期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 105, 期 5, 页码 1741-1750出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2016.02.021
关键词
cancer chemotherapy; drug delivery system; encapsulation; nanoparticle; PLGA; polymeric drug delivery systems; targeted drug delivery
资金
- Iran National Science Foundation [9000719]
- Mashhad University of Medical Sciences [901051, 930872]
Molecularly targeted drug delivery systems represent a novel therapeutic strategy in the treatment of different cancers. In the present study, we have developed gemcitabine (GEM)-loaded AS1411 aptamer surface-decorated polyethylene glycol-poly(lactic-co-glycolic acid) nanopolymersome (Apt-GEM-NP) to target nucleolin-overexpressing non-small cell lung cancer (NSCLC; A549). The prepared Apt-GEM-NP showed average particle size of 128 +/- 5.23 nm and spherical morphology with encapsulation efficiency and loading content of 95.32 +/- 2.37% and 8.61 +/- 0.27%, respectively. Apt-GEM-NP exhibited a controlled release pattern. A sustained release of drug in physiological conditions will greatly improve the chemotherapeutic efficiency of a system. Enhanced cellular uptake and the cytotoxicity of aptamer-conjugated nanoparticles (NPs) in A549 cancer cells obviously verified nucleolin-mediated receptor-based active targeting. Nucleolin-mediated internalization of the targeted polymeric NP was further confirmed by flow cytometry and fluorescence microscopy. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay clearly showed the enhanced cell proliferation inhibitory effect of AS1411-conjugated NP on account of the selective delivery of GEM to the nucleolin-overexpressing cancer cells. Our results showed that AS1411 aptamer conjugation on the surface of NP could be a potential treatment strategy for A549 as a nucleolin-overexpressing cell line. This suggests that AS1411-GEM-NPs could be potentially used for the treatment of NSCLC. (C) 2016 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
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