The structure and bioactivity of Ginkgo biloba leaves polyprenol (GBP) are similar to that of dolichol which widely exists in human and mammalian organs. GBP possesses potential pharmacological activities against cancer. This study involved oil-in-water type nanoemulsion (NE) loading GBP was prepared by dissolving polyprenol in nanoemulsion of sodium tripolyphosphate (TPP)/TiO2 solution, Triton X-100, and 1-octanol by inversed-phase emulsification (EIP) and ultrasonic emulsification (UE) method. Folic acid (FA)-coupled chitosan (CS) nanoparticles (NPs), GBP-FA-CS-NPs and GBP-TiO2-FA-CS-NPs, were fabricated by ionic cross-linking of positively charged FA-CS conjugates and negatively charged nanoemulsion with TPP/TiO2. And characterizations of them were investigated by TEM, SEM, FTIR, particle size, and zeta potential. The cytotoxic and genotoxic effects of GBP-TiO2-FA-CS-NP treatment were higher than GBP-NE, GBP-FA-CS-NPs, TiO2-NE, GBP-TiO2-NE, TiO2-FA-CS-NPs, and GBP-TiO2-FA-CS-NP treatment at the same tested concentrations in HepG2 cells. GBP-TiO2-FA-CS-NPs at low TiO2 concentration (from 1 to 2.5 μg/ml) showed good inhibition capacity on HepG2 cells and low cytotoxic and genotoxic effects on HL-7702 cells. The possible mechanism of cytotoxicity on GBP-TiO2-FA-CS-NPs against HepG2 cells is by preventing excessive intracellular Ca2+ into extracellular spaces via inhibiting Ca2+-ATPase and Ca2+/Mg2+-ATPase.
Keywords: Cytotoxicity; Genotoxicity; Nanoemulsion; Nanoparticles; Polyprenol; TiO2.