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Hydrophobized SN38 to Redox-hypersensitive Nanorods for Cancer Therapy


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 deliver. The hydrophobized SN38 was synthesized by conjugating SN38 with oleic acid using the linker of disulfanyl-ethyl carbonate. Interestingly, the resulting prodrug could self-assemble into nanorods with high drug loading capacity (45 %) and colloidal stability. Moreover, these nanorods displayed an impressively high redox-sensitivity to release SN38: 100 % SN38 within 1 h in the 10 mM DTT versus 1 % in the 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 a potent antitumor activity in CT26 colorectal cancer xenograft. The nanoaggregates of such redox-hypersensitive hydrophobized SN38 represent an alternatively effective strategy for developing novel SN38 nanomedicines.

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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, 2018, Accepted Manuscript
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    Hydrophobized SN38 to Redox-hypersensitive Nanorods for Cancer Therapy

    Y. Zheng, Y. Xueling, Y. Wang, D. Xin, X. Wang, C. Chen, D. Tian, Z. Luo, Z. Zhang and Y. C. Zeng, J. Mater. Chem. B, 2018, Accepted Manuscript , DOI: 10.1039/C8TB02319K

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