Formulation, Optimization, and Evaluation of Gastro-Retentive Floating Delivery Systems of Dexlansoprazole: In-Vitro and In-Vivo Characterization for Bioavailability Enhancement

Abstract

Dexlansoprazole, a proton pump inhibitor (PPI) used in the treatment of gastroesophageal reflux disease (GERD) and peptic ulcers, has limited bioavailability due to its short half-life and rapid gastric emptying. A gastro-retentive floating drug delivery system (GRFDDS) can enhance its therapeutic efficacy by prolonging gastric residence time and ensuring controlled drug release. Floating tablets of dexlansoprazole were formulated using hydrophilic polymers (HPMC K4M, HPMC K100M), gas-generating agents (sodium bicarbonate, citric acid), and other excipients. A 3² factorial design was employed to optimize formulation variables. The prepared formulations were evaluated for in-vitro buoyancy, drug release kinetics, swelling behavior, and stability. The optimized formulation was further subjected to in-vivo pharmacokinetic studies in animal models to assess bioavailability enhancement.

The optimized formulation exhibited a buoyancy lag time of <30 seconds and remained afloat for over 12 hours. In-vitro drug release studies demonstrated a sustained release profile, following non-Fickian diffusion kinetics. In-vivo pharmacokinetic analysis confirmed a significant improvement in bioavailability compared to conventional immediate-release formulations. The developed gastro-retentive floating system of dexlansoprazole successfully enhanced gastric retention, prolonged drug release, and improved bioavailability. This optimized formulation presents a promising approach for effective GERD management, reducing dosing frequency and improving patient compliance. Further clinical studies are warranted to validate its therapeutic potential.