Abstract

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

Waleed M. Khattab*, Shadeed Gad , Mohamed M. El-sayed and Mamdouh M.Ghorab

¹Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Industries,Sinai University, Al-Arish, North Sinai, Egypt.

²Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez CanalUniversity, Ismailia, Egypt.

ABSTRACT

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 37.670.65% 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 32.72.1 g. Drug release was 86.933.73 % after 7 h following zero order kinetics and permeation flux was 0.045 mg/cm2 h. Tablets were physically stable in normal human saliva for 6 h. These formulations are very promising ones to control the drug delivery of such drugs which in turn will improve their bioavailability and therapeutic response.

Keywords: Buccal, Mucoadhesive, Carbopol 934LR, Chitosan, Xanthan gum.