Formulation and Evaluation of Chitosan-Based Buccal Bioadhesive Films of Zolmitriptan

Purpose Therapeutic efficacy of zolmitriptan in oral therapy is primarily limited by the biopharmaceutical issues. The objective of this study is to design and optimize chitosan-based buccal bioadhesive system for the effective delivery of zolmitriptan in the treatment of migraine. Methods Factorial design (3(2)) is constructed and conducted in a fully randomized manner to study all nine possible experimental runs. The films were prepared by solvent casting method by varying the content of chitosan (X-1) and polyvinyl alcohol (X-2). The effect of these two independent variables on swelling index (Y1), percent drug release in 15 min (Y2) and 5 h (Y3), and mucoadhesive strength (Y4) of prepared films was evaluated. Results The physical and chemical characteristics displayed by the prepared films (F1-F9) were found to be optimal. It was observed that the factor X-1 has positive and X-2 has negative effect on response Y1. In contrast, factor X-1 showed negative effects on drug release at both time intervals (15 min and 5 h) while X-2 displayed positive responses for these variables (Y2 and Y3). However, the mucoadhesion increased with an increase in factor X-1 and decreased when the factor X-2 was increased. Indeed, the desirable characteristics exhibited by the film F7 are ideal for buccal application. Greater flux (63.93 +/- 12.51 mu g/cm(2)/h) demonstrated in ex vivo studies substantiated the potential of optimized film to effectively deliver zolmitriptan across the buccal membrane. Conclusions This study concludes that the chitosan-based buccal film (F7) could be used in both prophylaxis and acute treatment of migraine, although need to be proved in vivo.