health concerns across the world. [1] Particularly significant is the effort directed toward the treatment of cancer, which has remained as one of the leading causes of rapidly growing morbidity and mortality rates for centuries. Among a number of significant advances achieved in this domain, cancer theranostics is one such advancement that allows the ingenious integration of accurate diagnosis with therapeutic intervention in a single formulation within spatial colocalization. This phenomenon has captivated the interest of researchers for the evaluation of the potential in fundamental studies and clinical application, [2] primarily due to the attribution of various intrinsic advantages to theranostics, including maximized therapeutic efficacy, optimized drug safety, and improved pharmacokinetics. [3] Notably, in comparison with the conventional therapeutic methods for cancers such as surgical removal, chemotherapy, and radiotherapy, [4] theranostics involves some burgeoning therapeutic strategies including photothermal therapy (PTT), [5] photodynamic therapy (PDT), [6] and gene therapy. It has become one of the most intensive areas of research during recent years due to high efficiency, minimal side effects, excellent tumor suppression, and non-invasive conversion. One of the major pursuits of biomedical science is to develop advanced strategies for theranostics, which is expected to be an effective approach for achieving the transition from conventional medicine to precision medicine. Supramolecular assembly can serve as a powerful tool in the development of nanotheranostics with accurate imaging of tumors and real-time monitoring of the therapeutic process upon the incorporation of aggregation-induced emission (AIE) ability. AIE luminogens (AIEgens) will not only enable fluorescence imaging but will also aid in improving the efficacy of therapies. Furthermore, the fluorescent signals and therapeutic performance of these nanomaterials can be manipulated precisely owing to the reversible and stimuli-responsive characteristics of the supramolecular systems. Inspired by rapid advances in this field, recent research conducted on nanotheranostics with the AIE effect based on supramolecular assembly is summarized. Here, three representative strategies for supramolecular nanomaterials are presented as follows: a) supramolecular self-assembly of AIEgens, b) the loading of AIEgens within nanocarriers with supramolecular assembly, and c) supramolecular macrocycle-guided assembly via host-guest interactions. Meanwhile, the diverse applications of such nanomaterials in diagnostics and therapeutics have also been discussed in detail. Finally, the challenges of this field are listed in this review.
