Fahriye Figen TIRNAKSIZ, Mahmut Ozan TOKSOY

Development of rasagiline mesylate loaded solid lipid nanoparticles in a thermosensitive mucoadhesive gel: Formulation design using DoE, in-vitro and ex-vivo characterization

Rasagiline mesylate (RM) is a selective irreversible MAO-B inhibitor used in the treatment of Parkinson’s disease. This study was designed to prepare and optimize RM loaded solid lipid nanoparticles (RM-SLNs) in a thermosensitive mucoadhesive gel (RM-SLNs-GEL). RM-SLNs were prepared combining Gelucire 50/13 (10%), Labrasol (0.3%) Cremophor RH40 (12%) with a mixing rate and time of 500 rpm, 45 min. Mucoadhesive gels were prepared combining Poloxamer 407 and HPMC E5 (15.5% + 0.25%). Optimized formulation (RM-SLNs-GEL) was evaluated for sol-gel transition temperature, viscosity, mucoadhesive force, particle size and distribution, SEM imaging, in-vitro drug release and ex-vivo drug permeation. It was found that optimal formulation had a suitable gelation temperature at 31°C ± 0.2°C. It was observed that the system was fluid during nasal application at 25°C and viscous at nasal temperature at 32°C. RM-SLNs-GEL has shown particle size, polydispersity index (PDI), % encapsulation efficiency (EE%); 253 nm, 0.282, 37.8% respectively. Ex-vivo permeation study exposed significant enhancement of permeability of RM-SLNs-GEL across mucosa than RM loaded thermosensitive gel (RM-GEL). Our results show that RM-SLNs-GEL formulation could be a potential drug delivery system for the treatment of Parkinson’s disease.

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