A methodology to enhance biological delivery of photosensitizers by incorporating them into nanomaterials has been developed. In order to prepare photosensitizer nanoconjugates as biocompatible and selective probes, initially, bioconjugatable porphyrinic photosensitizers were prepared through rational routes. The porphyrins with carboxyl groups (as conjugatable handles) were successfully attached on the surface of the bioinspired nanoparticles (through a stable ester bond formation) affording hydrophilic and biocompatible nanophotosensitizers. The loading efficiency of the photosensitizer into nanomaterials was found to be 12–16%. Given their biocompatibility and efficient loading on nanoparticles, the photosensitizers prepared in this study could find use in photodynamic therapy and dual photodynamic–photothermal therapy.