Recent advances in natural small molecules as drug delivery systems.

Drug delivery systems (DDSs) are a multidisciplinary approach toward the effective delivery of drugs to their target sites. Natural small molecule (NSM) compounds with anticancer activity, self-assembly and co-assembly functions show great potential for application as novel DDSs in the biomedical field. NSMs are widely sourced, have many modification sites, and readily form hydrogen bonds, π-π interactions, van der Waals interactions, and other non-covalent bonds in solvents, resulting in ordered structures. Moreover, their good biocompatibility and bioactivity allow compositions based on these compounds to be used in life science applications such as tissue engineering, drug delivery and cell imaging, showing the potential medical value of NSMs as DDSs. In this review, we summarise the role, assembly principles and applications of natural products such as triterpenoids, diterpenoids, sterols, alkaloids and polysaccharides in the construction of small molecule systems, which are expected to provide an important reference for the development of more active natural nanomaterials and the study of single or multi-component interactions.