Abstract
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.