期刊
ACS APPLIED MATERIALS & INTERFACES
卷 7, 期 3, 页码 2104-2115出版社
AMER CHEMICAL SOC
DOI: 10.1021/am508291k
关键词
theranostic; near-infrared (NIR); amphiphilic copolymer; fluorescence; pH responsive
资金
- National Basic Research Program of China [2011CB921403]
- National Natural Science Foundation of China [51373162]
Theranostic polymeric nanomaterials are of special important in cancer treatment. Here, novel galactose targeted pH-responsive amphiphilic multiblock copolymer conjugated with both drug and near-infrared fluorescence (NIR) probe has been designed and prepared by a four-steps process: (1) ring-opening polymerization (ROP) of N-carboxy anhydride (NCA) monomers using propargylamine as initiator; (2) reversible additionfragmentation chain transfer (RAFT) polymerization of oligo(ethylene glycol) methacrylate (OEGMA) and gal monomer by an azido modified RAFT agent; (3) combing the obtained two polymeric segments by click reaction; (4) NIR copolymer prodrug was synthesized by chemical linkage of both cyanine dye and anticancer drug doxorubicin to the block copolymer via amide bond and hydrazone, respectively. The obtained NIRF copolymers were characterized by nuclear magnetic resonance (NMR), gel permeation chromatography (GPC), and its was measured by means of micelles dynamic light scattering (DLS), field emission transmission electron microscopy (FETEM), and UVvis and fluorescence spectrophotometry. The prodrug has strong fluorescence in the near-infrared region, and a pH sensitive drug release was confirmed at pH of 5.4 via an in vitro drug release experiment. Confocal laser scanning microscopy (CLSM) and flow cytometry experiments of the prodrug on both HepG(2) and NIH3T3 cells reveal that the galactose targeted polymeric prodrug shows a fast and enhanced endocytosis due to the specific interaction for HepG(2) cells, indicating the as-prepared polymer is a candidate for theranosis of liver cancer.
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