Abstract Some nanotherapeutics based on cyclodextrin polymers are currently undergoing clinical trials. In light of this interest, we synthesized new linear polymers based on ?-cyclodextrins containing targeting units, such as biotin or arginine, to explore the advantage of functionalization for drug delivery. The polymers increased doxorubicin solubility. Furthermore, they slightly enhanced doxorubicin cytotoxicity in A2780 cells. In particular, the polymer containing arginine moieties was the most effective system by increasing doxorubicin cytotoxicity by 50%.