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Hydrophobized SN38 to redox-hypersensitive nanorods for cancer therapy

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Abstract

The clinical application of SN38 (7-ethyl-10-hydroxy-camptothecin) is severely restricted by its extremely low water solubility. Nanoaggregates formed by amphiphilic SN38 prodrugs have been widely used for the delivery of SN38. In this study, we used a hydrophobized SN38 prodrug, rather than a typical SN38 amphiphile, to construct rod-shaped nanoaggregates for efficient SN38 delivery. The hydrophobized SN38 was synthesized by conjugating SN38 with oleic acid using disulfanyl-ethyl carbonate as the linker. Interestingly, the resulting prodrug self-assembled into nanorods with high drug loading capacity (45%) and colloidal stability. Moreover, these nanorods displayed an impressively high redox-sensitivity to release 100% SN38 within 1 h in 10 mM DTT, versus 1% in phosphate buffer (pH 7.4). The efficient drug release resulted in an uncompromised in vitro cytotoxicity, which was comparable to free SN38 and nearly 93-fold more potent than CPT-11. Most importantly, these novel prodrug nanoaggregates exhibited potent antitumor activity in the CT26 colorectal cancer xenograft. The nanoaggregates of such redox-hypersensitive hydrophobized SN38 represent an effective alternative strategy for developing novel SN38 nanomedicines.

Graphical abstract: Hydrophobized SN38 to redox-hypersensitive nanorods for cancer therapy

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Publication details

The article was received on 03 Sep 2018, accepted on 26 Nov 2018 and first published on 28 Nov 2018


Article type: Paper
DOI: 10.1039/C8TB02319K
Citation: J. Mater. Chem. B, 2019, Advance Article
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    Hydrophobized SN38 to redox-hypersensitive nanorods for cancer therapy

    Y. Zheng, X. Yan, Y. Wang, X. Duan, X. Wang, C. Chen, D. Tian, Z. Luo, Z. Zhang and Y. Zeng, J. Mater. Chem. B, 2019, Advance Article , DOI: 10.1039/C8TB02319K

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