The fullerene family, and especially C60, has delighted the scientific community during the last 25 years
with perspective applications in a wide variety of fields, including the biological and the biomedical
domains. Several biomedical uses have been explored using water-soluble C60-derivatives. However,
the employment of fullerenes for drug delivery is still at an early stage of development. The design and
synthesis of multifunctionalized and multimodal C60 systems able to cross the cell membranes and
efficiently deliver active molecules is an attracting challenge that involves multidisciplinary strategies.
Promising results have emerged in the last years, bringing fullerenes again to the front of interest.
Herein, the state of the art of this emerging field is presented and illustrated with some of the most
representative examples.
