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 (35%). 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-2) 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 24% and dspe: lecithin of 50% resulted in stable nanoparticles having a particle size of 132±4.58 nm, polydispersity index of 0.273±0.02, zeta potential of -25.6±3.3, entrapment efficiency of 46±3.9%, and drug loading of 51.93±6.5. results showed that the diffusion was more effective on the release profile than the degradation and resulted in a fickian diffusion mechanism.