Drug Discov Ther. 2009;3(6):266-271.

In vitro evaluation of different transnasal formulations of sumatriptan succinate: A comparative analysis.

Gonjari ID, Karmarkar AB, Kasture PV


SUMMARY

Sumatriptan succinate is an agonist for a vascular 5-hydroxytryptamine (5-HT)1 receptor subtype (probably a member of the 5-HT1D family). It does not have significant affinity for the remaining 5-HT receptors. It does not have affinity for alpha1, alpha2 or beta-adrenergic, dopamine1, dopamine2, muscarinic or benzodiazepine receptors. The objective of the study was to evaluate the in vitro transnasal absorption of sumatriptan succinate through sheep nasal mucosa and to determine its in vitro permeation behavior from various formulations containing penetration enhancers. In this study four different thermoreversible gel formulations designed for nasal delivery of sumatriptan succinate were formulated. The formulations were prepared by using a poly(oxythylene) poly(oxypropylene) block copolymer (Pluronic F 127) based gel along with different permeation enhancers and a pluronic lecithin organogel base. The effect of different concentrations of sodium glycocolate, EDTA and transcutol on in vitro nasal diffusion of sumatriptan succinate was studied. The best permeation profile was obtained with a formulation containing transcutol at a concentration of 0.005% w/w. Pluronic lecithin organogel showed good gelling properties at a concentration in the 20% range.


KEYWORDS: Sumatriptan succinate (SS), Pluronic F 127 (PF 127), transcutol (TC), sodium glycocolate (SG), EDTA, pluronic lecithin organogel (PLO)

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