DESIGN AND OPTIMIZATION OF RASAGILINE MESYLATE TRANSDERMAL PATCHES BY USING CENTRAL COMPOSITE DESIGN, CHARACTERIZATION OF PHYSICO-CHEMICAL, IN-VITRO AND EX-VIVO STUDIES

Objective: Rasagiline mesylate (RM) is an effective BCS class III act as a potent, irreversible monoamine oxidase- B (MAO-B) inhibitor, mainly used to treat Parkinson’s disease. It has low permeability and low oral bioavailability (35%). To overcome these disadvantages and to maintain constant plasma concentration for maximum therapeutic activity, there is a need to design an alternative route i.e. transdermal route. The pharmacokinetic parameters make RM a suitable candidate for transdermal delivery. Present investigation consists of the study of in-vitro and ex-vivo skin flux of Rasagiline mesylate (RM) from transdermal patches. Methods: The patches were fabricated by solvent casting method using hydrophilic and hydrophobic polymer with different composition. Tween 80 incorporated as solubilizer, PEG 600 as plasticizer, Menthol, Lemongrass oil used as permeation enhancers respectively. The prepared TDDS were extensively evaluated for in-vitro release, ex-vivo permeation through pig ear skin, moisture content, moisture absorption, water vapour transmission, mechanical properties. The physicochemical interaction between RM and polymers were investigated by Fourier transform infrared spectroscopy (FTIR). Results: All the formulations exhibited satisfactory physicochemical and mechanical characteristics. A flux of 31.1µg/cm² h and 26.9 µg/cm² h was achieved for optimized formulations containing lemongrass oil and menthol respectively permeation enhancers. Values of tensile strength (0.099±0.030kg/mm²), elongation at break (0.9864±0.115%mm²) revealed that formulation F18 was strong but not brittle. Drug and excipients compatibility studies showed no evidence of interaction between the active ingredient and polymers. Conclusion: Rasagiline mesylate transdermal patches could be prepared with required flux and suitable mechanical properties.