- The impact of porous silicon nanoparticles on human cytochrome P450 metabolism in human liver microsomes in vitro.
The impact of porous silicon nanoparticles on human cytochrome P450 metabolism in human liver microsomes in vitro.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences (2017-04-04)
Elisa Ollikainen, Dongfei Liu, Arttu Kallio, Ermei Mäkilä, Hongbo Zhang, Jarno Salonen, Hélder A Santos, Tiina M Sikanen
PMID28366651
ABSTRACT
Engineered nanoparticles are increasingly used as drug carriers in pharmaceutical formulations. This study focuses on the hitherto unaddressed impact of porous silicon (PSi) nanoparticles on human cytochrome P450 (CYP) metabolism, which is the major detoxification route of most pharmaceuticals and other xenobiotics. Three different surface chemistries, including thermally carbonized PSi (TCPSi), aminopropylsilane-modified TCPSi (APTES-TCPSi) and alkyne-terminated thermally hydrocarbonized PSi (Alkyne-THCPSi), were compared for their effects on the enzyme kinetics of the major CYP isoforms (CYP1A2, CYP2A6, CYP2D6, and CYP3A4) in human liver microsomes (HLM) in vitro. The enzyme kinetic parameters, K
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