Formulation and Evaluation of Sitagliptin Liposomes

Abstract

Sitagliptin is a (BCS) III drug which has low permeability and high solubility. The major purpose of the study is to develop & differentiate the Anti-diabetic liposomal formulation and to evaluate the prepared formulations. The Liposomes were formulated by 'Thin Film hydration technique'. Six liposomal formulations of 'sitagliptin' were prepared. Soy lecithin and cholesterol in the concentration range of 300:100mg were used as an polymer. The Invitro release data of different formulations was studied and observed through cellophane membrane using Franz Diffusion cell. The formulation (F6) showed best 'drug release'. Finalised formulation (F6) gave the best In-Vitro drug release 87.85% at 8 hours in comparision with the 'pure drug release. The DSC thermogram of physical mixture of cholesterol along with soy lecithin was found to be 42.1°C and 220.3°C.DSC confirmed that there is negative interaction between the drug and excipients. To check the Antihyperglycaemic activity, Oral glucose tolerance test and Anti-diabetic action In-vivo antidiabetic activities were performed by using SD rats for the optimised formulation. In-Vivo studies revealed that optimised formulation (F6) of sitagliptin was found to be more potent than sitagliptin marketed formulation and activity was persisted till 4 hour.