Silicon-containing nanoparticles (NPs) are considered promising drug carriers for targeted drug delivery. In this study, we investigated the physical and chemical properties of siliconcontaining NPs, including silica and organomodified silica NPs (SiO 2 NPs and OrSiO 2 NPs, 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 OrSiO 2 NPs, as well as new hybrid OrSiO 2 NPs with a silica core (SiO 2 + OrSiO 2 NPs). 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 OrSiO 2 NPs. In drug release kinetics studies, adenosine was immobilized on SiO 2 NPs 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 SiO 2 NP surface modification technique. Adsorption of adenosine on SiO 2 + OrSiO 2 NPs resulted in a significant attenuation of adenosine-induced hypotension and bradycardia.