Ginsenoside Rg3 bile salt-phosphatidylcholine-based mixed micelles: Design, characterization, and evaluation

Abstract

20(R)-Ginsenoside Rg3 (G-Rg3) has good inhibition of tumor angiogenesis and anti-tumor effect. However, its poor aqueous solubility and liposolubility are not ideal for clinical applications. In this study, a G-Rg3 bile salt-phosphatidylcholine-based mixed micelle system (BS-PC-MMS) was prepared. The optimization of G-Rg3 BS-PC-MMS was carried out using response surface methodology based on a central composite design. The encapsulation efficiency (EE) and light transmission (LT) of the optimized formulation were 90.69±2.54% and 99.10±3.12%, respectively. The average particle size of micelles was 20 nm. To increase the stability of G-Rg3 BS-PC-MMS, the lyophilized formulation of micelles was prepared. The G-Rg3 BS-PCMMS did not produce hemolysis of erythrocytes within a certain concentration range and exhibited a good inhibition of tumor cells. The chick embryo chorioallantoic membrane assay results showed that the G-Rg3 BS-PC-MMS significantly inhibited angiogenesis. The G-Rg3 BS-PC-MMS is thus shown to be a safe, stable, and promising drug delivery system.