Abstract
Type 2 Diabetes Mellitus (T2DM) is one of the prevalent metabolic disorders and is the leading cause of death across the globe. In the present invention, we reported significant synergistic anti-diabetic efficacy of novel SGLT II inhibitor, Canagliflozin (CFZ) with natural phytoconstituent, Trigonelline (TGL) in fenugreek oil using a self-microemulsifying based formulation. The optimized liquid SMEDD formulation (NADF) containing fenugreek oil (18.11% w/w), vitamin E TPGS (53.40% w/w) and linalool (10.12% w/w) were optimized by Design of Experiments and produces nanoparticulate stable microemulsion in vitro. Conversion to solid SMEDDS (NADF-SD) was facilitated by adsorption onto natural biosorbent coffee husk. The optimized solid formulation containing CFZ was in amorphous state with enhanced surface area, negligible chemical incompatibility and uniform drug content. Scanning electron microscopy validated the powdered SMEDDS′ spherical form. The release behavior of CFZ in NADF-SD in diverse biorelevant environments is enhanced by in vitro dissolution. Furthermore, neither pure CFZ nor the marketed product had any food impact. The permeability of the jejunum intestinal segment in rats was remarkable, as validated by confocal microscopy. In comparison to a pure drug and a commercial product, these trials show a 3.99 and 2.56 fold increase in Cmax and a 2.23 and 1.56 fold increase in AUC0-24h, respectively. Through biochemical levels, urine glucose excretion investigations, and SGLT II expression in rats, pharmacodynamic examination of improved NADF-SD demonstrates enhanced anti-diabetic effectiveness of CFZ. In a nutshell, this natural lipid-based micro particulate system is well-suited for this drug's anti-diabetic activity and synergy with CFZ.
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