Effect of PEGylation on the biological properties of cationic carbosilane dendronized gold nanoparticles

[Display omitted] •Heterofunctionalized gold nanoparticles (AuNP) are easily obtained in a one pot reaction.•Dendron/PEG ratio and dendron generation are very relevant for biological properties of AuNP.•The exposure of cationic charge of dendrons and of PEG ligands depends on their relative sizes.•T...

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Veröffentlicht in:International journal of pharmaceutics 2020-01, Vol.573, p.118867-118867, Article 118867
Hauptverfasser: Barrios-Gumiel, Andrea, Sánchez-Nieves, Javier, Pedziwiatr-Werbicka, Elzbieta, Abashkin, Viktar, Shcharbina, Natallia, Shcharbin, Dzmitry, Glińska, Sława, Ciepluch, Karol, Kuc-Ciepluch, Dorota, Lach, Dominika, Bryszewska, Maria, Gómez, Rafael, de la Mata, F. Javier
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Sprache:eng
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Zusammenfassung:[Display omitted] •Heterofunctionalized gold nanoparticles (AuNP) are easily obtained in a one pot reaction.•Dendron/PEG ratio and dendron generation are very relevant for biological properties of AuNP.•The exposure of cationic charge of dendrons and of PEG ligands depends on their relative sizes.•The presence of PEG reduces toxicity but favour recognition by anti-PEG antibodies. Heterofunctionalized gold nanoparticles (AuNPs) were obtained in a one pot reaction of gold precursor with cationic carbosilane dendrons (first to third generations, 1-3G) and (polyethylene)glycol (PEG) ligands in the presence of a reducing agent. The final dendron/PEG proportion on AuNPs depends on the initial dendron/PEG ratio (3/1, 1/1, 1/3) and dendron generation. AuNPs were characterized by transmission electron microscopy (TEM), dynamic light scattering (DLS), ultraviolet spectroscopy (UV–VIS), thermogravimetric analysis (TGA), nuclear magnetic resonance (1H NMR) and zeta potential (ZP). Several assays have been carried out to determine the relevance of PEG/dendron ratio and dendron generation in the biomedical properties of PEGylated AuNPs and the results have been compared with those obtained for non-PEGylated AuNPs. Finally, analyses of PEG recognition by anti-PEG antibodies were carried out. In general, haemolysis, platelet aggregation and toxicity were reduced after PEGylation of AuNPs, the effect being dependent on dendron generation and dendron/PEG ratio. Dendron generation determines the exposure of PEG ligand and the interaction of this ligand with AuNPs environment. On the other hand, increasing PEG proportion diminishes toxicity but also favors interaction with antibodies.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2019.118867