Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2021 , Vol 25 , Issue 5
Development of rasagiline mesylate loaded solid lipid nanoparticles in a thermosensitive mucoadhesive gel: Formulation design using DoE, in-vitro and ex-vivo characterization
Mahmut Ozan TOKSOY1,Fahriye Figen TIRNAKSIZ2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Dicle University, 21280, Sur, Diyarbakır, Turkey
2Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330, Yenimahalle, Ankara, Turkey
DOI : 10.29228/jrp.61 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. Keywords : Rasagiline mesylate; solid lipid nanoparticle; thermosensitive mucoadhesive gel; full factorial design; ex-vivo permeation
Marmara University