FORMULATION AND EVALUATION OF GLICLAZIDE ETHOSOMES AS A NOVEL DRUG CARRIER

The main aim of the present investigation was to evaluate transdermal potential ethosomes bearing anti-diabetic drug Gliclazide. Total eight formulations (F1F8) of ethosomes were prepared by using cold method with three different concentrations of phospholipid (0.5, 1, 2 % w/w) and ethanol (10, 20, 30 % v/v) and it was compared with hydroethanolic solution. They were evaluated for vesicular shape, size, entrapment efficiency and in-vitro studies. The formulation F6 (ethanol 20 % v/v and phospholipid (1 % w/w) was selected as the best formulation due to its optimum vesicle size, entrapment efficiency, less turbidity and maximum invitro release. The stability studies performed on F6 formulation at two different temperatures of 25o ± 2oC and 4o ± 2oC for the period of 6 months also shows the satisfactory results. It was further incorporated into gel using carbopol 934 (1, 1.5, 2 % w/w) as a base. The carbopol concentration of 1.5% w/w gives the maximum in-vitro release of 96.06 ± 0.16 % in dialysis membrane and ex-vivo release of 79.67 ± 0.35 % in case of skin of mice. The results showed the potential of ethosomes of being a safe and very efficient drug carrier for transdermal delivery of drug. INTRODUCTION: Diabetes mellitus is the most common endocrine disorder affecting around 2-3% of the population worldwide and its incidence is rising day by day. In the year 2000, 150 million people worldwide had diabetes and expected to double by this year. By 2030, the WHO estimates that the number of people with diabetes will almost double to 366 million. More than 220 million people worldwide have diabetes and almost 80% of the people die with diabetes in low and middleincome countries 1-2 . Diabetes mellitus is a heterogeneous group of metabolic disorder characterized by chronic hyperglycemia with disturbance of carbohydrate, protein and fat metabolism. There are two major types of diabetes mellitus -Type 1: Insulin dependent diabetes mellitus (IDDM) and Type 2: Non-insulin dependent diabetes mellitus (NIDDM) 3-7 . QUICK RESPONSE CODE DOI: 10.13040/IJPSR.0975-8232.6(5). 2072-80 Article can be accessed online on: www.ijpsr. com DOI link: http://dx.doi. org/10.13040/IJPSR.0975-8232.6(5). 2072-80 Second generation sulfonylurea are 20-100 times more potent than first generation sulfonylurea. Glibenclamide, Glimepride, Glipizide, Gliclazide are the second generation sulfonylurea class of insulin secretagogues used in management of noninsulin dependent diabetes mellitus (NIDDM). The sulfonylurea acts by stimulating β-cells of pancreas to release insulin. It increases both basal insulin secretion and meal stimulated insulin release. It also increases peripheral glucose utilization; decrease gluconeogenesis; increases number and sensitivity of insulin receptor. Gliclazide has demonstrated superior efficacy and safety and lower incidence of hypoglycemia compared to other sulfonylureas 8-11 . Ethosomes are soft, malleable ethanol containing novel vesicular carriers that transport active substances through stratum corneum into the deeper layers of the skin. The high concentrations of ethanol cause inter – digitation effect on the lipid barriers, allows vesicles to penetrate through stratum corneum barrier. These novel vesicles showed enhanced permeation, increased bioavailability with no toxic raw materials