Silicon-containing nanocarriers for targeted drug delivery: synthesis, physicochemical properties and acute toxicity

Abstract

Silicon-containing nanoparticles (NPs) are considered promising drug carriers for targeted drug delivery. In this study, we investigated the physical and chemical properties of silicon-containing NPs, including silica and organomodified silica NPs (SiO₂NPs and OrSiO₂NPs, respectively), with different surface modifications, with the aim of increasing drug-loading efficiency. In addition, we described the original synthesis methods of different sizes of OrSiO₂NPs, as well as new hybrid OrSiO₂NPs with a silica core (SiO₂ + OrSiO₂NPs). Animal experiments revealed that the silicon-containing NPs investigated were non-toxic, as evidenced by a lack of hemodynamic response after intravenous administration. Bioelimination studies showed rapid renal excretion of OrSiO₂NPs. In drug release kinetics studies, adenosine was immobilized on SiO₂NPs using three different approaches: physical adsorption, ionic, and covalent bonding. We observed that the rate of adenosine desorption critically depended on the type of immobilization; therefore, adenosine release kinetics can be adjusted by SiO₂NP surface modification technique. Adsorption of adenosine on SiO₂ + OrSiO₂NPs resulted in a significant attenuation of adenosine-induced hypotension and bradycardia.

• Adenosine
• bioelimination
• hybrid nanoparticle
• organomodified silica
• surface modification

Declaration of interest

The authors report that they have no conflicts of interest. This study was supported by the Russian Science Foundation (Project 14-15-00473).