Advances in antitumor nanomedicine based on functional metal–organic frameworks beyond drug carriers

Nanoscale metal-organic frameworks (MOFs) have attracted widespread interest due to their unique properties including a tunable porous structure, high drug loading capacity, structural diversity, and outstanding biocompatibility. MOFs have been extensively explored as drug nanocarriers in biotherapeutics. However, by harnessing the functionality of ligands and metal ions or clusters in MOFs, the applications of MOFs can be extended beyond drug delivery vehicles. Based on the intrinsic properties of the components of MOFs (e.g. magnetic moments of metal ions and fluorescence of ligands), different imaging modes can be achieved with varied MOFs. With careful design of the composition of MOFs (e.g. modification of organic linkers), they can respond to tumor microenvironments to realize on-demand treatment. By incorporating porphyrin-based ligands (photosensitizers for photodynamic therapy) or high-Z metal ions (radiosensitizers for radiotherapy) into the scaffold of MOFs, MOFs themselves can act as anticancer therapeutic agents. In this review, we highlight the application of MOFs from the above-mentioned aspects and discuss the prospects and challenges for using MOFs in stimuli-responsive imaging-guided antitumor therapy.