Formulation and Evaluation of Pioglitazone-Loaded Floating Microspheres for Gastroretentive Drug Delivery
Аннотация
The present study aimed to develop and evaluate pioglitazone-loaded floating microspheres as a gastroretentive drug delivery system to enhance gastric residence time and achieve sustained drug release. Floating microspheres were prepared using the solvent evaporation technique employing ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC K4M) as polymers. The prepared formulations were evaluated for particle size, surface morphology, percentage yield, drug entrapment efficiency, in vitro buoyancy, and drug release characteristics. The microspheres exhibited a particle size range of 180–350 µm with a spherical shape and porous surface morphology as confirmed by scanning electron microscopy. The percentage yield and entrapment efficiency were found to be in the range of 70–88% and 65–85%, respectively. In vitro buoyancy studies demonstrated that the optimized formulation remained buoyant for more than 12 hours with a floating percentage exceeding 90%. Drug release studies revealed a sustained release profile of pioglitazone over 12 hours, with an initial burst release followed by controlled release. Release kinetics analysis indicated that the drug release followed the Higuchi model with non-Fickian diffusion behavior. FTIR and DSC studies confirmed the absence of significant drug– polymer interactions, indicating formulation stability. The results suggest that the developed floating microspheres are a promising gastroretentive system capable of improving the bioavailability and therapeutic efficacy of pioglitazone. Further in vivo studies are recommended to establish clinical relevance.
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