Evaluation of polymeric systems for buccal drug delivery of Rasagiline mesylate

Abstract

The present work is planned to evaluate various polymeric systems for buccal drug delivery of Rasagiline Mesylate. Because the route avoids first pass metabolism and improve the bioavailability; in addition to its ease of administration, termination and high patient compliance; the buccal route became very important among other mucosal routes. The various forms of drug delivery systems like tablets, gels, patches and films were administered by buccal route. Because of small size, reduced thickness, flexibility and comfortness, films were selected as the formulation for the evaluation. Rasagiline Mesylate is a selective MAO type B inhibitor, indicated for the treatment of Parkinson s disease either as mono therapy or as an adjuvant to other drugs depending on the severity. The low dose of 1 mg and low oral bioavailability of 36% because of intestinal and first pass hepatic metabolism made the drug suitable for the study. In addition, hypertensive crisis, the major disadvantage of MAO inhibitors, can be overcome by buccal administration as the contact of the drug with peripheral intestinal MAO will be avoided. The patients of Parkinsonism suffer from delayed gastric emptying and swallowing disorders. These effects also can be overcome by buccal administration and thereby patience compliance can be improved. Statistical optimization method was used to evaluate the effects of combination of selected polymers on dependent parameters like mucoadhesive strength, in-vitro residence time, % swelling and % drug release.Polymers like Na CMC, HPMC, HPC, HEC, and Sodium alginate, Carbopol, PVA, Chitosan,Gelatin, PVP, Polycarbophil and Eudragit were included in the study as a combination of two or three polymers. newline