Nanomaterials (Feb 2020)

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

  • Lucía Morillas-Becerril,
  • Elektra Peta,
  • Luca Gabrielli,
  • Venera Russo,
  • Elisa Lubian,
  • Luca Nodari,
  • Maria Grazia Ferlin,
  • Paolo Scrimin,
  • Giorgio Palù,
  • Luisa Barzon,
  • Ignazio Castagliuolo,
  • Fabrizio Mancin,
  • Marta Trevisan

DOI
https://doi.org/10.3390/nano10020298
Journal volume & issue
Vol. 10, no. 2
p. 298

Abstract

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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.

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