BUCCO-ADHESIVE DELIVERY SYSTEM FOR AN ANTI-MIGRAINE DRUG: IN-VITRO/EX-VIVO EVALUATION

Mucoadhesion was employed for improving performance and bioavailability of many drugs. Different dosage forms were developed based on this principle. This study aims to prepare bucco-adhesive tablets of anti-migraine drug zolmitriptan as a suitable candidate for improving its oral bioavailability and therapeutic efficacy and to evaluate them for many pre/post-formulation parameters in-vitro/exvivo. The bucco-adhesive tablets containing 2.5 mg zolmitriptan were prepared using carbopol 934LR as a primary polymer alone or in combination with chitosan or xanthan gum as secondary polymers by direct compression. Drug-excipients compatibility and micromeritics study were carried out. Tablets were evaluated for physico-chemical parameters, surface pH, ex-vivo residence time, in-vitro swelling study, ex-vivo mucoadhesive strength, in-vitro drug release study, ex-vivo permeation study and physical stability in human saliva. No interactions were found between drug and excipients. Tablets had good physico-chemical characters. Formulation containing carbopol 934LR and chitosan in a ratio of 1: 3 approximately was the optimum one. It swelled by only 37.67±0.65% after 5 h and showed a nearly neutral surface pH. Ex-vivo residence time was long enough for delivery of the drug for more than 8 h. Ex-vivo mucoadhesive strength was 32.7±2.1 g. Drug release was 86.93±3.73 % after 7 h following zero order kinetics and permeation flux was 0.045 mg/cm 2 h. Tablets were physically stable