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Issue 20, 2017
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Cellular uptake of pH/reduction responsive phosphorylcholine micelles

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Abstract

Phosphorylcholine micelles based on pH/reduction responsive copolymers, poly(ε-caprolactone)-ss-b-poly((N,N-diethylaminoethyl methacrylate)-r-poly(2-methacryloyloxyethyl phosphorylcholine)) (PCL-ss-PDEAPMPC) were developed for the intracellular delivery of doxorubicin. The micelles were spherical (less than 90 nm in diameter) and demonstrated pH/reduction sensitivity. The DOX loaded micelles presented the fastest drug release under simultaneously acidic and reductive conditions. Although PCL20-ss-PDEA5PMPC10 had lower pH sensitivity than PCL20-ss-PDEA15PMPC10, the DOX loaded micelles of the former released the drug faster than the latter at pH 5.0 and in the presence of a reductant. The cytotoxicities of the blank micelles and the drug-loaded micelles were investigated using the human cervical cancer cell line (HeLa). The IC50 (half maximal inhibitory concentration) of PCL20-ss-PDEA5PMPC10 micelles was the lowest among PCL-ss-PDEAPMPC micelles. The results of CLSM and flow cytometry showed that the micelles effectively delivered the drug cargo into cancer cells. The cellular uptake pathways of PCL-ss-PDEAPMPC micelles were mainly clathrin-mediated endocytosis, and accompanied by a certain degree of giant pinocytosis.

Graphical abstract: Cellular uptake of pH/reduction responsive phosphorylcholine micelles

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Publication details

The article was received on 10 Jul 2017, accepted on 29 Aug 2017 and first published on 29 Aug 2017


Article type: Paper
DOI: 10.1039/C7NJ02484C
Citation: New J. Chem., 2017,41, 11828-11838
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    Cellular uptake of pH/reduction responsive phosphorylcholine micelles

    Y. Cai, S. Li, M. Cai, Y. Chen and X. Luo, New J. Chem., 2017, 41, 11828
    DOI: 10.1039/C7NJ02484C

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