Chapter 13 - Dendrimer–drug conjugates

Abstract

Dendrimers have been emerged as a potential carrier for therapeutic agents due to the unique properties they possess, i.e., well-defined structure, monodispersity, and pliability for surface functionalization with ligands or therapeutic molecule. Dendrimers have been explored as scaffold for delivery of therapeutic agents. The presence of functional surface groups over periphery of dendrimers has been employed for conjugating the therapeutic entities through covalent bonding to improve drug release kinetics via stimuli-responsive, controlled, and targeted release of attached therapeutic moieties. The stimuli-responsive functionality allows the release of drug in response to the specific trigger (acid, redox potentials, or enzyme) at the targeted site. For the development of dendrimer–drug conjugates (DDCs), linker chemistry plays an important role in determining the optimal drug delivery at the targeted sites by conserving efficacy of therapeutic agent and influencing desired drug release pattern. DDCs have emerged as a promising delivery system with improved drug stability during systemic circulation, better pharmacokinetic profile, and targeted drug delivery. The DDCs have received a considerable attention for the delivery of various therapeutic agents including anticancer, antiinflammatory, and antimicrobial drugs. This chapter discusses the functionalization of dendrimers with drug either directly or via different linkers and highlights the significance of chemical nature of bonds for the controlled release of the free drug at the targeted site.