ABSTRACT

This chapter reviews the design, synthesis and potential of polymer-drug conjugates in development of efficient anticancer drugs. It discusses structures and strategies used for design and synthesis of polymer prodrugs, conjugates of synthetic polymers and in most cases anticancer drugs as well as an impact of the conjugate structure on their biological behavior, in particular anticancer activity. Biodegradable or nondegradable polymers and copolymers can be employed in the synthesis of a variety of polymer-drug conjugates. The importance of poly(ethylene glycol)s (PEG) in synthesis of therapeutically utilizable polymer-protein conjugates can be demonstrated by a number of conjugates already introduced into clinical practice or undergoing advanced stages of clinical evaluation. One of the most frequently studied drugs conjugated with PEG has been the anticancer drug doxorubicin. The conjugates demonstrated superior contrast enhancement in heart, blood vessels and liver as compared with low-molecular-weight control agent, but only with small enhancement in muscle.