Preparation of ROS-responsive core crosslinked polycarbonate micelles with thioketal linkage

[Display omitted] •ROS-responsive core crosslinked micelles were conveniently prepared.•The obtained CCL/TK micelles exhibited good biocompatibility and low toxicity.•DOX-loaded CCL/TK micelles had higher toxicity effects for HeLa and MCF-7 cells. Herein, we prepared novel reactive oxygen species (R...

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Veröffentlicht in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2020-11, Vol.195, p.111276, Article 111276
Hauptverfasser: Wang, Deqi, Wang, Song, Xia, Yingchun, Liu, Simeng, Jia, Ruixin, Xu, Gege, Zhan, Junjie, Lu, Yanbing
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Sprache:eng
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Zusammenfassung:[Display omitted] •ROS-responsive core crosslinked micelles were conveniently prepared.•The obtained CCL/TK micelles exhibited good biocompatibility and low toxicity.•DOX-loaded CCL/TK micelles had higher toxicity effects for HeLa and MCF-7 cells. Herein, we prepared novel reactive oxygen species (ROS) responsive core crosslinked (CCL/TK) polycarbonate micelles conveniently by click reaction between amphiphilic diblock copolymer poly(ethylene glycol)-poly(5-methyl-5-propargylxycar-bonyl-1,3-dioxane-2-one) (PEG-PMPC) with pendant alkynyl group and thioketal containing azide derivative bis (2-azidoethyl) 3, 3′- (propane-2, 2-diylbis (sulfanediyl)) dipropanoate (TK-N3). The CCL/TK micelles were obtained with small size of 146.4 nm, showing excellent stability against dilution and high doxorubicin (DOX) loading. In vitro toxicity tests demonstrated that the obtained CCL/TK micelles have good biocompatibility and low toxicity with cell viability above 95 %. Furthermore, DOX-loaded CCL/TK micelles showed significantly superior toxicity with IC50 values for HeLa and MCF-7 cells about 3.74 μg/mL and 3.91 μg/mL, respectively. Confocal laser scanning microscope (CLSM) and flow cytometry showed excellent internalization efficiency and intracellular drug release of DOX-loaded CCL/TK micelles. The obtained ROS-responsive CCL/TK micelles showed great potential for anticancer drug delivery.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2020.111276