Doxorubicin (DOX) is one of the most commonly used chemotherapeutic agents for treating human cancer. However, its clinical use has been limited by DOX-induced cardiotoxicity as well as other side effects. In the present study, we designed and synthesized the fullerenol (FU)-DOX conjugates and folic acid (FA)-grafted FU-DOX conjugates for improving the selectivity and activity of DOX in cancer cells. We further characterized the physicochemical properties and examined the release kinetics, cellular uptake, and in vitro anticancer activities of FU-DOX and FA-FU-DOX. The results showed that FU-DOX and FA-FU-DOX had a mean diameter of
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