Abstract

DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE MUCOADHESIVE MICROSPHERES LOADED WITH ANTI DIABETIC DRUG BY USING SUITABLE POLYMER

Vikas B. M.*, Mohammad Ali, Parthiban S.

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Abstract

Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, possesses a short half-life and low protein binding, necessitating frequent dosing. To address this limitation, this study aimed to develop and evaluate gastro-retentive mucoadhesive microspheres of Vildagliptin using the ionic gelation method. The objective was to prolong the drug’s retention time in the gastrointestinal tract, thereby maintaining steady plasma levels and enhancing bioavailability while reducing dosing frequency. Microspheres were prepared and characterized for physicochemical properties, including FT-IR, DSC, mucoadhesive wash-off, drug content, drug release, SEM, and stability studies. Results demonstrated no significant drug-polymer interaction and showed drug content ranging from 86% to 93%, with entrapment efficiency between 88% and 95%. In vitro drug release varied from 77% to 89% over 12 hours, indicating effective sustained release. These findings suggest that the prepared microspheres are a promising deliverysystem for Vildagliptin. The ionic gelation method offers a viable approach for once-daily dosing, improving therapeutic outcomes in the management of type 2 diabetes mellitus.

Keywords: Microspheres, Mucoadhesion, Control-release, Gastro-retentive, Drug targeting.