Ginsenoside Rg3 liposomes regulate tumor microenvironment for the treatment of triple negative breast cancer

To improve the solubility and targeting of Ginsenoside Rg3 (G-Rg3), in the current study, we constructed a novel targeting functional material folic acid -poly(2-ethyl-2-oxazoline)-cholesteryl methyl carbonate (FA-PEOz-CHMC, FPC) modified G-Rg3 liposomes (FPC-Rg3-L).

FPC was synthesized by using folic acid (FA) as a targeted head coupling with acid-activated poly(2-ethyl-2-oxazoline)-cholesteryl methyl carbonate. The inhibitory effects of the G-Rg3 preparations on mouse breast cancer cells (4T1) were investigated by CCK-8 assay. Paraffin sections of female BALB/c mice viscera were taken for hematoxylin-eosin (H&E) staining after continuous tail vein injection of G-Rg3 preparations. BALB/c mice bearing triple-negative breast cancer (TNBC) were used as animal models to investigate the inhibition of G-Rg3 preparations on tumor growth and improving quality of life. Transforming growth factor-β1 (TGF-β1) and α-smooth muscular actin (α-SMA) were used to investigate the expression of two fibrosis factors in tumor tissues by western blotting.

Compared with G-Rg3 solution (Rg3-S) and Rg3-L, FPC-Rg3-L had a significant inhibitory effect on 4T1 cells (p < .01), and the half maximal inhibitory concentration (IC₅₀) of FPC-Rg3-L was significantly lower (p < .01). The H&E results showed that the injection of FPC-Rg3-L and Rg3-S did not cause damage to the organs of mice. Compared with the control group, tumor growth was significantly inhibited in mice treated with FPC-Rg3-L and G-Rg3 solutions (p < .01).

This study presents a new and safe treatment for TNBC, reduces the toxic and side effects of the drug, and provides a reference for the efficient use of Chinese herbal medicine components.