摘要
In the paper, folic acid（FA）-mediated and β-cyclodextrin（β-CD） derivatives ftmctionalized magnetic Fe3O4 nanoparticles（MNPs） were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticaneer drug. FA-sulfobutyl ether-β-CD-MNPs（FA-SBE-β-CD-MNPs）, FA-hydroxypropyl- β-CD-MNPs（FA-HP-β-CD-MNPs） and FA-carboxymethyl-β-CD-MNPs（FA-CM-β-CD-MNPs） were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE-β-CD-MNPs, 9.6 mg/g, 81.63% for FA-HP-β-CD-MNPs and 7.88 mg/g, 85,28% for FA-CM-β-CD-MNPs, respectively. Meanwhile, at pH：5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE-β-CD-MNPs in 5 h. Cellular uptake in- dicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE-β-CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE-β-CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.
In the paper, folic acid（FA）-mediated and β-cyclodextrin（β-CD） derivatives ftmctionalized magnetic Fe3O4 nanoparticles（MNPs） were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticaneer drug. FA-sulfobutyl ether-β-CD-MNPs（FA-SBE-β-CD-MNPs）, FA-hydroxypropyl- β-CD-MNPs（FA-HP-β-CD-MNPs） and FA-carboxymethyl-β-CD-MNPs（FA-CM-β-CD-MNPs） were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE-β-CD-MNPs, 9.6 mg/g, 81.63% for FA-HP-β-CD-MNPs and 7.88 mg/g, 85,28% for FA-CM-β-CD-MNPs, respectively. Meanwhile, at pH：5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE-β-CD-MNPs in 5 h. Cellular uptake in- dicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE-β-CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE-β-CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.
基金
Supported by the National Natural Science Foundation for the Youth, China（No.21205076） and the Applied Basic Research Project of Shanxi Province, China（No.201601D102017）.
