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Issue 36, 2018
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Self-assembly of folic acid dextran conjugates for cancer chemotherapy

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Folic acid (FA) has long been used as a specific targeting agent since many cancer cells overexpress folate receptors (FRs). Herein, novel functionalities of FA will be explored: directed self-assembly of nanoparticles for drug delivery together with pH responsive release. By conjugating with dextran (DEX), DEX-FA exerts a pH dependent self-assembly behavior: it self-associates into nanoparticles (NPs) around physiological pH (pH 7) and disassembles at higher pH (pH > 9). Doxorubicin (DOX), a model antitumor drug, has been successfully encapsulated via electrostatic interactions between DOX and FA. Moreover, the pH responsive release behaviors of DOX are controlled by FA. The DOX@DEX-FA NPs exhibit typical FA-FRs-mediated endocytosis in vitro and targeted delivery in vivo, altogether contributing to an enhanced antitumor efficacy, alleviated side effects, and elongated overall survival in a 4T1 subcutaneous tumor-bearing mouse model. The DOX@DEX-FA NPs have been demonstrated to be a simple, safe and efficient nanoplatform, holding significant translation potential for treating FR-overexpressing cancers. This study may present novel functionalities of FA in cancer-targeted nanotherapeutics.

Graphical abstract: Self-assembly of folic acid dextran conjugates for cancer chemotherapy

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Supplementary files

Article information

08 Jun 2018
19 Aug 2018
First published
24 Aug 2018

Nanoscale, 2018,10, 17265-17274
Article type

Self-assembly of folic acid dextran conjugates for cancer chemotherapy

Y. Tang, Y. Li, R. Xu, S. Li, H. Hu, C. Xiao, H. Wu, L. Zhu, J. Ming, Z. Chu, H. Xu, X. Yang and Z. Li, Nanoscale, 2018, 10, 17265
DOI: 10.1039/C8NR04657C

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