RESUMO
Objective: To investigate the anticancer activity of the novel lactosyl-norcantharidin nanoparticles (Lac-NCTD-NPs) in vivo and in vitro. Methods: The MTT method was used to study the cytotoxic effects of Lac-NCTD and Lac-NCTD-NPs on HepG2, SMMC-7721, and SGC-7901 cell lines for 12 and 48 h, respectively, and the inhibitory effects of Gal-FBS; Lac-NCTD accumulated in SMMC-7721 cells was assayed by HPLC; The in vivo anticancer activity was evaluated by the tumor-growth inhibition in H22 tumor bearing mice. Results: The in vitro studies showed that the cytotoxic effects of Lac-NCTD-NPs against HepG2 and SMMC-7721 cells were the most powerful, as well as the IC 50 was the lowest, then Lac-NCTD, and they were inhibited remarkably by Gal-FBS; As for SGC-7901 cell line, the cytotoxic effects of Lac-NCTD-NPs and Lac-NCTD were not stronger than that of NCTD, and Gal-FBS had no influence on them at all; The amount of Lac-NCTD accumulated in SMMC-7721 cells was 3. 89 μg (7.02×10-3 μmol, 1×106 cell) after treatment for 12 h; The results of the antitumor activity in vivo suggested that the inhibitory rate of Lac-NCTD-NPs on tumor weight was 63.9%, which was significantly higher than that of NCTD and Lac-NCTD groups at the same molar concentration. Conclusion: The tumor-growth is inhibited effectively by Lac-NCTD-NPs which may be a kind of novel liver-targeting agents and could strongly inhibit the tumor-growth.