Fullerenes in vivo. Toxicity and protective effects

The data available in the literature on the toxicity of fullerenes are numerous but contradictory. The ambiguity of research results hinders the transition from scientific research to real-world drug development. The ability of fullerenes to accumulate in some organs and tissues is interpreted in most cases as their disadvantage, while a number of studies have shown that there is no relationship between the accumulation of fullerenes and toxic effects. Moreover, fullerenes often exert potent protective effects. The pharmacokinetics and toxicity of fullerenes depend on the route of administration and are closely related to their functionalization, since pristine fullerenes are generally harmless. These factors, as well as the risk-benefit ratio, need to be considered when developing fullerene-based drugs. In this review, open-source data on in vivo toxicity, biodistribution, metabolism, and some protective properties of both native fullerene and a number of its derivatives are collected and analyzed. The problems and prospects for using fullerenes through various methods of delivery to the body, such as through the gastrointestinal tract, intravenous administration, intraperitoneal administration, dermal application or respiratory exposure are described.