Formulation and Evaluation of Mucoadhesive Microspheres Loaded with Antiulcer Drug

Abstract

The present study aimed to develop and evaluate gastro-retentive mucoadhesive microspheres of esomeprazole for the effective management of Helicobacter pylori -associated gastric ulcer. Gastro-retentive drug delivery systems (GRDDS) are designed to prolong the residence time of dosage forms in the stomach, thereby enhancing local drug availability, improving therapeutic efficacy, and minimizing dosing frequency. Mucoadhesive microspheres of esomeprazole were prepared using an emulsification cross-linking technique with hydroxypropyl methylcellulose (HPMC), chitosan, and Acrycoat S100 at different polymer ratios. The prepared formulations were characterized for drug-excipient compatibility, percentage yield, micromeritic properties, particle size, drug content, entrapment efficiency, drug loading, swelling index, in vitro drug release, and release kinetics. Fourier-transform infrared (FTIR) spectroscopy confirmed the absence of significant drug-polymer interactions, indicating good compatibility between esomeprazole and the selected excipients. Among all the formulations, formulation EM8 containing HPMC and Acrycoat S100 exhibited the most desirable sustained drug release profile, extending up to 12 h with controlled release characteristics. The optimized formulation demonstrated excellent mucoadhesive properties and prolonged drug release, suggesting its potential as a promising gastro-retentive delivery system for the sustained treatment of H. pylori -associated gastric disorders.