Design of PEGylated Three Ligands Silica Nanoparticles for Multi-Receptor Targeting

The synthesis of silica nanoparticles (SiNPs) decorated on their surface with a range of various elements (e.g., ligands, drugs, fluorophores, vectors, etc.) in a controlled ratio remains a big challenge. We have previously developed an efficient strategy to obtain in one-step, well-defined multifun...

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Published in:Nanomaterials (Basel, Switzerland) Switzerland), 2021-01, Vol.11 (1), p.177
Main Authors: Maurel, Manon, Montheil, Titouan, Martin, Julie, Chaar, Line, Guzman-Gonzalez, Veronica, Couvet, Morgane, Jacquet, Thibault, Jia, Tao, Eymin, Beatrice, Parra, Karine, Dumy, Pascal, Martinez, Jean, Ruggiero, Florence, Vaganay, Elisabeth, Mehdi, Ahmad, Coll, Jean-Luc, Subra, Gilles
Format: Article
Language:English
Subjects:
Biocompatibility
cancer targeting
Chemical compounds
Chemical Sciences
Conjugation
Endothelial cells
Fluorescence
fluorophore
Fluorophores
In vivo methods and tests
Ligands
Material chemistry
Melanoma
Nanoparticles
NMR
Nuclear magnetic resonance
Peptides
Receptors
Silica
silica nanoparticles
Silicon dioxide
Siloxanes
silylated peptides
Sol-gel processes
sol–gel
Spheroids
surface functionalization
Surface stability
Vascular endothelial growth factor
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Summary:The synthesis of silica nanoparticles (SiNPs) decorated on their surface with a range of various elements (e.g., ligands, drugs, fluorophores, vectors, etc.) in a controlled ratio remains a big challenge. We have previously developed an efficient strategy to obtain in one-step, well-defined multifunctional fluorescent SiNPs displaying fluorophores and two peptides ligands as targeting elements, allowing selective detection of cancer cells. In this paper, we demonstrate that additional level of controlled multifunctionality can be achieved, getting even closer to the original concept of "magic bullet", using solely sol-gel chemistry to achieve conjugation of PEG chains for stealth, along with three different ligands. In addition, we have answered the recurrent question of the surface ungrafting by investigating the stability of different siloxane linkages with the ERETIC Method (Electronic Reference to Access Concentrations) by F NMR quantification. We also compared the efficiency of the hybrid silylated fluorophore covalent linkage in the core of the SiNP to conventional methods. Finally, the tumor-cell-targeting efficiency of these multi-ligand NPs on human endothelial cells (HUVEC or HDMEC) and mixed spheroids of human melanoma cells and HUVEC displaying different types of receptors were evaluated .
ISSN:2079-4991
2079-4991
DOI:10.3390/nano11010177