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Open AccessArticle

Multifunctional, CD44v6-Targeted ORMOSIL Nanoparticles Enhance Drugs Toxicity in Cancer Cells

1
Dipartimento di Scienze Chimiche, Università di Padova, via Marzolo 1, 35131 Padova, Italy
2
Department of Molecular Medicine, University of Padova, via Gabelli 63, 35121 Padova, Italy
3
ICMATE-CNR, Area della Ricerca di Padova, C.so Stati Uniti 4, 35127 Padova, Italy
4
Dipartimento di Scienze Farmaceutiche, Università di Padova, Via Marzolo 5, 35131 Padova, Italy
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Nanomaterials 2020, 10(2), 298; https://doi.org/10.3390/nano10020298
Received: 27 November 2019 / Revised: 24 January 2020 / Accepted: 31 January 2020 / Published: 10 February 2020
(This article belongs to the Special Issue Application of Nanoscale Materials for Cancer Diagnostic and Therapy)
Drug-loaded, PEGylated, organic-modified silica (ORMOSIL) nanoparticles prepared by microemulsion condensation of vinyltriethoxysilane (VTES) were investigated as potential nanovectors for cancer therapy. To target cancer stem cells, anti-CD44v6 antibody and hyaluronic acid (HA) were conjugated to amine-functionalized PEGylated ORMOSIL nanoparticles through thiol-maleimide and amide coupling chemistries, respectively. Specific binding and uptake of conjugated nanoparticles were studied on cells overexpressing the CD44v6 receptor. Cytotoxicity was subsequently evaluated in the same cells after the uptake of the nanoparticles. Internalization of nanocarriers loaded with the anticancer drug 3N-cyclopropylmethyl-7-phenyl-pyrrolo- quinolinone (MG2477) into cells resulted in a substantial increase of the cytotoxicity with respect to the free formulation. Targeting with anti-CD44v6 antibodies or HA yielded nanoparticles with similar effectiveness, in their optimized formulation. View Full-Text
Keywords: silica nanoparticles; targeted delivery; CD44 receptor; hyaluronic acid; antibodies silica nanoparticles; targeted delivery; CD44 receptor; hyaluronic acid; antibodies
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Morillas-Becerril, L.; Peta, E.; Gabrielli, L.; Russo, V.; Lubian, E.; Nodari, L.; Ferlin, M.G.; Scrimin, P.; Palù, G.; Barzon, L.; Castagliuolo, I.; Mancin, F.; Trevisan, M. Multifunctional, CD44v6-Targeted ORMOSIL Nanoparticles Enhance Drugs Toxicity in Cancer Cells. Nanomaterials 2020, 10, 298.

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