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

Abstract

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.

Micron and nano hybrid ufasomes from conjugated linoleic acid, their vesiculation and encapsulation of ginsenoside Rg3

“…To assay the in vitro releasing characteristics of Rg3 from CLAVs, dialysis was conducted with free Rg3 as the control at different pH condition. 27 First, the dialysis bag (molecular weight cut-off 8000 Da) containing 5 mL of the CLAV-Rg3 suspension was immersed in 100 mL of PBS buffer (pH 7.4 or pH 3.0, 0.1 mol L −1 , containing Tween 80 of 0.2% w/v); the dialysis medium was stirred at 37 °C. At each time interval, 0.5 mL of dialysis medium was taken for sampling, filtrated and analyzed using HPLC as described earlier.…”

“…26 Its clinical application is limited due to its poor water solubility, short circulating half-life and poor specificity for tumor tissue targeting. 27 The most applied stratagem to overcome the solubility issue is encapsulation, which can improve oral bioavailability, significantly prolong pharmacodynamics and reduce drug toxicity. 25,[28][29][30] The wall material for the encapsulation could be polymer, 29,[31][32][33] or small molecules like cholesterol accompanied with polyethylene glycol (PEG), that has been questioned due to various disadvantages, 31 while the popular capsules could be liposomes, 5,31,[34][35][36] gel 37 and micelle.…”

“…Herein, as a hydrophobic core material, ginsenoside Rg3 is selected for its various medicinal properties such as anti‐inflammatory, anti‐oxidant and anticancer effects 26 . Its clinical application is limited due to its poor water solubility, short circulating half‐life and poor specificity for tumor tissue targeting 27 . The most applied stratagem to overcome the solubility issue is encapsulation, which can improve oral bioavailability, significantly prolong pharmacodynamics and reduce drug toxicity 25,28‐30 .…”