ABSTRACT
OBJECTIVE: To prepare nimodipine-loaded nanoemulsion(NimNE) suitable for intranasal administration and preliminary investigate their physical and chemical properties and brain tissue targeting. METHODS: Nanoemulsion were prepared using titration method and characterized for viscosity, pH, globule size and size distributions, Zeta potential and ciliotoxicity. Biodistribution of NimNE and Nim solution in the brain tissue and plasma of rats following intranasal and intravenous administrations were examined using HPLC. RESULTS: The optimal nanoemulsion formulation consisted of isopropyl myristate(IPM), solutol® HS-15/glycerin(4:1) and water and were transparent and stable with mean globule size between 20 to 30 nm and almost no ciliotoxicity. After intranasal (in) administration of NimNE at a dose of 2 mg·kg-1, the ratios of AUC in brain tissues to that in plasma obtained after nasal administration were significantly higher than those after iv administration in 240 min. CONCLUSION: These results suggest that the nanoemulsion system is a promising approach for intranasal delivery of Nim to brain tissue. Copyright 2012 by the Chinese Pharmaceutical Association.