FORMULATION, OPTIMIZATION AND EVALUATION OF GLIMEPIRIDE TRANSFERO-SOMAL GEL FOR ANTIDIABETIC ACTIVITY IN RATS

Transferosomes are a special liposome type consisting of phosphatidylcholine and an edge activator. Glimepiride is a second-generation sulphonylurea exerting its effects in patients with type II Diabetes. Glimepiride is hydrophobic in nature possess less solubility and permeability. The study aims to formulate, optimize and evaluate Glimepiride Transferosomal gel for antidiabetic activity in Rats. Glimepiride loaded Transferosomes were prepared using thin film hydration method and were optimized using factorial design (3²) using Design-expert® software (Version 7.0.0, Stat-Ease Inc., Minneapolis, USA); different formulations (F1-F9) were prepared. Two different independent variables were used, which include: Amount of Soya lecithin (X1), Amount of tween 80 (X2), and the responses are Entrapment Efficiency (Y1), vesicle size (Y2). The optimized formulation of Glimepiride transferosomes was incorporated into a Carbopol 934 gel base and 1.5 % of Glimepiride transferosomal gel was prepared, which was evaluated for drug content, pH, spreadability, viscosity and in-vitro drug release. The prepared Glimepiride transferosomes had a maximum EE% was found to be (73.25 %), particle size was found to be (323 nm), the Spreadability value was 12.88 cm. The prepared transferosomal gel was found to be 86.02%, which represents good content uniformity. The viscosity was found to 1656±1.25 cps. The percentage drug release for Glimepiride transferosomal gel was found to be 89.05±0.25. R² values for the optimized formulation were highest for the Higuchi model. This indicated that the drug release from all the formulations followed diffusion controlled release mechanism. Stability studies showed that Glimepiride Transferosomal gel is more stable at 4°C when compared to room temperature.