Glibenclamide is a second generation hypoglycaemic agent used for the management of Diabetes Mellitus. In the present study, matrix type transdermal patches of Glibenclamide were prepared by solvent casting technique using various combinations of hydrophobic (ethyl cellulose) and hydrophilic (Polyvinyl pyrrolidone) polymer, named as batch A (without penetration enhancer) and batch B (with penetration enhancer). Initial studies included with the compatibility among the drug and the polymers. All fabricated patches were subjected to physicochemical characterization, in vitro performance of transdermal patches and stability studies. An optimized ethyl cellulose and polyvinyl pyrrolidone composition was chosen to measure the effect of vegetable oils as penetration enhancers on the drug permeation across Wistar rat skin and on the skin itself. In vivo acute hypoglycemic activity in Wistar rats using streptozotocin-induced diabetes model was also performed.The results indicated no interaction between the drug and the polymers. The data obtained from the physicochemical characterization suggested less variations among the patches. Percentage cumulative drug release from the in vitro study depicted the effect of polyvinyl pyrrolidone, on increasing its concentration with respect to ethyl cellulose increases the release of Glibenclamide from the matrix. Significant effect of vegetable oils on the lipid and protein framework of the skin was seen which results in approximately 1.3 fold times increase of Glibenclamide flux. The hypoglycemic activity revealed the significant reduction in blood glucose levels (≈55% at 12th hour) from the transdermal patches which proves the sustained release of Glibenclamide over a prolonged period of time. Thus combination of polymers with the use of vegetable oils as penetration enhancers could be used to prepare stable and effective Glibenclamide transdermal patches which exhibit better control of the blood glucose level in diabetes mellitus.
Keywords: Hypoglycemic activity, in vitro permeation, solvent casting technique, transdermal patches, vegetable oils.
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