A ginsenoside G-Rg3 PEGylated long-circulating liposome for hyperglycemia and insulin resistance therapy in streptozotocin-induced type 2 diabetes mice

Abstract

Ginsenoside (GS), one of the main active components in ginseng, can enhance insulin sensitivity, improve the function of islet β cells, and reduce cell apoptosis in the treatment of diabetes. However, the drawbacks of high lipid solubility, poor water solubility, and low oral availability in Ginsenoside Rg3 (G-Rg3) seriously limit further application of GS. In this work, a G-Rg3 PEGylated long-circulating liposome (PEG-L-Rg3) is designed and developed to improve symptoms in type 2 diabetic mice. The as-prepared PEG-L-Rg3 with a spherical structure shows a particle size of ∼ 140.5 ± 1.4 nm, the zeta potential of −0.10 ± 0.05 mV, and a high encapsulation rate of 99.8 %. Notably, in vivo experimental results demonstrate that PEG-L-Rg3 exhibits efficient ability to improve body weight and food intake in streptozotocin-induced type 2 diabetic mice. Moreover, PEG-L-Rg3 also enhances fasting insulin (FINS) and insulin sensitivity index (ISI). In addition, the glucose tolerance of mice is significantly improved after the treatment of PEG-L-Rg3, indicating that PEG-L-Rg3 can be a potential drug for the treatment of type 2 diabetes, which provides a new way for the treatment of type 2 diabetes using ginsenosides.