In vitro and in vivo toxicity of thiolated and PEGylated organosilica nanoparticles

This study comprises the comprehensive toxicological assessment of thiolated organosilica nanoparticles (NPs) synthesised from 3-mercaptopropyltrimethoxysilane (MPTS). We investigated the influence of three different types of nanoparticles synthesised from 3-mercaptopropyltrimethoxysilane: the starting thiolated silica (Si-NP-SH) and their derivatives prepared by surface PEGylation with PEG 750 (Si-NP-PEG750) and 5000 Da (Si-NP-PEG5000) on biological subjects from in vitro to in vivo experiments to explore the possible applications of those nanoparticles in biomedical research.

As a result of this study, we generated a comprehensive understanding of the toxicological properties of these nanoparticles, including their cytotoxicity in different cell lines, hemolytic properties, in vitro localisation, mucosal irritation properties and biodistribution in BALB/c mice. Our findings indicate that all three types of nanoparticles can be considered safe and have promising prospects for use in biomedical applications. Nanoparticles did not affect the viability of HPF, MCF7, HEK293 and A549 cell lines at low concentrations (up to 100 µg/mL); moreover, they did not cause organ damage to BALB/c mice at concentrations of 10 mg/kg.

The outcomes of this study enhance our understanding of the impact of organosilica nanoparticles on health and the environment, which is vital for developing silica nanoparticle-based drug delivery systems and provides opportunities to expand the applications of organosilica nanoparticles.

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Balnur A. Zhaisanbayeva, Ellina A. Mun, Leila Ulmanova, Zarina Zhunissova, Bauyrzhan Umbayev, Farkhad Olzhayev, Ivan A. Vorobjev, Gonzalo Hortelano, Vitaliy V. Khutoryanskiy, In vitro and in vivo toxicity of thiolated and PEGylated organosilica nanoparticles, International Journal of Pharmaceutics, Volume 652, 2024, 123852, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2024.123852.

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