Trimethyl chitosan and its applications in drug delivery

摘要

Chitosan, a polymer obtained by deacetylation of chitin is widely studied for its pharmaceutical and nonpharmaceutical applications. Recommendations about uses of this polymer although could not be always realized due to limited solubility. Chitosan, for example, has been extensively evaluated for its mucoadhesive and absorption enhancement properties. The positive charge on the chitosan molecule gained by acidic environment in which it is soluble seems to be important for absorption enhancement. However chitosan is not soluble in medium except below pH 5.6. This limits its use as permeation enhancer in body compartments where pH is high. In this regard there is a need for chitosan derivatives with increased solubility, especially at neutral and basic pH values. Trimethylation of chitosan is an effort in this direction. Despite the abundance of the research related to trimethyl chitosan (TMC), the overview of the topic is not available. Hence an attempt is made in this review to cover the recent findings pertaining to synthesis, characterization and applications of TMC especially in pharmaceutical field. TMC has been synthesized by different ways and characterized by FTIR, NMR, DSC etc. This quaternized derivative of chitosan possesses a positive charge and is soluble over a wide range of pH. TMC, being a derivative of cationic polymer enriched with positive charge shows better mucoadhesive, permeation enhancement, drug delivery and DNA delivery properties. TMC can be further derivitized or grafted for modulating properties as solubility, cytotoxicity or cell recognition ability. Apart from these applications, TMCrnitself and its derivatives exhibit antimicrobial properties also. Quaternization of chitosan not only with methyl group but higher group as ethyl or along with spacer or quaternization of modified chitosan can be of interest too.