Block copolymer prodrugs: Synthesis, self‐assembly, and applications for cancer therapy

Block copolymer prodrugs (BCPs) have emerged as one of the most promising anticancer drug delivery strategies, which can self-assemble into nanoparticles with optimal physicochemical properties including sizes, morphologies, surface properties, and integration of multifunction for improved in vivo applications. Moreover, the utility of stimuli-responsive linkages to conjugate drugs onto the polymer backbones can achieve efficient and targeting drug release. Several BCP micellar delivery systems have been pushed ahead into the clinical trials, which showed great promising potentials for cancer therapy. In recent years, various novel and more efficient BCP systems have been developed for better in vivo performance. In this focus article, we focus on the recent advances of BCPs including the synthesis, self-assembly, and applications for cancer therapy. The synthetic methods are first introduced, and the self-assembly of BCPs for in vivo anticancer applications is discussed along the line of varying endogenous stimuli-responsive linkages including amide or ester bonds, pH, reduction, and oxidation-responsive linkages. Finally, conclusions along with the brief future perspectives are presented. This article is categorized under: Therapeutic Approaches and Drug Discovery > Nanomedicine for Oncologic Disease Nanotechnology Approaches to Biology > Nanoscale Systems in Biology.