Development and characterization of anti-diabetic liposomal formulation

K. Florence Rachel


Introduction: Diabetes is a chronic health condition that affects how human body turns food into energy. It is most commonly occurring disease. Liposomal technology has been employed for the flourishing encapsulation of various drug molecules and oral route of administration is much more convenient. The main aim was to develop and characterize oral antidiabetic liposomal formulation. Further, prepared liposomal formulations evaluated for particle size, % drug release, differential scanning calorimetry (DSC), Fourier transform infrared, in vitro release, release kinetics model, animal studies, and experimental data subjected to statistical testing using one-way analysis of variance followed by Dunnett test were carried out. Materials and Methods: The liposomal formulations were formulated using thin-film hydration technique. Sitagliptin liposomal formulations (F1-F6) were prepared by employing soy lecithin and cholesterol in varying concentration. Results: In vitro release of different antidiabetic liposomal formulations was performed and observed through cellophane membrane using Franz Diffusion cell. The finalized liposomal formulation (F6) showed better release. To check the antihyperglycemic activity was performed using oral glucose tolerance test using Sprague Dawley (SD) rats for the optimized formulation. Finalized formulation (F6) elicited the better in-vitro release 87.85% at 8 h in comparison with the pure drug release was initiate to be 59.57%. Particle size distribution and zeta potential were found to be 40 nm as well as 40 mV, respectively. In vitro release kinetic models were shown that it follows first-order kinetics and high regression coefficient r2 value was 0.975. The DSC thermogram of sitagliptin was found 221.7°C. The DSC thermogram of physical mixture of cholesterol along with soy lecithin was found to be 42.1°C and 220.3°C. DSC analysis confirmed that there was negative interaction between the drug and excipients. Discussion and Conclusion: It would be concluded that antidiabetic liposomal formulation using sitagliptin as drug, soy lecithin and cholesterol as polymer can be formulated thereby can enhance oral bio-availability. The optimized formulation (F6) has shown best formulation based on the in vitro drug release. In vivo studies for the optimized formulation (F6) observed that sitagliptin was found to be more potent than sitagliptin marketed formulation and activity was persisted till 4 h.

Full Text:




  • There are currently no refbacks.