Synthesis and characterization of carboxymethyl chitosan hydrogel: Application as site specific delivery for lercanidipine hydrochloride

Abstract

In the present study, carboxymethylchitosan (CMCS) was prepared from chitosan, crosslinked with glutaraldehyde and evaluated in vitro as a potential carrier for site specific drug delivery of lercanidipine hydrochloride (LERH). LERH was incorporated at the time of crosslinking of CMCS. The chitosan was evaluated for its degree of deacetylation (DD) and average molecular weight, which were found to be 84·6% and 3·5 × 10⁴ Da, respectively. The degree of substitution on prepared CMCS was found to be 0·68. All hydrogel formulations showed more than 86% and 77% yield and drug loading, respectively. The swelling behaviour of prepared hydrogels were checked in different pH values, 1·2, 6·8 and 7·4, indicated pH responsive swelling characteristic with very less swelling at pH 1·2 and quick swelling at pH 6·8 followed by linear swelling at pH 7·4 with slight increase. In vitro release profile was carried out at the same conditions as in swelling and drug release was found to be dependent on swelling of hydrogels and showed biphasic release pattern with non-fickian diffusion kinetics at higher pH. The carboxymethylation of chitosan, entrapment of drug and its interaction in prepared hydrogels were checked by FTIR, ¹H-NMR, DSC and p-XRD studies, which confirmed formation of CMCS from chitosan and absence of any significant chemical change in LERH after being entrapped in crosslinked hydrogel formulations. The surface morphology of formulation S6 was checked before and after dissolution, revealed open channel like pores formation after dissolution.