Biocompatibility of thermally hydrocarbonized porous silicon nanoparticles and their biodistribution in rats.
Porous silicon (PSi) particles have been studied for the effects they elicit in Caco-2 and RAW 264.7 macrophage cells in terms of toxicity, oxidative stress, and inflammatory response. The most suitable particles were then functionalized with a novel (18)F label to assess their biodistribution after enteral and parenteral administration in a rat model. The results show that thermally hydrocarbonized porous silicon (THCPSi) nanoparticles did not induce any significant toxicity, oxidative stress, or inflammatory response in Caco-2 and RAW 264.7 macrophage cells. Fluorescently labeled nanoparticles were associated with the cells surface but were not extensively internalized. Biodistribution studies in rats using novel (18)F-labeled THCPSi nanoparticles demonstrated that the particles passed intact through the gastrointestinal tract after oral administration and were also not absorbed from a subcutaneous deposit. After intravenous administration, the particles were found mainly in the liver and spleen, indicating rapid removal from the circulation. Overall, these silicon-based nanosystems exhibit excellent in vivo stability, low cytotoxicity, and nonimmunogenic profiles, ideal for oral drug delivery purposes.
Division of Pharmaceutical Technology, Faculty of Pharmacy, University of Helsinki, FI-00014 Finland.
Luis M
LM
Bimbo
Mirkka
M
Sarparanta
Hélder A
HA
Santos
Anu J
AJ
Airaksinen
Ermei
E
Mäkilä
Timo
T
Laaksonen
Leena
L
Peltonen
Vesa-Pekka
VP
Lehto
Jouni
J
Hirvonen
Jarno
J
Salonen
D000284:Administration, Oral; D000818:Animals; D004058:Diffusion; D006358:Hot Temperature; D006838:Hydrocarbons / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D009928:Organ Specificity; D016062:Porosity; D051381:Rats; D017208:Rats, Wistar; D012825:Silicon / Q000008:administration & dosage* / Q000737:chemistry*; D014018:Tissue Distribution
D006838:Hydrocarbons; D012825:Silicon