Enhanced antidiabetic performance through optimized charantin-loaded nanostructured lipid carriers: Formulation and In vivo studies in diabetic mice

Abstract

The hypoglycemic potential of charantin, a compound from Momordica charantia L., has been well-documented, but its pharmaceutical application faces challenges like poor solubility, low permeability, and suboptimal bioavailability. This study aimed to develop and optimize charantin-loaded nanostructured lipid carriers (Ch-NLCs) to enhance their antidiabetic efficacy. Using a 32 factorial design and high-pressure homogenization, Ch-NLCs were formulated with Precirol and Labrasol as solid and liquid lipids, respectively, combined with surfactants Tween 80 and Poloxamer 188. The optimization focused on key parameters such as particle size, entrapment efficiency (%EE), and zeta potential. FTIR confirmed the interaction between charantin and lipids, while DSC and XRD analyses showed the amorphous nature of Ch-NLCs. The optimized Ch-NLCs exhibited a particle size of 221.0 nm, an %EE of 81.89 %, and a zeta potential of −24.42 mV. In vitro release studies demonstrated a sustained release profile of charantin from the NLCs. In vivo studies on streptozotocin (STZ)-induced diabetic mice revealed significantly enhanced antidiabetic effects of Ch-NLCs compared to pure charantin. Specifically, Ch-NLCs led to substantial reductions in blood glucose levels, total cholesterol (T-Cho), low-density lipoprotein (LDL) and glycosylated hemoglobin (HbA1c) levels, while improving high-density lipoprotein (HDL). These findings highlight the potential of Ch-NLCs as an effective delivery system for charantin in diabetes management. In conclusion, the study successfully engineered and optimized Ch-NLCs, demonstrating their superior pharmacokinetic profiles over pure charantin. These results suggest that Ch-NLCs could be a promising candidate for effective diabetes management, warranting further clinical investigation to confirm their therapeutic potential in human subjects.