A targeted self-assembling photosensitizer nanofiber constructed by multicomponent coordination.

Employing a peptide-based supramolecular photosensitizer nanofiber that combines the flexibility of a self-assembling short peptide and high spatiotemporal precision is a promising approach in photodynamic therapy (PDT). Herein, we developed a versatile multicomponent and multifunctional coordination self-assembling photosensitizer nanofiber based on the combination of a diphenylalanine (FF) short peptide, cell penetrating peptide 44 (CPP44) and 5-(4-aminophenyl)-10,15,20-triphenyl porphine (TPP-NH2), resulting in CPP44-FF-TPP-NH2 nanofibers (CFTNFs). Transmission electron microscopy observations showed the filamentous morphology of CFTNFs. Compared with free TPP-NH2, CFTNFs exhibited a higher cell uptake ability in HepG2 cells and a better tumor targeting ability in in vivo experiments. Furthermore, CFTNFs induced apoptosis and necrosis of more HepG2 cells in vitro and showed higher tumor growth inhibitory activity in vivo. In summary, these results indicated that CFTNFs could lead to greatly enhanced photodynamic treatment efficacy. Moreover, our study provides new opportunities for the development of peptide-based multicomponent coordination self-assembling photosensitizer nanofibers to enhance tumor-specific delivery and the anticancer efficiency.