Ligand-directed reduction-sensitive shell-sheddable biodegradable micelles actively deliver doxorubicin into the nuclei of target cancer cells.
作者： Yinan Zhong , Weijing Yang , Huanli Sun , Ru Cheng , Fenghua Meng
DOI: 10.1021/BM401098W
关键词: Cancer cell 、 Intracellular 、 PEG ratio 、 Ethylene glycol 、 Ligand 、 Chemistry 、 Micelle 、 Molecular biology 、 In vitro 、 Doxorubicin 、 Biophysics
摘要: The therapeutic performance of biodegradable micellar drugs is far from optimal due to existing challenges like poor tumor cell uptake and intracellular drug release. Here, we report on ligand-directed reduction-sensitive shell-sheddable micelles based poly(ethylene glycol)-poly(e-caprolactone) (PEG-PCL) copolymer actively delivering doxorubicin (DOX) into the nuclei target cancer cells, inducing superb in vitro antitumor effects. were constructed PEG-SS-PCL galactose-PEG-PCL (Gal-PEG-PCL) block copolymers, which Gal-PEG-PCL was designed with a longer PEG than that (6.0 vs 5.0 kDa) fully expose Gal ligands onto surface for effective targeting hepatocellular carcinoma cells. combining 10 or 20 wt % formed uniform average sizes 56.1 58.2 nm (denoted as PEG-SS-PCL/Gal10 PEG-SS-PCL/Gal20, respectively). release studies showed about 81.1 75.0% DOX re...
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