Abstract

FORMULATION AND IN VITRO EVALUATION OF AN ANTIMIGRAINE NANOPARTICULATE SYSTEM IN A MUCOADHESIVE THERMOREVERSIBLE INTRANASAL GEL

Sherilraj P. M.*, Prasanth M. S. and Ammu Shaji

Abstract

Migraine is simply a headache associated with nausea and sensitiveness to light and sound. The present work aims to formulate, optimize and evaluate mucoadhesive thermoreversible in situ gel of antimigraine drug-loaded nanoparticle for intranasal delivery. Characterization studies of drug and excipients were performed and results confirmed drug compatibility with polymers. Ionic gelation method was employed in the preparation of drug-loaded nanoparticles. The drug-loaded nanoparticles were incorporated in the optimized gel formulation. By using the optimized formula, in situ gel with the desired range of gelation temperature and gelling time were obtained. Sumatriptan showed a rapid drug release from the solution. The release of Sumatriptan from the gel-containing nanoparticulate system was very slow and in a controlled manner when compared to the release profile of solution form. In vitro drug release of Sumatriptan nanoparticle-loaded gel was best explained by Higuchi’s model. The mechanism of release of drug from gel containing nanoparticulate system follows a non-Fickian or anomalous diffusion. From the Ex vivo skin permeation study, decrease in flux was observed for Sumatriptan nanoparticle-loaded gel compared with plain Sumatriptan solution. From the result, it was observed that drug permeation became slower when the drug was added to the formulation in its entrapped form rather than in solution form. With this kind of formulation, the bioavailability of drugs can be increased and undesirable side effects can be avoided. Therefore, an antimigraine drug-loaded nanoparticulate system in a mucoadhesive thermoreversible intranasal gel prepared in this study is more useful than a conventional formulation in therapy.

Keywords: Migraine, Thermoreversible gel, Nanoparticles, Intranasal drug delivery.