FORMULATION AND EVALUATION OF GLIMEPIRIDE LOADED TRANSETHOSOME FOR TREATMENT OF DIABETES
Hardik Soni, Sunil Kumar Jain, Vivek Jain, Mansha Singhai, Rupesh Kumar Jain
ABSTRACT
The present study focuses on the formulation, optimization, and evaluation of Glimepiride-loaded transethosomal gel for enhanced transdermal drug delivery in the treatment of type 2 diabetes mellitus. Glimepiride, a poorly water-soluble sulfonylurea, suffers from variable oral bioavailability and hepatic first-pass metabolism, which limits its therapeutic efficacy. To overcome these challenges, transethosomes a novel class of ultra-deformable lipid vesicles were employed to improve the drug’s skin permeation and sustained release characteristics. A series of fourteen formulations (F1–F14) were prepared by varying lipid ratios, ethanol concentration, drug content, and stirring duration. Among them, formulation F12 was optimized based on its smallest vesicle size (125.36 nm), high entrapment efficiency (74.65%), and stable zeta potential (-40.36 mV). The optimized formulation was incorporated into a gel base and evaluated for viscosity, drug content, spreadability, extrudability, and in vitro drug release. The gel exhibited suitable viscosity (3510?±?20 cps), uniform drug distribution (99.45?±?0.15%), and favorable spreadability and extrudability. In vitro release studies revealed a sustained drug release profile, with 94.65% cumulative drug release over 10 hours. Kinetic modeling indicated that the drug release followed the Higuchi model (R² = 0.9837), confirming diffusion-controlled release. The Glimepiride-loaded transethosomal gel demonstrated excellent physicochemical properties, enhanced drug release behavior, and potential for improved therapeutic efficacy through transdermal application. This delivery system may offer a promising alternative to conventional oral administration of Glimepiride, improving patient compliance and minimizing systemic side effects.
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