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Acid-Active Supramolecular Anticancer Nanoparticles Based on Cyclodextrin Polyrotaxanes Damaging both Mitochondria and Nuclei of Tumor Cells

Abstract

As a supramolecular macrocyclic polymer, cyclodextrin (CD) polyrotaxanes (PRs) have many advantages for developing nanomedicines, such as stable chemical composition, abundant functionalized hydroxyl groups, getting across biological barrier, adjustable nanoparticle size and good biocompatibility. Herein, we syntheisized a class of acid-active therapeutic nanoparticles comprising a α-CD-based PRs polymeric prodrug (PR-PDOX-co-POEGMA, denoted as PRMO@DOX) to reduce drug leakage and selectively deliver drugs into tumor cells, aiming to achieve maximal treatment efficacy of supramolecular therapeutics. The obtained PRMO@DOX showed desirable features of high drug loading rate (>25 wt%), fast cellular uptake, acid-active controlled release, effective anti-tumor activity and low systemic toxicity. Benefited from the unique amphiphilic nanostructure, PRMO@DOX can form water-soluble prodrug nanoparticles in aqueous medium. The acid-active hydrazone bond in the prodrug can break and thus release drug molecules precisely and timely under acidic tumor microenvironment, damaging the nuclei and mitochondria of tumor cells. Both in vitro and in vivo experiments clearly demonstrated a remarkable antitumor efficacy of this therapeutic platform, which provided a new strategy for development of polyrotaxanes-based nanomedicine for enhanced cancer therapy.

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Publication details

The article was received on 23 Aug 2018, accepted on 06 Oct 2018 and first published on 09 Oct 2018


Article type: Paper
DOI: 10.1039/C8BM01020J
Citation: Biomater. Sci., 2018, Accepted Manuscript
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    Acid-Active Supramolecular Anticancer Nanoparticles Based on Cyclodextrin Polyrotaxanes Damaging both Mitochondria and Nuclei of Tumor Cells

    S. Bai, X. Zhang, X. Ma, J. Chen, Q. Chen, X. Shi, M. Hou, P. Xue, Y. Kang and Z. Xu, Biomater. Sci., 2018, Accepted Manuscript , DOI: 10.1039/C8BM01020J

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