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iRGD-decorated reduction-responsive nanoclusters for targeted drug delivery

Abstract

Herein, reduction-responsive disintegratable nanoclusters (NCs) were prepared as a novel nanovehicle for targeted drug delivery. The NCs, with diameter of ~170 nm, were self-assembled from hydrophobically modified and iRGD decorated hydroxyethyl starch (iRGD-HES-SS-C18). DOX was loaded into the NCs as a model drug. DOX@iRGD-HES-SS-C18 NCs can disintegrate into smaller ones and release DOX under reduction stimuli. Due to the ligand-receptor binding interactions between iRGD and integrin αV, DOX@iRGD-HES-SS-C18 NCs can specifically bind to the cell membranes of HepG-2 and 4T1 cells (integrin αV positive), resulting in enhanced cellular uptake as compared to DOX@HES-SS-C18 NCs. After cellular internalization, the NCs were transported to endosomes/lysosomes in where the reductive environment triggered the disintegration and DOX release. As a consequence, DOX@iRGD-HES-SS-C18 NCs exhibited enhanced antitumor effect as compared to DOX@HES-SS-C18 NCs and free DOX, in in vitro antitumor activity study. The reduction-responsive disintegratable NCs reported here were proved to be a safe and efficient nanoplatform, holding significant translation potential for tumor-targeted drug delivery.

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Supplementary files

Publication details

The article was received on 28 Mar 2018, accepted on 03 May 2018 and first published on 04 May 2018


Article type: Paper
DOI: 10.1039/C8NR02534G
Citation: Nanoscale, 2018, Accepted Manuscript
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    iRGD-decorated reduction-responsive nanoclusters for targeted drug delivery

    H. Hu, J. Wan, X. Huang, Y. Tang, C. Xiao, H. Xu, X. Yang and Z. Li, Nanoscale, 2018, Accepted Manuscript , DOI: 10.1039/C8NR02534G

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