Volume 2

July-September 2010

Development and characterization of nasal mucoadhesive microemulsion of sumatriptan succinate

Ashwini Rasal, H S Mahajan, H T Shaikh, S J Surana

The purpose of this study was to enhance the brain uptake of sumatriptan succinate (SS) in o/w microemulsion, which was suitable for intranasal delivery. Microemulsion system with Tween 80, Span 80 as surfactants and n-butanol as cosolvent and iso propyl myristate as oil was developed for intranasal delivery of sumatriptan succinate. Single isotropic region, which is considered as o/w microemulsion was found in the pseudo-ternary phase diagrams developed at various tween 80, span 80 and n butanol ratios. The optimal microemulsion formulation consisted of 5% iso propyl myristate, 25% water, and 70% (w/w) surfactant/cosurfactant [surfactants are 52.5% (tween 80 36.75% span 80 15.75%) cosurfactant (n butanol) 17.5% at 3: 1 weight ratio] With the increase of tween 80 concentration, the microemulsion region area, microemulsion viscosity, and the amount of water into the microemulsion system increased. Mucoadhesive microemulsion was prepared by using HPMCK4M as a mucoadhesive polymer to increase the residence time inside the nasal cavity for prolonged action and direct targeting release of drug to the brain. Nasal absorption of sumatriptan succinate from this mucoadhesive microemulsion was found to be fairly rapid, as it converts into gel inside the nasal cavity and increase the residence time and could improve bioavailability of the drug. The result suggests that this mucoadhesive microemulsion may be a useful approach for the rapid onset delivery of sumatriptan succinate during the emergency treatment of acute attack of migraine.

Keywords: Microemulsion, Nasal Delivery, Mucoadhesion, Sumatriptan Succinate.