Abstract
Fullerene has attracted much attention in biomedical research due to its unique physical and chemical properties. However, the hydrophobic nature of fullerene is limited to deploy in the body, given that the biofluids are mainly water. In this study, a water-soluble supramolecular nanoformulation based on a deep cavitand calixarene (SAC4A) and fullerene is developed to overcome the hydrophobicity of fullerene and is used as a potential photodynamic agent. SAC4A solubilizes fullerene very well with a simple grinding method. The significantly increased water solubility of fullerene enables efficient activation of reactive oxygen species. The host–guest strategy to solubilize fullerene can not only provide a new method to achieve water solubility but also expand the biomedical applications of fullerene.
Highlights
Fullerene has been widely used in biomedical research, acting as an antimicrobial agent (Mashino et al, 1999; Tsao et al, 2001), a human immunodeficiency virus protease inhibitor (Friedman et al, 1993), and a photosensitizer to cleave DNA (Boutorine et al, 1995; Sharma et al, 2011)
We further evaluated its ability to generate reactive oxygen species (ROS) under LED irradiation, which is significant on account of its further biomedical applications
Calixarene was employed as the macrocyclic host because of its broad chemical design space (Böhmer, 1995)
Summary
Fullerene has been widely used in biomedical research, acting as an antimicrobial agent (Mashino et al, 1999; Tsao et al, 2001), a human immunodeficiency virus protease inhibitor (Friedman et al, 1993), and a photosensitizer to cleave DNA (Boutorine et al, 1995; Sharma et al, 2011). Komatsu et al examined that the equimolar amounts of C60 and sulfonatocalix[8]arene were subjected to high-speed vibration milling treatment, and the concentration of C60 was calculated to be 1.3 × 10–4 M (Komatsu et al, 1999). These water-soluble fullerenes solubilized by macrocycles confirm the feasibility of the host–guest strategy. We further evaluated its ability to generate ROS under LED irradiation, which is significant on account of its further biomedical applications
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