Preparation and In-Vitro Evaluation of Zolmitriptan Mucoadhesive Buccal Tablets

The buccal region of oral cavity is of particular interest with regard to systemic delivery of drug molecules that are subjected to first pass metabolic effect or those are instable in the ruthless environment of GIT. Zolmitriptan is antimigraine drug used for treatment of acute cluster headache of migraine, its known to suffer from first pass effect with variable bioavailability. The aim of the present study was to develop mucoadhesive tablet which reside on buccal cavity for specified period of time to achieve a therapeutic goal of zolmitriptan, avoiding its bioavailability problems and toxicity a raised from dose fluctuation. Buccal tablets were prepared by wet granulation method using different bioadhesive polymers namely xanthan gum (Xg), hydroxypropylmethylcellulose (HPMC) K4M, carbopol (Cb)940, chitosan and sodium alginate, where Xg used as primary polymer either alone or in combination with other polymers at ratio 3:2. Six formulations were developed and evaluated for their physicochemical proprieties like hardness, friability, thickness and drug content uniformity, along with assessing their in-vitro drug release characteristics, mucoadhesive strength, swelling index and surface pH. Formula F4 containing Xg and HPMC K4M was found to be optimum with respect to above evaluations where 88.8% of drug released at 6 hr following non fickian drug release with zero order model. Drug-exipient compatibility study was performed for such formulation by FTIR and DSC revealed that no evidence of drug-excipient interaction as well as in-vivo study show no evidence of irritation or heaviness of tablet.