Self‐Assembled Peptide‐Based Nanodrugs: Molecular Design, Synthesis, Functionalization, and Targeted Tumor Bioimaging and Biotherapy

Functional nanomaterials as nanodrugs based on the self-assembly of inorganics, polymers, and biomolecules have showed wide applications in biomedicine and tissue engineering. Ascribing to the unique biological, chemical, and physical properties of peptide molecules, peptide is used as an excellent precursor material for the synthesis of functional nanodrugs for highly effective cancer therapy. Herein, recent progress on the design, synthesis, functional regulation, and cancer bioimaging and biotherapy of peptide-based nanodrugs is summarized. For this aim, first molecular design and controllable synthesis of peptide nanodrugs with 0D to 3D structures are presented, and then the functional customization strategies for peptide nanodrugs are presented. Then, the applications of peptide-based nanodrugs in bioimaging, chemotherapy, photothermal therapy (PTT), and photodynamic therapy (PDT) are demonstrated and discussed in detail. Furthermore, peptide-based drugs in preclinical, clinical trials, and approved are briefly described. Finally, the challenges and potential solutions are pointed out on addressing the questions of this promising research topic. This comprehensive review can guide the motif design and functional regulation of peptide nanomaterials for facile synthesis of nanodrugs, and further promote their practical applications for diagnostics and therapy of diseases.