Malignant cancer remains the leading cause of mortality globally, and advancements in nanotechnology-driven nanomedicine are expected to yield promising alternative therapeutic strategies. Dendrimers, as synthetic polymers, possess a broad potential for biomedical applications. In this respect, self-assembling dendrimer nanoparticles derived from amphiphilic dendrimers represent a promising platform for drug delivery in cancer therapy. This potential stems from precise structural characteristics, ease of synthesis, cooperative multivalency, and adaptable assembly behavior. These nanoparticles can encapsulate therapeutic agents, enhance selective accumulation in tumor tissues, facilitate deep penetration, and enable stimulus-responsive drug release, thereby improving therapeutic efficacy while minimizing side effects. In this review, we briefly introduce the self-organizing strategies of self-assembling dendrimers and present representative examples of their applications in cancer chemotherapy, gene therapy, and combination therapy. We also discuss future perspectives for self-assembling dendrimers in personalized and effective cancer nanomedicine. Our goal is to provide valuable insights and inspire further development of self-assembling dendrimers for precision oncology. [Databases searched: Web of Science, PubMed, and Google Scholar; Inclusive dates: 2011-2025].
Keywords: Self-assembling; amphiphilic dendrimer; cancer therapy; nanomedicine; on-demand delivery.