Anthracycline cytostatics can be observed at the level of organelles, cells and whole organisms due to their fluorescent properties. Imaging techniques based on detection of fluorescence can be used not only for observation of drug interaction with tumor cells, but also for targeting therapy of tumors with nanoparticles containing anthracycline cytostatics. Doxorubicin and daunorubicin, enclosed in liposomes, as representatives of nanoparticles suitable for targeted therapy, are used in clinical practice. The main advantage of liposomal drugs is to reduce the side effects due to differences in pharmacokinetics and distribution of the drug in the body. Due to the fact that all biological mechanisms of action of anthracycline drugs are not still fully understood, modern imaging techniques offer tool for in vivo studies of these mechanisms.