Mucoadhesive Microparticulate Drug Delivery System of Esomeprazole Against Helicobacter Pylori Infection: Design, Development and Optimization

Abstract

The purpose of the present research was to develop and characterize mucoadhesive microspheres of esomeprazole for the potential use of treating gastric adenocarcinoma, gastric and duodenal ulcer associated with Helicobacter pylori. Esomeprazole mucoadhesive microspheres were prepared using HPMC, Chitosan and Acrycoat S 100 as a by an emulsion‑solvent evaporation technique. The factorial designing methodology was used for optimization of formulation for two factors at three levels each was employed to study the effect of independent variables, polymer1: polymer2: emulsifier ratio (chitosan: acrycoatS100) (X1) and surfactant concentration: tween80 (X2) on dependent variables, namely particle size, drug entrapment efficiency, percentage mucoadhesion and in vitro drug release. Optimized formulation was obtained using desirability approach of numerical optimization. The drug release was also found to be slow and extended more than 8 h and release rates were fitted to the Power law equation and Higuchi model to compute the diffusional parameters. The prolonged stomach residence time of esomeprazole mucoadhesive microspheres might make a contribution to H. pylori complete eradication in combination with other antimicrobial agents.