Ex-vivo skin permeation studies of sumatriptan succinate using different solvent systems and its comparison with PLGA nanoparticles

摘要

Sumatripatan succinate ( SS) is a 5-HTsub1D/sub agonist used in migraine therapy. Its low oral bioavailability (~15 %) is due to extensive pre-systemic metabolism and low biological half-life. The frequent administration of SS is required to maintain effective plasma concentration. In the present investigation, polymeric nanoparticles of SS (SS-NPs) were prepared by Wsub1/sub/O/Wsub2/sub double emulsion solvent evaporation method followed by probe sonication. Poly-(lactide-co-glycolide) (PLGA) and poloxamer 188 were used as polymer and surfactant respectively to formulate SS-NPs. The particle size, polydispersity index, zeta potential, percent entrapment efficiency of SS-NPs were found to be 126 nm, 0.06, (-) 24.1 mV, 32.52 ± 2.34 % respectively. Characterization of lyophilized SS-NPs revealed formation of drug entrapped amorphous SS-NPs. Ex-vivo skin permeation studies of SS were conducted using distilled water, ethanol (EtOH), propylene glycol (PG) and their binary combinations. The lag time, flux, permeability and steady state permeability coefficient and enhancement ratio were determined. The ex-vivo permeation profiles of SS in different solvent systems were compared with SS-NPs in distilled water. The maximum flux of 345.8 μg.cmsup-2/sup.hsup-1/sup was obtained with solvent system comprising 33% PG in EtOH. The minimum lag time and a comparable flux value was obtained in ex-vivo diffusion studies of SS-NPs. Hence, it can be concluded that SS-NPs can be administered in transdermal drug delivery system using a solvent system comprising 33%PG in EtOH. The present investigation indicated that using suitable solvent system and PLGA nanoparticles, the skin permeation of SS can be enhanced.