Anthracyclines are a clinically important class of antineoplastic agents used to treat a wide variety of solid and blood cancers. The first described anthracycline, daunorubicin, was first isolated from a strain of Streptomyces peucetius in the early 1960s. Clinically the most widely used are doxorubicin, daunorubicin and their semi-synthetic derivatives epirubicin and idarubicin. They primarily act by intercalating with DNA and inhibiting topoisomerase II, resulting in DNA breaks and abrogated DNA synthesis. The most serious side effect of anthracycline use is cumulative dose-dependent cardiotoxicity, limiting recommended maximum lifetime treatment to 400-450 mg/m2. Several liposomal formulations of doxorubicin are in use, having the benefits of prolonging retention rate while reducing peak plasma concentration of free drug. Several clinical trials of anthracycline-loaded nanoparticles are currently underway.