前药
阿霉素
药物输送
化学
PEG比率
细胞内
肿瘤微环境
药品
荧光寿命成像显微镜
生物物理学
化疗
荧光
药理学
癌症研究
生物化学
肿瘤细胞
医学
有机化学
经济
外科
物理
生物
量子力学
财务
作者
Mingliang Pei,Guoping Li,Kangwei Ma,Jianan Li,Yuanfan Wang,Peng Liu
标识
DOI:10.1016/j.colsurfb.2019.02.002
摘要
Theranostic nanoplatforms have been recognized for imaging-guided diagnosis and chemotherapy of cancer by integrating imaging function into the drug delivery systems (DDSs). Here, a facile approach was developed for the fabrication of polymeric prodrug microspheres by introducing pH sensitive "off-on" fluorochrome Rhodamine 6G into bioreducible cleavable bisulfide crosslinked PEGylated poly(glycidyl methacrylate) (PEG-PGMA) microspheres, followed with chemical conjugation of doxorubicin (DOX) via an acid-labile hydrazone linkage. High drug content of 25.4% was achieved for the final PEG-PGMA-Hy-DOX prodrug microspheres with average hydrodynamic diameter of 332 nm. The in vitro controlled release showed leakage-free in physiological medium but a sustained drug release up to 58% within 56 h in tumor intracellular microenvironment. The cellular experiments showed that the PEG-PGMA-Hy-DOX prodrug microspheres could be effectively internalized into HepG2 cells with enhanced anti-tumor efficacy than the free DOX. Furthermore, they showed fluorescence only in tumor intracellular microenvironment, indicating their promising potential for precise imaging-guided diagnosis and chemotherapy.
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