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Issue 10, 2018
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Ratiometric real-time monitoring of hydroxyapatite–doxorubicin nanotheranostic agents for on-demand tumor targeted chemotherapy

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Abstract

We reported dual-fluorescent hydroxyapatite–doxorubicin (DOX) (DDHAP) nanocomposites for tumor-targeted therapy. A newly designed fluorescent tumor-targeting group, DFA1, is grafted onto the nanoparticle surface, which can enhance the cellular uptake of DDHAP by binding to γ-glutamyl transpeptidase (GGT), a cell surface-associated enzyme that is overexpressed on cancer cell membranes. This DFA1 moiety could undergo fluorescence quenching after binding to GGT, and the whole nanocomposite collapsed under the cancerous pH condition, thereby releasing the free fluorescent DOX as an effective anticancer drug. Thus, ratiometric fluorescence tracking can be built up by measuring the DOX/DFA1 fluorescence ratio. The dual fluorescence for ratiometric real-time tracking of the nanotherapeutic agents provides a new platform for better understanding the detailed process of their cellular uptake and intracellular dissociation. Moreover, as confirmed by in vivo studies, hydroxyapatite–DOX nanotheranostic agents demonstrate specific tumor-targeting, efficient tumor tissue penetrating and excellent tumor inhibiting effects. Nanotheranostic agents based on DDHAP show high potential for effective cancer treatment in future clinical settings.

Graphical abstract: Ratiometric real-time monitoring of hydroxyapatite–doxorubicin nanotheranostic agents for on-demand tumor targeted chemotherapy

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Publication details

The article was received on 07 May 2018, accepted on 25 Jun 2018 and first published on 29 Jun 2018


Article type: Research Article
DOI: 10.1039/C8QM00215K
Citation: Mater. Chem. Front., 2018,2, 1791-1798

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    Ratiometric real-time monitoring of hydroxyapatite–doxorubicin nanotheranostic agents for on-demand tumor targeted chemotherapy

    Y. Kang, W. Sun, J. Fan, Z. Wei, S. Wang, M. Li, Z. Zhang, Y. Xie, J. Du and X. Peng, Mater. Chem. Front., 2018, 2, 1791
    DOI: 10.1039/C8QM00215K

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