DESIGN AND EVALUATION OF AMISULPRIDE LOADED CHITOSAN MICROPARTICLES

Abstract

Amisulpride is an atypical antipsychotic drug with dopamine (D2 /D3) receptor blocker
activity. The oral bioavailability of amisulpride was below 48% due to first pass metabolism and
poor aqueous solubility. Amisulpride is a BCS Class II drug .The objective of this study is to
develop controlled release formulation with lower dose of drug to uphold plasma concentration that
may upturn patients compliance, enhanced therapeutic efficacy, Better Bioavailability and abridged
side effects because of alteration in delivery pattern via slow release of drug from microparticles.
The present research work was aimed at development and optimization of Amisulpride loaded
microparticles with Chitosan natural polymer by using emulsification crosslinking and Ionotropic
Gelation techniques. Total 8 formulations were designed, among those F1 to F4 are prepared by
emulsification crosslinking method with chitosan as natural polymer for controlled release and
different concentrations of TPP (As crosslinking agent), and F5 to F8 formulations are prepared by
Ionotropic Gelation technique with same composition. All the formulations are subjected to their
characterization like size analysis, flow properties, % Drug Content, % Encapsulation Efficiency,
Wall thickness, SEM Analysis, IR Sprectroscopy and evaluation for invitro drug release studies.
From this study it was found that the microparticles formulated with Ionotropic gelation method
and Emulsification Crosslinking method techniques showed significant differences in their release
rate and permeability coefficient values. Emulsification Crosslinking method was found to be
more suitable for sustained release as it yielded slow release of the Amisulpride and offered
Improved Bioavailability.