Formulating And Optimizing Gastroretentive Floating Dexlansoprazole for Enhanced Bioavailability In Vitro And In Vivo
Abstract
Background: Gastroesophageal reflux disease (GERD) is commonly treated with the proton pump inhibitor dexlansoprazole (DLS). Its limited absorption window in the upper gastrointestinal (GI) tract, pH-dependent solubility, and brief plasma half-life, however, restrict its bioavailability and therapeutic effectiveness. Gastroretentive floating drug delivery systems (GRDDS) present a viable approach to overcoming these constraints by improving systemic absorption and extending the stomach residence duration.
objective : The objective of this study was to improve the bioavailability and therapeutic profile of Dexlansoprazole by developing, optimizing, and evaluating different GRDDS formulations using a factorial approach, with an emphasis on in-vitro and in-vivo parameters.
Methods: Gas-generating agents, swelling polymers, and mucoadhesive components were used to create three different GRDDS formulations: floating microspheres, bilayer tablets, and matrix tablets. Formulation variables were optimized using response surface approach and factororial design. Under simulated stomach circumstances (pH 1.2), physical-chemical characteristics, buoyancy, mucoadhesion, and in-vitro drug release were evaluated. To compare the bioavailability of improved formulations with the commercially available Dexilant®, in-vivo pharmacokinetic experiments were carried out in albino rabbits.
Results: Over a 12-hour period, the optimized floating microspheres (F17) demonstrated regulated drug release,…
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