Hyperbranched polymers (HBPs) have shown widespread academic and commercial success in the preparation of films and novel materials, and now are emerging into the biomedical research space as nanocarriers for use in drug delivery and diagnostics. HBPs exhibit ideal sizes for delivery in vivo, have well‐established chemistries for their synthesis, as well as offering multiple methods of incorporation of a variety of targeting, therapeutic, and diagnostic moieties. By choice of material and functionality, their biostability or biodegradability can be fine‐tuned for multistaged or time‐delayed release of therapeutics. With significant advances in the development of nanomedicines, in particular chemistries surrounding biomolecule conjugation and the evolution of imaging techniques, the multimodal capabilities of HBPs combined with facile and controlled synthetic engineering of HBPs have resulted in properties that are ideal for their application as nanocarriers. While HBP nanocarriers offer limitless synthetic opportunity, to address the many biological challenges that are now well‐established in nanotherapeutics, new approaches to how HBPs are designed are required. This overview aims to address the points that must be considered in the biologically driven nanomaterial design of HBP nanocarriers.