AGGRANDIZED TRANSDERMAL DELIVERY OF GLIMEPIRIDE VIA TRANSFERSOMES: FORMULATION, EVALUATION AND STATISTICAL OPTIMISATION

摘要

The aim of the study was to prepare and statistically optimize transdermal formulation of antidiabetic drug Glimepiride (Glmp). In the present investigation Protransfersome gel (PTG) of glimepiride was prepared by modified coacervation phase separation technique and characterised for various parameters like vesicles shape, vesicles size and size distribution, entrapment efficiency and stability. Box-Benkhen model was chosen as optimization design. Three factors (amount of phospholipids, amount of surfactant and amount of drug) were varied at three levels Box-Benkhen statistical experimental design. These factors were found to have significant effects on the vesicular size(296.6±1.2nm), PDI(0.241±0.4) and drug loading(71.90±4.8%) and were optimized based on the desirability of the responses. The skin permeation studies were performed for 24 hours on pig ear skin using Franz diffusion cell. The flux value obtained from PTG (5.129±1.24 μg/cm 2 /h) was greater as compared to the drug suspension (0.430 μg/cm 2 /h). PTG formulation showed good stability at 4±1 0 C and after 3 months of storage there was no change in liquid crystalline nature, size of vesicles, drug content and other characteristic parameters observed. In vivo pharmacokinetic study of PTG showed significant drug release as compared to plain transdermal patch of the drug. Hence, present study reveals that PTG generates a new breakthrough for the transdermal delivery of Glimepiride with higher bioavailability, negligible gastrointestinal and hepatic side effects and increased patient compliance.