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高等学校化学研究 ›› 2018, Vol. 34 ›› Issue (2): 203-211.doi: 10.1007/s40242-018-7293-0

• Articles • 上一篇    下一篇

Controlled Release of Curcumin via Folic Acid Conjugated Magnetic Drug Delivery System

SONG Shengmei, LI Minglu, GONG Xiaojuan, HAN Hui, ZHOU Yehong, WANG Li, SHUANG Shaomin, DONG Chuan   

  1. Institute of Environmental Science, Department of Chemistry and Chemical Engineering, Shanxi University, Taiyuan 030006, P. R. China
  • 收稿日期:2017-09-06 修回日期:2018-01-25 出版日期:2018-04-01 发布日期:2018-02-12
  • 通讯作者: SHUANG Shaomin,E-mail:smshuang@sxu.edu.cn E-mail:smshuang@sxu.edu.cn
  • 基金资助:
    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).

Controlled Release of Curcumin via Folic Acid Conjugated Magnetic Drug Delivery System

SONG Shengmei, LI Minglu, GONG Xiaojuan, HAN Hui, ZHOU Yehong, WANG Li, SHUANG Shaomin, DONG Chuan   

  1. Institute of Environmental Science, Department of Chemistry and Chemical Engineering, Shanxi University, Taiyuan 030006, P. R. China
  • Received:2017-09-06 Revised:2018-01-25 Online:2018-04-01 Published:2018-02-12
  • Contact: SHUANG Shaomin,E-mail:smshuang@sxu.edu.cn E-mail:smshuang@sxu.edu.cn
  • Supported by:
    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).

摘要: In the paper, folic acid(FA)-mediated and β-cyclodextrin(β-CD) derivatives functionalized magnetic Fe3O4 nanoparticles(MNPs) were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticancer 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 indicates 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.

关键词: Folic acid, β-Cyclodextrin, Anti-cancer drug, Targeted delivery, Magnetic nanoparticle

Abstract: In the paper, folic acid(FA)-mediated and β-cyclodextrin(β-CD) derivatives functionalized magnetic Fe3O4 nanoparticles(MNPs) were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticancer 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 indicates 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.

Key words: Folic acid, β-Cyclodextrin, Anti-cancer drug, Targeted delivery, Magnetic nanoparticle