<p>Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo</p>

Abstract

Background and purpose Ginsenoside Rg5 (Rg5), a triterpene saponin, extracted from the natural herbal plant ginseng, is one of the most potent anticancer drugs against various carcinoma cells. However, the therapeutic potential of Rg5 is limited by its low solubility in water, poor bioavailability, and nontargeted delivery. Therefore, we prepared folic acid (FA)-modified bovine serum albumin (BSA) nanoparticles (FA-Rg5-BSA NPs) to improve the therapeutic efficacy and tumor targetability of Rg5. Methods Various aspects of the FA-Rg5-BSA NPs were characterized, including size, polydispersity, zeta potential, morphology, entrapment efficiency (EE), drug loading (DL), in vitro drug release, thermal stability, in vitro cytotoxicity, cell apoptosis, cellular uptake, in vivo antitumor effects and in vivo biodistribution imaging. Results The FA-Rg5-BSA NPs showed a particle size of 201.4 nm with a polydispersity index of 0.081, uniform spherical shape, and drug loading of 12.64±4.02%. The aqueous solution of FA-Rg5-BSA NPs had favorable stability for 8 weeks at 4°C. The FA-Rg5-BSA NPs dissolved under acidic conditions. Moreover, the Rg5-BSA NPs and FA-Rg5-BSA NPs had advanced anticancer activity compared with Rg5 in MCF-7 cells, while poor cytotoxicity was observed in L929 cells. The FA-Rg5-BSA NPs facilitated cellular uptake and induced apoptosis in MCF-7 cells. In addition, in an MCF-7 xenograft mouse model, the in vivo antitumor evaluation revealed that FA-Rg5-BSA NPs were more effective in inhibiting tumor growth than Rg5 and Rg5-BSA NPs. The in vivo real-time bioimaging study showed that the FA-Rg5-BSA NPs exhibited superior tumor accumulation ability. Conclusion The results suggested that FA-Rg5-BSA NPs could serve as a promising system to improve the antitumor effect of Rg5.

Pharmacological activities of ginsenoside Rg5 (Review)

“…This in vivo real-time bioimaging study demonstrated that the FA-Rg5-BSA NPs had an advanced ability to accumulate in tumors. These results indicated that FA-Rg5-BSA NPs has the potential to serve as an attractive therapeutic strategy for the management of cancer ( 32 ).…”

“…With the development of nanomedicine, the antitumor effects of Rg5 through biocompatible nanoscale drug delivery systems has also been investigated ( 32 ). Dong et al ( 32 ) used folic acid (FA)-modified bovine serum albumin (BSA) nanoparticles (FA-Rg5-BSA NPs) as carriers to entrap Rg5. It was discovered that the FA-Rg5-BSA NPs exhibited superior anticancer activity compared with Rg5 in MCF-7 cells with low cytotoxicity to L929 cells.…”

Inhibitory Effect of pH-Responsive Nanogel Encapsulating Ginsenoside CK against Lung Cancer

“…The concentration of CK in the CMC-β-CD Ngs was determined using high performance liquid chromatography (HPLC; Agilent 1260 Infinity) [ 23 ]. The lyophilized samples were accurately weighed and dissolved in acetonitrile, sonicated for 30 min, filtered with a 0.45 μm membrane filter, and analysed by HPLC.…”

Ginsenosides emerging as both bifunctional drugs and nanocarriers for enhanced antitumor therapies

“…The EPR effect and receptor-mediated targeting were the main reasons for MCF-7 cell apoptosis. Furthermore, Rg5 released from FA-modified targeted NPs were efficiently accumulated within 8 h at the tumor site in a MCF-7 xenograft mouse model [ 118 ] (Fig. 8 ).…”