Anti-hepatoma activity of targeted pluronic f127/formononetin nanocomposite system in vitro / 中国组织工程研究

ABSTRACT

BACKGROUND: Natural flavonoid formononetin (FN) is traditional Chinese medicine extract and has anticancer effect, but the hydrophobic structure and short half-life in vivo limit their clinical applications. OBJECTIVE: To prepare FN loaded pluronic (PF)-folic acid (FA) conjugated micelles (FN-PF-FA) and to test in vitro drug release and anticancer activity. METHODS: FA coupling PF was prepared by carbodiimide crosslinker chemical method. FN-PF-FA micelles were prepared by film hydration method. The encapsulation efficiency, drug loading and drug release performance of FN-PF and FN-PF-FA micelles were measured. The in vitro anti-cancer activity of flavin, FN-PF micelles, and FN-PF-FA micelles on folic acid-overexpressing human liver cancer HepG2 cells was measured by in vitro thiohodamine B experiment. RESULTS AND CONCLUSION: (1) The encapsulation efficiency of FN-PF and FN-PF-FA micelles was (84.12±2.15)% and (82.50±1.78)%, respectively, and the drug loading was (21.33±2.27)% and (19.73±1.58)%, respectively. (2) The release rate of both micelles in acidic environment was faster than that in alkaline environment. In the same condition, the release rate of FN-PF-FA micelles was slower than that of FN-PF micelles. (3) At the same drug concentration, the ability of FN-PF micelles and FN-PF-FA micelles to inhibit the proliferation of human liver cancer HepG2 cells was stronger than that of free FN (P < 0.05). Moreover, the inhibitory effect of FN-PF-FA micelles was stronger than that of FN-PF micelles (P < 0.05). (4) The order of drug concentration required to inhibit tumors was FN-PF-FA < FN-PF < free FN, and there was a significant difference between groups (P < 0.01). (5) Results suggested that FN-PF-FA micelles had the potential to target the release of anticancer drugs.