期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 129, 期 -, 页码 63-70出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2015.03.028
关键词
Self-assembled nanoparticles; Phytosterol; Folate receptor; Anticancer drug; Targeted delivery
资金
- Opening Project of Hubei Key Laboratory of Lipid Chemistry and Nutrition, Oil Crops Research Institute Chinese Academy of Agricultural Science
- Key Laboratory of Bioresource Protection and Utilization of Anhui Province
- Key Laboratory of Biotic Environment and Ecological Safety of Anhui Province
- Program for Innovative Research Team at Anhui Normal University
- Independent Research Foundation of Anhui Province Key Laboratory of Biological Macromolecules Research [LAB201401, LAB201403]
Self-assembled core/shell nanoparticles (NPs) were synthesized from water-soluble alginate substituted by hydrophobic phytosterols. Folate, a cancer-cell-specific ligand, was conjugated to the phytosterol-alginate (PA) NPs for targeting folate-receptor-overexpressing cancer cells. The physicochemical properties of folate-phytosterol-alginate (FPA) NPs were characterized by nuclear magnetic resonance, transmission electron microscopy, dynamic light scattering, electrophoretic light scattering, and fluorescence spectroscopy. Doxorubicin (DOX), an anticancer drug, was entrapped inside prepared NPs by dialysis method. The identification of prepared FPA NPs to folate-receptor-overexpressing cancer cells (KB cells) was confirmed by cytotoxicity and folate competition assays. Compared to the pure DOX and DOX/PA NPs, the DOX/FPA NPs had lower IC50 value to KB cells because of folate-receptor-mediated endocytosis process and the cytotoxicity of DOX/FPA NPs to KB cells could be competitively inhibited by free folate. The cellular uptake and internalization of pure DOX and DOX/FPA NPs was confirmed by confocal laser scanning microscopy image and the higher intracellular uptake of drug for DOX/FPA NPs over pure DOX was observed. The FPA NPs had the potential as a promising carrier to target drugs to cancer cells overexpressing folate receptors and avoid cytotoxicity to normal tissues. (C) 2015 Elsevier BAT. All rights reserved.
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