Preparation and in vitro evaluation of sublingual film of selegilline hydrocholoride

Abstract

Background: Selegiline Hydrochloride is a selective irreversible MAO-B inhibitor which is used in the treatment of early-stage Parkinson's disease, depression and dementia. It shows low bioavailability due to high hepatic first pass metabolism. Objective: The present work was undertaken to formulate mucoadhesive sublingual films of selegiline with the objective of improving the therapeutic efficacy, patient compliance and bioavailability. Methods: The sublingual films were formulated by solvent casting technique using various polymers as hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), sodium carboxymethyl cellulose and Maltodextrin. Glycerol (plasticizer), sodium saccharin (sweetener), mannitol (to sweetener and increase drug dissolution rate by forming pores on the surface of drug forms) and citric acid (to adjust the pH according to the mouth and as permeability enhancer) were used. This study was also designed to evaluate the physicochemical and mucoadhesive characteristics of the films. The films were evaluated for their weight, thickness, folding endurance, drug content efficiency, disintegration time, release, bioadhesion and mucoadhesion. Results: They showed good appearance and elasticity. The best drug to polymer ratio was F2 (1:4 drug to PVA polymer ratio). The film of F2 showed 0.6 mg weight, 0.1 mm thickness, >200 folding endurance, 100% drug content, respectively. The Differential Scanning Calorimetry (DSC) showed stable character of selegiline in the drug loaded films and revealed amorphous. The results showed that the films prepared were fast dissolving. The film of F2 exhibited very good mucoadhesive properties (4.77 g/cm2) and disintegration time (68 sec). Conclusions: The formulations of F2 were found to be suitable candidates for the development of sublingual films instead of oral tablet for the therapeutic use.