Many therapeutic and diagnostic agents suffer from short circulation times or poor selectivity resulting in the need for frequent drug administration and adverse side‐effects. On this basis, selective nanocarriers have been used to address most of the drawbacks via the encapsulation or conjugation of therapeutic and diagnostic agents to allow the targeted release of cargo to diseased sites or tumours, while maintaining low levels of cytotoxicity. Saccharides, which can be classified as monosaccharides, disaccharides and oligo/polysaccharides, have demonstrated great potential in the construction of nanocarriers, as well as the targeted guidance of the nanocarriers to diseased tissues. The fabrication of nanocarriers from natural materials such as polysaccharides affords biodegradability and biocompatibility, and in some instances confers targeting capabilities. The most recent progress in saccharide‐based targeted nanocarriers fabricated via facile one‐pot routes or complex two‐pot synthetic routes is reviewed here, with a particular focus on the high efficiency and flexibility of the one‐pot approach. In addition, inspired by the self‐assembly processes involving saccharides that occur in living organisms, particular emphasis is placed on disease‐targeting nanocarriers that are constructed from or modified by saccharides. © 2018 Society of Chemical Industry