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Issue 8, 2019
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Acidity-triggered zwitterionic prodrug nano-carriers with AIE properties and amplification of oxidative stress for mitochondria-targeted cancer theranostics

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Abstract

Although biodegradable polymer–drug conjugate delivery systems exhibit great promise toward many types of cancers, several challenges still remain, associated with specific targeting of organelles as well as real-time tracking and observing. Herein, an innovative pH-responsive zwitterionic prodrug is prepared that can easily self-assemble into stable micelles with high drug loading. This new nanocarrier is composed of the following vital factors: (i) a zwitterionic outer shell to prolong the blood circulation and aggregate at the tumor site; (ii) surface-encoded triphenyl-phosphonium groups to enhance organelle targeting; (iii) ketal bonds of nanomicelles to realize the controlled release of therapeutic molecules; (iv) aggregation-induced emission (AIE) luminogen tetraphenylethene (TPE) to realize labelling and real-time monitoring of the mitochondria in living cells. This targeted pH-responsive polyprodrug can effectively release therapeutic molecules to activate the generation of the local ROS level and enable real-time monitoring of the status of mitochondria, which presents a practicable strategy for simultaneous cancer diagnostics and therapeutics.

Graphical abstract: Acidity-triggered zwitterionic prodrug nano-carriers with AIE properties and amplification of oxidative stress for mitochondria-targeted cancer theranostics

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Publication details

The article was received on 25 Oct 2018, accepted on 11 Jan 2019 and first published on 11 Jan 2019


Article type: Paper
DOI: 10.1039/C8PY01518J
Citation: Polym. Chem., 2019,10, 983-990

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    Acidity-triggered zwitterionic prodrug nano-carriers with AIE properties and amplification of oxidative stress for mitochondria-targeted cancer theranostics

    J. Xu, B. Yan, X. Du, J. Xiong, M. Zhou, H. Wang and Z. Du, Polym. Chem., 2019, 10, 983
    DOI: 10.1039/C8PY01518J

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