Formulation and Evaluation of Oral Mucoadhesive Tablets of Cisplatin (Only Abstract)

Abstract

Background and Aim: Cisplatin, an anticancer drug is used to treat various types of cancer. It is available only in the form of injection to be administered as an i.v. infusion. For that, it needs to be administered under the supervision of an oncologist. The inconvenience and cost of hospitalization can be avoided by the development of oral formulation of cisplatin.Thereisnomarketedtabletformulationof Cisplatin availabletilldate.In the present study, an attempt was made to develop oral enteric coated, sustained release, mucoadhesive tablets of cisplatin in order to prevent upper GIT side effects like nausea and vomiting and to prolong its residence time in intestine. Methods: Eight formulations were developed by direct compression method using various proportions of mucoadhesive polymers, HPMC (400 cps) and carbopol 940. Prepared tablets were evaluated for physical parameters, swelling index, surface pH, mucoadhesive strength and in vitro drug release. Results: Among all the formulations, F4C was found to be the best as it showed high swelling index 125.51± 1.63 % at 12 h, optimum mucoadhesive strength of 13.11±0.65 g and superior in vitro drug release of 91.30% in 12 h respectively. Optimized F4C batch was further subjected to ex-vivo permeation study by everted gut sac technique and permeability co-efficient was found to be 0.0013 at 12 h. The prepared mucoadhesive sustained release tablets of optimized batch (F4C) were further enteric coated with Eudragit L 100 suspension up to 20 %. The final formulations were studied forin vitrodrugrelease in0.1N HCl for 2 h followed by that in0.2M phosphate buffer pH 6.8 up to 16 h. Data showed no drug release in first 2 h in 0.1N HCl. However, sustained drug release of cisplatin could be observed in 0.2M phosphate buffer pH. A maximum of 82.52% drug release was observed at the end of 12 h. Conclusion: It was concluded that 20% Eudragit coated sustained release mucoadhesive tablets of cisplatin (F4C) containing 100 mg of carbopol has shown desired in vitro drug release as well as mucoadhesive strength and could be further explored for its in vivo performance.