EVALUATION OF CELLULOSE POLYMERS FOR BUCCAL FILM FORMULATION OF RASAGILINE

Abstract

Objective: Rasagiline Mesylate is used to treat the signs and symptoms of Parkinsonism. It has an oral bioavailability of 36% due to first pass hepatic and intestinal metabolism. To improve the bioavailability; a buccal films formulation was planned.

Methods:Compatibility of the drug with the excipients was studied with the help of FTIR and DSC. 2³ factorial design was planned using concentration of polyox, concentration of film former as numerical variables and type of film former as a categorical variable. Solvent casting method was used for the fabrication of films. Weight, thickness, surface pH, mucoadhesive strength, in vitro residence time, % swelling and % drug release were evaluated for the prepared film formulations.

 Results:All the films were found havesurface pH close to neutral pHand  werefound to have content uniformity. Mucoadhesive strength was found to increase with increase in concentration of polyox. Three polymers polyox, sodium CMC and HPMC were showing positive effect on swelling. Comparatively polyox has less influence than either of the cellulose polymers on swelling.Drug release is more controlled by the high swelling film formers than polyox. Among the film formers, though swelling is more, % drug release is also more from Na CMC films because of its ionic nature and more solubility.

Conclusion: Because of high mucoadhesive strength and more % drug release, combination of Polyox with  Na CMC film formulations were selected over HPMCfilm formulation  to improve the bioavailability of Rasagiline. 

Key words: Rasagiline, buccal film, Sodium carboxy methyl cellulose, factorial design