Folic acid and deoxycholic acid derivative modified Fe 3 O 4 nanoparticles for efficient pH-dependent drug release and multi-targeting against liver cancer cells.

The novel nano-drug carrier (FDCA-FA-MNPs) was constructed by grafting formyl deoxycholic acid (FDCA) and folic acid (FA) on the surface of Fe 3 O 4 magnetic nanoparticles (MNPs), possessing the advantages of superparamagnetism, good stability, low cytotoxicity and good blood compatibility. The hydrophobic anti-cancer drug doxorubicin hydrochloride (DOX) was successfully loaded onto FDCA-FA-MNPs through supramolecular interactions (hydrogen bond between FDCA and drug and hydrophobic interaction and π-π stacking between drug and drug). The drug loading amount and drug loading capacity were 509.1 mg g -1 and 33.73 wt%, respectively. In addition, drug release had a pH responsive and controllable release performance, the release rate at pH 5.3 (45.6%) was four times that at pH 7.4 (11.5%), and the tumor microenvironment was favorable for drug release. More importantly, the novel nano-drug carrier combined the hepatocellular targeting of FDCA, the cancer cell targeting of FA, and the magnetic targeting of Fe 3 O 4 , showing excellent cancer-killing efficiency (78%) in vitro . Therefore, the nano-drug carrier synthesized in this paper has potential practical application value in the targeted therapy of liver cancer.