Pharmaceutical Significance of Chitosan: A Review: Home Info Zone Community Articles E-Journal Contact Help My Page
Pharmaceutical Significance of Chitosan: A Review: Home Info Zone Community Articles E-Journal Contact Help My Page
Pharmaceutical Significance of Chitosan: A Review: Home Info Zone Community Articles E-Journal Contact Help My Page
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Sanjay S. Patel
The science of drug delivery is always affected by the choice of polymers
which act as carriers. Synthetic polymers frequently suffer from the
problem
of being non-biocompatible, non-biodegradable and expensive. Natural
polymers
therefore are a promising solution to this problem.
Among the natural polymer, Chitosan is the most abundant polysaccharide,
infact second only to cellulose. Chitosan is obtained by deacetylation of
chitin. The main commercial sources of chitin are the shell wastes of shrimp,
crab, lobster, krill, and squid. Chitosan is a natural, cationic, hydrophilic,
nontoxic, biocompatible and biodegradable polysaccharide suitable for application
in pharmaceutical technology. Being a bioadhesive polymer and having antibacterial
activity. The bioadhesive nature of chitosan can be attributed to the same
type of ionic interactions with mucosal membrane components. Chitosan is soluble
at acidic pH, forming gel; hydrogels are also formed in the presence of negative
charged drugs or polyanions and represent a sustained drug release form. The
aim of this review is to provide an insight into the many potential applications
of chitosan as a pharmaceutical excipient. Various investigations carried
out recently are reported, although references to research performed on chitosan
prior to the recent reviews have also been included where appropriate.
Introduction
There is growing interest in
developing chemical and biochemical processes to obtain and modify biopolymers,
and to other useful technical properties for their applications in different
fields.1-3 One of the latest and most interesting example is chitin,
it is mainly used for production of chitosan by a deacetylation reaction
usually obtained in alkaline medium. Chitosan exhibits several favorable properties,
such as biodegradability and biocompatibility.4 It also has
mucoadhesive properties due to its positive charges at neutral pH that enable
an ionic interaction with the negative charges of sialic acid residues of the
mucus.5,6 Some of which include binding, disintegrating, and tablet
coating properties. Numerous studies have demonstrated that chitosan and
its derivatives (N-trimethyl chitosan, mono-N-carboxymethyl chitosan) are
effective and safe absorption enhancers to improve mucosal (nasal, peroral)
delivery of hydrophilic macromolecules, such as peptides, proteins, and
heparins. Chitosan
has been developed for a variety of biomedical applications including wound
dressings and drug delivery systems. In the context of drug delivery, chitosan
has been used as a stabilizing constituent of liposomes7 as an
excipient controlling drug release in oral formulations.8 The polymer has
also been investigated as a potential adjuvant for swellable controlled drug
delivery systems. Chitosan exhibits a myriad of biological actions, namely
hypocholesterolemic, antimicrobial, and wound-healing properties. Low toxicity
coupled with wide applicability makes it a promising candidate not only for the
purpose of drug delivery for a host of drug moieties (anti-inflammatory,
peptides, etc) but also as a biologically active agent. Chitosan nano-and
micro-particles are also suitable for controlled drug release. Association of
vaccines to some of these particulate systems has shown to enhance the antigen
uptake by mucosal lymphoid tissues, thereby inducing strong systemic and
mucosal immune responses against the antigens.
Chemical Structure and Preparation of Chitosan
Chitin
and chitosan are one of the most abundant polysaccharide in nature, after
cellulose. Chitin is long and unbranched homopolymer,9 it form a
major part of cell wall of crustaceans (shrimp, crab, lobster, krill,
and squid), insects, fungi, annelids, molluscus and coelentrates. Structurally, it is poly
(N-acetyl-2-amino-2-deoxy-D-glycopyranose) in which the N-acetyl-2-amino-2-deoxy-
D-glycopyranose
units are linked by (1-4) β bonds.
Its β (1-4) linked glucose-NAC
units with a three dimensional α-helical configuration are stabilized by
hydrogen bonding.10 Chitin is highly hydrophobic material, insoluble
in eater as well as most organic solvents but its aqueous solubility can be
increased by deacetylation.11 The principal derivative of chitin,
namely chitosan [(1-4) 2-amino-2-deoxy-β-D-glucan] is a unique
polysaccharide and hydrophilic polymer, which is usually obtained by alkaline
deacetylation, the two polymers being distinguished by solubility in dilute
aqueous acid solutions.11,12 Commercial chitin and chitosan consists of both
types of monomers. Chitosan is found in nature, to a lesser extent than
chitin, in the cell walls of fungi. The
annual biosynthesis of chitin has been estimated to 109 to 1011 tons. Chitin is widely
distributed in
nature. Among several sources, the exoskeleton of crustaceans consists of 15%
to 20 % chitin of dry weight. Chitin found in nature is a renewable
bioresource. 13-16 Chitin and chitosan are both prepared
using the common process illustrated and described in Figure 1. The chemical
and biological properties of chitosan17 are listed in Table 1. The
pharmaceutical requirement for chitosan include appearance, particle size,
density, viscosity, loss on drying and heavy metal content are listed in Table
2.
Figure: - 1. Preparation of Chitin and Chitosan
Shellfish wastes from food processing (shrimp, crab, squid,
lobster,)
Chitin
Chitosan
Natavarlal M. Patel
Principal in Shri B. M. Shah College of Pharmaceutical Education and Research,
Modasa, Gujarat, India
Girish N. Patel
Lecturer in pharmaceutical technology department, S. K. Patel College of
Pharmaceutical Education and Research,
Ganpat University, Kherva, Gujarat
Kanu R. Patel
Lecturer in pharmaceutical technology department, Shri B. M. Shah College
of Pharmaceutical Education and Research,
Modasa-383315, Gujarat
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