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pH-sensitive micelle with mitochondria-targeted and aggregation-induced emission characterization: synthesis, cytotoxicity and biological applications

Abstract

Subcellular organelle-specific reagents for simultaneous tumor targeting, imaging, and treatment are of enormous interest in cancer therapy. Herein, we present a mitochondria targeting micelle (PEG-AIE-TPP) by conjugating a triphenylphosphonium (TPP) with a fluorogen which can undergo aggregation-induced emission (AIE). At first, the in vitro and in vivo properties of PEG-AIE-TPP micelle were characterized in detail. It was found that the micelle was reasonably stable at physiologic pH and high sensitive to mildly acidic pH stimulus. Importantly, this micelle could selectively localize and accumulate in the mitochondrial, then generating an aggregation-induced emission (AIE) effect confirmed by the green fluorescence. Additionally, the micelle exhibited selective cytotoxicity to cancer cells while negligible toxicity to normal cells in vitro. The in vivo imaging and ex vivo imaging results showed that accumulation tendency of the micelle at the tumor region was obvious. We also further proved the biocompatible, tumor targeting ability and antitumor activity of PEG-AIE-TPP micelle in MCF-7 tumor-bearing mice. Accordingly, this mitochondria-targeted therapeutic micelle with good stability, biocompatible, tumor-targeting and antitumor activity provides a potentially unique tumor-targeted system for cancer therapy.

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Publication details

The article was received on 28 Jul 2018, accepted on 09 Sep 2018 and first published on 11 Sep 2018


Article type: Paper
DOI: 10.1039/C8BM00889B
Citation: Biomater. Sci., 2018, Accepted Manuscript
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    pH-sensitive micelle with mitochondria-targeted and aggregation-induced emission characterization: synthesis, cytotoxicity and biological applications

    J. Li, Y. Liu, H. Li, W. Shi, X. Bi, Q. Qiu, B. Zhang, W. Huang and H. Qian, Biomater. Sci., 2018, Accepted Manuscript , DOI: 10.1039/C8BM00889B

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