Preparation and in vitro Evaluation of Rasagiline Mesylate Hybrid Nanoparticles

Rasagiline is a selective and irreversible inhibitor of monoamine oxidase B (MAO-B) that is effective in the treatment of Parkinson’s disease (PD). It had antioxidant and anti-apoptotic activity in experimental models. Moreover, it has low permeability and its oral bioavailability is weak and highly variable due to extensive first-pass hepatic metabolism (۳۵%). This study aimed to formulate rasagiline mesylate (RM) as a lipid-polymer hybrid nanoparticle in order to enhance its permeation and increase its chance to be absorbed by lymphatic circulation to avoid metabolism and control its release. Successful formulation (PCL-۲) was reached by the nanoprecipitation method using polycaprolactone with RM in the organic phase and lecithin in the aqueous phase DSPE-PEG. The lipid:polymer ratio of ۲۴% and DSPE: lecithin of ۵۰% resulted in stable nanoparticles having a particle size of ۱۳۲±۴.۵۸ nm, polydispersity index of ۰.۲۷۳±۰.۰۲, zeta potential of -۲۵.۶±۳.۳, entrapment efficiency of ۴۶±۳.۹%, and drug loading of ۵۱.۹۳±۶.۵. Results showed that the diffusion was more effective on the release profile than the degradation and resulted in a Fickian diffusion mechanism.

کلیدواژه ها:

Nanoparticles ، Parkinson's disease ، Propargylamine ، Rasagiline