Preparation and in vitro Evaluation of Rasagiline Mesylate Hybrid Nanoparticles

سال انتشار: 1402
نوع سند: مقاله ژورنالی
زبان: انگلیسی
مشاهده: 51

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شناسه ملی سند علمی:

JR_ARCHRAZI-78-3_028

تاریخ نمایه سازی: 6 دی 1402

چکیده مقاله:

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.

نویسندگان

B. W Mahde

College of Pharmacy, University of Al-Qadisiyah, Al-Qadisiyah, Iraq

A Abbas Hussein

Baghdad College of Medical Sciences, Baghdad, Iraq

A. S Sahib

Al-Mustaqbal University College, Babylon, Iraq

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