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A hyperbranched amphiphilic acetal polymer for pH-sensitive drug delivery

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Abstract

Nanoparticles are appealing drug delivery systems since they promise prolonged circulation time and predictable release behaviors. The current work reports a novel hyperbranched amphiphilic block copolymer synthesized using deactivation-enhanced atom transfer radical polymerization (DE-ATRP) for smart drug delivery. PEG2000-Br was applied as a macroinitiator to initiate acid-cleavable divinyl (ACD) monomers linked by acetal groups, formulating the hydrophilic (PEG) and hydrophobic (ACD) segments. The polymer appeared to self-assemble into micelles with diameters in the range of 70–100 nm, and was examined for the controlled release of doxorubicin (DOX). Results showed that DOX-loaded micelles (∼90 nm) could achieve drug loading as high as 8.2 wt%, with interesting pH-dependent release behaviors. Studies with flow cytometry (FCM) and confocal laser scanning microscopy (CLSM) showed that DOX-loaded micelles exhibited a high cellular uptake performance by HeLa cells, which indicated promising anti-tumor efficacy for such a drug delivery system. Additionally, such DOX-loaded micelles exhibited remarkable cytotoxicity against HeLa cells in a dose- and time-dependent manner due to the enhanced cell uptake behavior of micelles. These results indicated that the polymeric micelles might be used as a promising candidate for a pH-responsive drug delivery for cancer therapy.

Graphical abstract: A hyperbranched amphiphilic acetal polymer for pH-sensitive drug delivery

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Publication details

The article was received on 16 Oct 2017, accepted on 24 Nov 2017 and first published on 24 Nov 2017


Article type: Paper
DOI: 10.1039/C7PY01739A
Citation: Polym. Chem., 2018, Advance Article
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    A hyperbranched amphiphilic acetal polymer for pH-sensitive drug delivery

    H. Cao, C. Chen, D. Xie, X. Chen, P. Wang, Y. Wang, H. Song and W. Wang, Polym. Chem., 2018, Advance Article , DOI: 10.1039/C7PY01739A

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