PEGylation of Ginsenoside Rg3-Entrapped Bovine Serum Albumin Nanoparticles: Preparation, Characterization, and In Vitro Biological Studies

Ginsenoside Rg3 (Rg3) is one of three triterpene saponins from red ginseng. It has important structural functions and pharmacological properties. However, due to its poor solubility, low bioavailability, and short half-life in blood circulation, its clinical application was unsuccessful for the treatment of a variety of cancers. In order to overcome this limitation, this study prepared mPEGylation-Rg3 bovine serum albumin nanoparticles (mPEG-Rg3-BSA NPs). The characteristics of the NPs, such as drug entrapment efficiency, drug loading efficiency, surface morphology, thermal stability, and cytotoxicity in vitro, were investigated. The results showed that the appropriate particle size of the obtained NPs was 149.5 nm, the water solubility and stability were better than free Rg3, and the drug entrapment efficiency and drug loading efficiency were 76.56% and 17.65%, respectively. Moreover, the cytotoxicity assays of the mPEG-Rg3-BSA NPs and free Rg3 revealed that the mPEG-Rg3-BSA NPs have greater anticancer effects in HepG2 cells and A549 cells. However, the cytotoxic effect of free Rg3 was higher than the mPEG-Rg3-BSA NPs in L929 cells. The results indicated that using the mPEGylation method and selecting BSA as a carrier to form the nanodrug carrier system were effective for improving the properties of Rg3.