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Targeted delivery of anticancer agents by functional nanoparticles is an attractive strategy to increase their therapeutic efficacy while reducing toxicity. In this work, doxorubicin (DOX)-loaded mesoporous silica nanoparticles (MSNs) were modified with aptamer (Ap) against the epithelial cell adhesion molecule (EpCAM) for targeted delivery of DOX to colon cancer cells. These nanoparticles (Ap-MSN-DOX) were characterized by particle size, zeta potential, aptamer conjugation efficiency, drug encapsulation efficiency, and drug release properties. The in vitro cell recognition, cellular uptake, EpCAM protein inhibition efficiency, and cytotoxicity of Ap-MSN-DOX were also studied. Results demonstrated that EpCAM conjugation increased binding of Ap-MSN-DOX to EpCAM over-expressing SW620 colon cancer cells but not EpCAM-negative Ramos cells, resulting in enhanced cellular uptake and increased cytotoxicity of the DOX in SW620 cells when compared to non-Ap-modified nanoparticles (MSN-DOX). Additionally, Ap-MSN-DOX exhibited significant inhibition effects on the expression of EpCAM on SW620 cells. These results suggested that Ap-MSN-DOX has the potential for the targeted delivery of therapeutic agents into EpCAM positive colon cancer cells to improve therapeutic index while reducing side effects. (C) 2015 Elsevier B.V. All rights reserved.
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
ISSN: 0928-0987
Year: 2016
Volume: 83
Page: 28-35
3 . 7 5 6
JCR@2016
4 . 3 0 0
JCR@2023
ESI Discipline: PHARMACOLOGY & TOXICOLOGY;
ESI HC Threshold:180
JCR Journal Grade:1
CAS Journal Grade:2
Cited Count:
WoS CC Cited Count: 143
SCOPUS Cited Count: 155
ESI Highly Cited Papers on the List: 11 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 3
Affiliated Colleges: