In Vitro and In Vivo Evaluation of Hydrophilic C60(OH)10/2-Hydroxypropyl-β-cyclodextrin Nanoparticles as an Antioxidant.

The objective of this study was to assess the antioxidant ability of C60(OH)10/2-hydroxypropyl-β-cyclodextrin (HP-β-CD) nanoparticles, by comparing their scavenging ability for reactive nitrogen species, their cytoprotective effects under conditions of oxidative stress, and their therapeutic effects against diseases that are induced by oxidative stress. The C60(OH)10/HP-β-CD nanoparticles had a higher scavenging activity against nitric acid and peroxynitrite (ONOO(-)) than the other antioxidants such as ascorbic acid, trolox, and edaravone. The cytoprotective effect of C60(OH)10/HP-β-CD nanoparticles was examined on HeLa and HepG2 cells by monitoring the percentage of cell death induced by H2O2. Treatment with C60(OH)10/HP-β-CD nanoparticles resulted in an increase in cell viability, due to the suppression of the oxidative stress. Furthermore, the nanoparticles had a high cytoprotective effect, compared with other polyhydroxylated C60 (C60(OH)24 and C60(OH)40). The C60(OH)10/HP-β-CD nanoparticles were intravenously administered to mice with a liver injury induced by an over dose of acetaminophen. Levels of alanine transaminase and aspartate transaminase were essentially the same as those of normal mice and the survival rate was also prolonged by the intravenous administration of the C60(OH)10/HP-β-CD nanoparticles. The results indicate that C60(OH)10/HP-β-CD nanoparticles are a promising antioxidant for use in the treatment of diseases caused by oxidative stresses.