Abstract Cancer is the second leading cause of death worldwide after cardiovascular disease. Depending on the type and the location of the tumor, several cancer treatments are implemented. Among these, the three most conventional therapies are surgery, radiotherapy and chemotherapy. However, there are other therapeutic approaches such as photodynamic therapy (PDT). PDT relies on the combined action of light, a photoactivable molecule called photosensitizer (PS) and molecular oxygen. Most of the PSs used for clinical applications are not cancer-cell specific. One of the solutions to overcome this problem is the use of nanoparticles (NPs) to induce a passive targeting. It is also possible to graft a vector onto the NPs to specifically target membrane receptors overexpressed in the tumor cells or neovessels surrounding the tumor. In this review, we focus on the NPs loaded with PSs and coupled to peptides for targeted PDT. We described nanosystems that targeted Neuropilin-1 (NRP-1), α_vβ₃ integrins, nucleolin membrane receptor, epidermal growth factor (EGF) receptor, protein-glutamine-gamma-glutamyltransferase (TGM2), p32, transferrin, PD-1, and mitochondrial membrane. The use of a cell absorbing-peptide is also described.