Buccal Systems to Enhance Buspirone Hydrochloride Bioavailability: Formulation and In-vitro / In-vivo Evaluation

Buccal delivery systems involves the administration of the drug through the buccal mucosal membrane lining of the oral cavity bypassing the first pass effect. Buspirone hydrochloride is an anxiolytic drug which undergoes extensive first-pass metabolism that results in very low oral bioavailability (4%). In addition, buspirone hydrochloride has short and variable elimination half–life (approximately 2.4 h). So it is a good candidate for the preparation of sustained release buccal dosage forms. The aim of this work was to formulate and evaluate buspirone hydrochloride buccal mucoadhesive cup and core tablets and sponges to sustain its action and improve its systemic bioavailability. The results of the in-vivo performance study confirmed that the prepared cup and core buccal tablets succeeded in increasing the bioavailability of buspirone 5.6 folds in comparison to the oral immediate release market product.