Magnetic Fe₃ O ₄ nanoparticles grafted with single-chain antibody (scFv) and docetaxel loaded β-cyclodextrin potential for ovarian cancer dual-targeting therapy.

In order to improve the therapeutic efficiency and reduce the side effects on nonpathological cells and tissues, targeting drug delivery systems have gained more and more attraction. Here, we report a novel dual-targeting drug delivery system for ovarian cancer therapy. The inner core was made of iron oxide (Fe3O4) nanoparticles, synthesized by co-precipitation method. It was further surface-functionalized with amine groups to link single-chain antibody (scFv) and β-cyclodextrin (β-CD). Docetaxel (TXT) was finally included in the grafted β-CD. FTIR and XPS confirmed the reactions. SEM found that the diameters of these Fe3O4 nanoparticles before and after functionalization were around 40nm. Magnetization test showed that these particles were superparamagnetic. The in vitro release of TXT was concentration-driven and sustained, depending on the renewal rate of release medium. The in vitro flow chamber experiment revealed its magnetic targeting property; modified ELISA and static binding experiments displayed its good affinity to Endoglin, indicating that our drug delivery system has the potential to be dual-targeted to ovarian cancer tissue by externally applied magnetic field and native active binding of grafted scFv to Endoglin, overexpressed by ovarian cancer tissue. MTT assays showed that the TXT released from this drug delivery system continuously inhibited the growth of Skov3 ovarian cancer cells in 72h, better than the control raw TXT. All these results demonstrated a promising dual-targeting drug delivery system with great potential for ovarian cancer therapy.