Recent Advances in Drugs and Prodrugs Design of Chitosan

Abstract

The aim of this review is to outline the recent advances in chitosan molecular modeling, especially its usage as a prodrug or drug in a field of antibacterial, anticarcinogenic and antioxidant activity. Polymeric materials like peptides, polysaccharides and other natural products have recently attracted attention as biodegradabile drug carriers. They can optimize clinical drug application, minimize the undesirable drug properties and improve drug efficiency. They are used for the slow release of effective components as depot forms, to improve membrane permeability, solubility and site-specific targeting. Chitosan is such a prospective cationic polysaccharide which has shown number of functions in many fields, including bio medicinal, pharmaceutical, preservative, microbial and others. This article discusses the structure characteristics of chitosan, a number of factors such as degree of polymerization, level of deacetylation, types of quarternisation, installation of various hydrophilic substituents, metal complexation, and combination with other active agents. Biodegradable, non-toxic and non-allergenic nature of chitosan encourages its potential use as a carrier for drug delivery systems in all above mentioned targets. The use of chitosan prodrug conjugates is aimed at the site-specific transport to the target cells use, for example, a spacer tetrapeptide Gly-Phe-Leu-Gly, promotion of drug incorporation into cells via endocytosis, hybridization or synergism of two types of drugs or a drug with a bioactive carrier. The design of chitosan macromolecule prodrugs is also discussed.

Transformation of Thionin Genes Using Chitosan Nanoparticle into Potato Plant to Be Resistant to Fungal Infection

“…Chitosan (CS) is the only naturally existing cationic biodegradable alkaline polysaccharide and binds strongly to negatively charged DNA. Also [21] enumerated the properties of CS as it is a nontoxic, semicrystalline, biodegradable, biocompatible linear polysaccharide, chemical inertness, wound healing ability and low cost. It is a linear polysaccharide composed of randomly distributed β-(1-4)-linked D-glucosamine (deacetylated unit) and N-acetyl-D-glucosamine (acetylated unit).…”

Charged hydrophilic polymer brushes and their relevance for understanding marine biofouling

“…Inherent antimicrobial activities of cationic polymers have been utilized for contact-active coatings (Ferreira & Zumbuehl 2009). Chitosan, a cationic polysaccharide, has antimicrobial activity against both Gram-positive and Gram-negative bacteria (Li et al 2011, Vinsova & Vavrikova 2008. Other cationic polymers containing derivatives of quaternary ammonium amine (Lee et al 2004) and imine (Yudovin-Farber et al 2010), or poly(vinyl-N-hexylpyridinium) (Tiller et al 2001) have also shown antibacterial activity in solution.…”

Effects of Spray Drying on Physicochemical Properties of Chitosan Acid Salts

“…Chitosan forms water-soluble salts with both inorganic acids and organic acids such as hydrochloric acid, formic acid, glutamic acid, lactic acid, citric acid, acetic acid, and ascorbic acid (5)(6)(7). The reactive amino groups present in chitosan chains can be protonated (NH 3 + OCOR − ) by the abovementioned acids, and the resultant water-soluble polysaccharide is positively charged (5).…”