Controlled release matrix tablet formulation using synthesized N-acyl Thiolated Chitosan derivatives

Abstract

Chitosan derivative was successively synthesized by initial preparation of acyl thiourea reagent using ammonium thiocyanate and making it to react with at primary amino groups of chitosan and then reduced to yield Thiolated Chitosan. Due to the formation of disulphide bonds with mFucus glycoproteins, mucoadhesiveness is augmented. The thiol groups were then quantified using Ellman’s reagent. The derivatives inherit good swelling property in neutral and alkaline media. The different derivatives containing thiol groups were formulated into tablets using reference drug for evaluation. The Thiolated Chitosan display in situ gelling features due to the pH-dependent (alkaline pH) formation of inter-molecular disulphide bonds which makes the application of Thiolated Chitosan on intestinal mucosa and can guarantee prolonged controlled release of embedded therapeutic ingredients. Keywords: Thiolated Chitosan, Acyl isothiocyanate, Isopropanol, Mucoadhesion, Matrix tablet