期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 160, 期 -, 页码 649-660出版社
ELSEVIER
DOI: 10.1016/j.colsurfb.2017.10.013
关键词
Drug-fluorophore; Antisolvent method; Theranostic prodrug nanocrystals; Cell imaging; Chemotherapy
资金
- National Nature Science Foundation of China [21502007, 31271071]
- Technology Personnel Training Project of the Xinjiang Uygur Autonomous Region of China [qn2015bs014]
- Thirteenth Five-year Key Disciplines of Xinjiang Uygur Autonomous Region (Materials Science and Engineering)
- Natural Science Foundation of Fujian Province of China [2016J01406]
As one of nanomedicine delivery systems (NDSs), drug nanocrystals exhibited an excellent anticancer effect. Recently, differences of internalization mechanisms and subcellular localization of both drug nanocrystals and small molecular free drug have drawn much attention. In this paper, paclitaxel (PTX) as a model anticancer drug was directly labeled with 4-chloro-7-nitro-1, 2, 3-benzoxadiazole (NBD-Cl) (a drug-fluorophore conjugate Ma et al. (2016) and Wang et al. (2016) [1,2] (PTX-NBD)). PTX-NBD was synthesized by nucleophilic substitution reaction of PTX with NBD-Cl in high yield and characterized by fluorescence, XRD, ESI-MS, and FT-IR analysis. Subsequently, the cube-shaped PTX-NBD nanocrystals were prepared with an antisolvent method followed by surface functionalization of SPC and MPEG-DSPE. The obtained specific shaped PTX-NBD@PC-PEG NCs had a hydrodynamic particle size of similar to 50 nm, excellent colloidal stability, and a high drug-loading content of similar to 64%. Moreover, in comparison with free PTX-NBD and the sphere-shaped PTX-NBD nanocrystals with surface functionalization of SPC and MPEG-DSPE (PTX-NBD@PC-PEG NSs), PTX-NBD@PC-PEG NCs remarkably reduced burst release and improved cellular uptake efficiency and in vitro cancer cell killing ability. In a word, the work highlights the potential of theranostic prodrug nanocrystals based on the drug-fluorophore conjugates for cell imaging and chemotherapy. (C) 2017 Elsevier B.V. All rights reserved.
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