Publication:

Enhanced glycemic control and organ protection with empagliflozin microemulsion in alloxan-induced diabetic mice

Background Diabetes mellitus (DM) is a serious challenge for worldwide health and is predominant in most populations living with type 2 diabetes (T2DM), thus new drug strategies must be created to enhance drug delivery and use. Empagliflozin is also a sodium-glucose cotransporter-2 (SGLT2) inhibitor that has high solubility and low intestinal permeability, thereby making its bioavailability in traditional formulations is limited. To overcome these drawbacks, we have formulated an empagliflozin microemulsion, which we expect to enhance permeability and therapeutic efficacy.

Methods The microemulsion was formulated according to a double emulsion technique with olive oil, Tween 80, ethanol, and xanthan gum, and followed by analysis on physical properties, stability, and drug release kinetics. The microemulsion was compared to the empagliflozin tablet for glycemic control and protection of organs in alloxan-induced diabetic Swiss albino mice.

Results The formulation yielded spherical droplets (0.2-0.3 µm), high encapsulation efficiency (EE) (84.9%), and sustained in vitro release (76% after 12 h). The in vivo findings indicated the microemulsion was more effective, with 63.50% reduction in blood glucose levels vs. 55.70% for the tablet, and a significant recovery of body weight (30.16 g vs. 28.93 g). Histopathological examination of microemulsion group revealed restored pancreatic islets and normal renal structures in contrast to significant destruction in diabetic controls.

Conclusions These results emphasize the ability of the microemulsion to enhance the pharmacodynamic profile of empagliflozin and can be considered as a new alternative to classical drugs in diabetes treatment. This study highlights significance of the above therapeutic benefits including patient compliance in a novel phase of drug delivery systems.