugs in
natural polymers, dosage forms that release the drug over a prolong length of time can be
prepared in variety of shapes and sizes. Polymers play a vital role in the drug delivery so; the
selection of polymer plays an important role in drug manufacturing. But while selecting
polymers care has to be taken regarding its toxicity, drug compatibility and degradation
pattern. By this review, we can say that natural polymers can be good substitute for the
synthetic polymers and many of the side effects of the synthetic polymers can be overcome
by using natural polymers.
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