Folate-conjugated pH-responsive nanocarrier designed for active tumor targeting and controlled release of doxorubicin

doi:10.1007/s11706-017-0401-0

Frontiers of Materials Science

2017, Vol. 11

Issue (4): 328-343 https://doi.org/10.1007/s11706-017-0401-0

本期目录

Folate-conjugated pH-responsive nanocarrier designed for active tumor targeting and controlled release of doxorubicin

Lulu WEI¹, Beibei LU¹, Lin CUI², Xueying PENG¹, Jianning WU¹, Deqiang LI³, Zhiyong LIU¹(

), Xuhong GUO^1,⁴

¹. School of Chemistry & Chemical Engineering, Shihezi University/Key Laboratory of Green Processing for Chemical Engineering/Key Laboratory of Materials-Oriented Chemical Engineering of Xinjiang Uygur Autonomous Region/Engineering Research Center of Materials-Oriented Chemical Engineering of Xinjiang Bingtuan, Shihezi 832003, China
². School of Medicine, Shihezi University, Shihezi 832003, China
³. College of Chemistry and Chemical Engineering, Xinjiang Agricultural University, Urumqi 830001, China
⁴. State Key Laboratory of Chemical Engineering, East China University of Science and Technology, Shanghai 200237, China

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Abstract：

A novel type of amphiphilic pH-responsive folate-poly(ε-caprolactone)-block-poly(2-hydroxyethylmethacrylate)-co-poly(2-(dimethylamino)-ethylmethacrylate) (FA-PCL-b-P(HEMA-co-DMAEMA)) (MFP) block copolymers were designed and synthesized via atom transfer radical polymerization (ATRP) and ring opening polymerization (ROP) techniques. The molecular structures of the copolymers were confirmed with¹H NMR, FTIR and GPC measurements. The critical micelle concentration (CMC) of MFP in aqueous solution was extremely low (about 6.54 mg/L). Thein vitro release behavior of DOX-loaded micelles was significantly accelerated when the pH value of solution decreased from 7.4 to 5.0. In vitro antitumor efficiency was evaluated by incubating DOX- loaded micelles with Hela cells. The results demonstrated that this copolymer possessed excellent biocompatibility, and FA-decorated micelles MFP showed higher cellular uptake than those micelles without the FA moiety, indicating their unique targetability. These folate-conjugated biodegradable micelles are highly promising for targeted cancer chemothe-rapy.

Key words： amphiphilic polymer pH-sensitive active targeting drug delivery system folic acid

收稿日期: 2017-07-16 出版日期: 2017-11-29

Corresponding Author(s): Zhiyong LIU

引用本文:

. [J]. Frontiers of Materials Science, 2017, 11(4): 328-343.
Lulu WEI, Beibei LU, Lin CUI, Xueying PENG, Jianning WU, Deqiang LI, Zhiyong LIU, Xuhong GUO. Folate-conjugated pH-responsive nanocarrier designed for active tumor targeting and controlled release of doxorubicin. Front. Mater. Sci., 2017, 11(4): 328-343.

链接本文:

https://academic.hep.com.cn/foms/CN/10.1007/s11706-017-0401-0
https://academic.hep.com.cn/foms/CN/Y2017/V11/I4/328

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