Silica nanoparticles: Preparation, characterization and in vitro/in vivo biodistribution studies

• Published in: European journal of pharmaceutical sciences 2015-04, Vol.71, p.46-55
• Main Authors: Tamba, B.I., Dondas, A., Leon, M., Neagu, A.N., Dodi, G., Stefanescu, C., Tijani, A.
• Format: Article
• Language: English
• Subjects: Animals; Biodistribution; Carbocyanines - pharmacokinetics; Drug Compounding; Fluorescent; Fluorescent Dyes - pharmacokinetics; Guinea Pigs; Male; Mice; Microscopy; Nanoparticles - toxicity; Particle Size; Scintigraphy; Silica nanoparticles; Silicon Dioxide - pharmacokinetics; Silicon Dioxide - toxicity; Surface Properties; Tissue Distribution
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2015.02.002

[Display omitted] The current progress in pharmaceutical nanotechnology field has been exploited in the design of functionalized radiolabelled nanoparticles that are able to deliver radionuclides in a selective manner to improve the outcome of diagnosis and treatment. Silica nanoparticles (SNPs) have been widely developed for biomedical applications due to their high versatility, excellent functional properties and low cost production, with the possibility to control different topological parameters relevant for multidisciplinary applications. The aim of the present study was to characterize and evaluate both in vitro, by microscopy techniques, and in vivo, by scintigraphic imaging, the biodistribution of silica nanostructures derivatives (Cy5.5 conjugated SNPs and 99mTc radiolabelled SNPs) to be applied as radiotracers in biomedicine. SNPs were synthesized by hydrolysis and condensation of silicon alkoxides, followed by surface functionalization with amino groups available for fluorescent dye and radiolabelling possibility. Our data showed the particles size distribution (200–350nm), the surface charge (negative for bare and fluorescent SNPs and positive for amino SNPs), polydispersity index (broad distribution), the qualitative composition and the toxicity assessments (safe material) that made the obtained SNPs candidates for in vitro/in vivo studies. A high uptake of fluorescent SNPs in all the investigated organs was evidenced by confocal microscopy. The 99mTc radiolabelled SNPs biodistribution was quantified in the range of 12–100% counts/g organ using the scintigraphic images. The obtained results reveal improved properties, namely, reduced toxicity with a low level of side effects, an improved biodistribution, high labelling efficiency and stability of the radiolabelled SNPs with potential to be applied in biomedical science, particularly in nuclear medicine as a radiotracer.