Design and development of Ethosomal Gel of Diacerein by using cold method

B. Madhura, M. Kishore Babu*
Department of Pharmaceutics, Krishna Teja Pharmacy College, Tirupati-517506, Chittoor Dist, Andhra Pradesh

A B S T R A C T
Trans dermal route offers several potential advantages over conventional routes. These advantages includes avoidance of first pass metabolism, predictable and extended duration of action, minimizing undesirable side effects, utility of short half-life drugs, improving physiological and pharmacological response, avoiding the fluctuation in the blood levels, and most important it provides patient convenience. Recently advancement in liposomes was done and result obtained was “Ethosomal system”. Ethosomal system showed topical delivery with higher trans dermal flux and higher skin deposition and became an attractive option as it has several desirable advantages. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications. Diacerein Ethosomes were prepared using the method reported by Touitou et al.,(2000) with little modification. Studies were performed on Ethosomes containing 20%, 30%, 40% and 50% w/w ethanol with sonication used for their size reduction. To confirm the presence of vesicular structure, formulations were visualized under microscope at different magnified fields, which showed presence of lipid bilayer as well as spherical structure of vesicles. Using the same microscopic method and special software “particle size analysis”, size of vesicle was determined for sonicated Ethosomes. Vesicular size was found to be in the range of 0 – 5.483 µm. Vesicular size was reduced up to 3 folds by sonication. In-vitro release was carried out using dialysis membrane. The values of drug release were EF₁ (20% alcohol) 76.89%, EF₂ (20% alcohol) 82.31%, EF₃ (20% alcohol) 73.62, EF₄ (30% alcohol) 86.42%, EF₅ (40% alcohol) 72.09%, EF₆ (50% alcohol) 63.21%. The order of drug release was found to be first order for all the formulations. Percentage drug accumulation into skin was also found to be maximum by the Ethosomes containing 30 % w/w ethanol and 3% lecithin which showed effective subdermal deposition and indicated better subdermal   action for hypertension
Keywords: Trans dermal, lipid bilayer, alcohol, lecithin, Ethosomal system