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

Ginsenoside (GS), one of the main active components in ginseng, can enhance insulin sensitivity, improve the function of islet ß 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 âˆ¼ 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.

Oral liposomes encapsulating ginsenoside compound K for rheumatoid arthritis therapy.

Ginsenoside compound K (GCK) can efficiently treat rheumatoid arthritis (RA) due to its immune and anti-inflammatory functions. However, GCK exists some shortcomings such as poor aqueous solubility, low permeability to the intestinal cell membrane, and serious P-gp efflux, thus limiting its application. In order to solve these problems, a folic acid-targeted drug delivery system based on liposomes (FA-LP-GCK) was developed. The prepared FA-LP-GCK had a uniform size distribution and spherical structure, the particle size was 249.13 ± 1.40 nm. Meanwhile, they had high encapsulation efficiency (93.33 ± 0.05 %). FA-LP-GCK also presented good stability in artificial gastric juice, so they can be absorbed into the intestine and enter the blood circulation. The activated RAW 264.7 cells were chosen to evaluate the cytotoxicity and cellular uptake capacity of FA-LP-GCK. FA-LP-GCK showed stronger growth inhibition and cellular uptake ability against activated macrophages. Finally, the efficacy of FA-LP-GCK in vivo was evaluated in the adjuvant arthritis rat model. The results showed that FA-LP-GCK can significantly reduce joint swelling. Furthermore, it can significantly inhibit the expression of pro-inflammatory cytokines and improve synovial hyperplasia of joints and pathological changes in the spleen. Therefore, FA-LP-GCK may be a potential therapeutic approach for RA.