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Issue 10, 2015
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A pH-activatable and aniline-substituted photosensitizer for near-infrared cancer theranostics

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Abstract

This work reports a newly designed pH-activatable and aniline-substituted aza-boron-dipyrromethene as a trifunctional photosensitizer to achieve highly selective tumor imaging, efficient photodynamic therapy (PDT) and therapeutic self-monitoring through encapsulation in a cRGD-functionalized nanomicelle. The diethylaminophenyl is introduced in to the structure for pH-activatable near-infrared fluorescence and singlet oxygen (1O2) generation, and bromophenyl is imported to increase the 1O2 generation efficiency upon pH activation by virtue of its heavy atom effect. After encapsulation, the nanoprobe can target αvβ3 integrin-rich tumor cells via cRGD and is activated by physiologically acidic pH for cancer discrimination and PDT. The fascinating advantage of the nanoprobe is near-infrared implementation beyond 800 nm, which significantly improves the imaging sensitivity and increases the penetration depth of the PDT. By monitoring the fluorescence decrease in the tumor region after PDT, the therapeutic efficacy is demonstrated in situ and in real time, which provides a valuable and convenient self-feedback function for PDT efficacy tracking. Therefore, this rationally designed and carefully engineered nanoprobe offers a new paradigm for precise tumor theranostics and may provide novel opportunities for future clinical cancer treatment.

Graphical abstract: A pH-activatable and aniline-substituted photosensitizer for near-infrared cancer theranostics

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Publication details

The article was received on 11 May 2015, accepted on 11 Jul 2015 and first published on 13 Jul 2015


Article type: Edge Article
DOI: 10.1039/C5SC01721A
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Chem. Sci., 2015,6, 5969-5977
  • Open access: Creative Commons BY license
    All publication charges for this article have been paid for by the Royal Society of Chemistry

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    A pH-activatable and aniline-substituted photosensitizer for near-infrared cancer theranostics

    J. Tian, J. Zhou, Z. Shen, L. Ding, J. Yu and H. Ju, Chem. Sci., 2015, 6, 5969
    DOI: 10.1039/C5SC01721A

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