Lactose-conjugated porphyrin: synthesis and photobiological evaluation as potential agents for photodynamic therapy

Porphyrin-based photosensitizers are conventional photodynamic agents that are used clinically. However, their clinical applications have been overshadowed by poor water solubility. In addition, they have weak tumor selectivity, which may cause undesirable side effects. The preparation of novel porphyrin derivatives has been explored for potential applications in photodynamic therapy (PDT). To achieve this goal, lactose-conjugated porphyrin nanoparticles (Lac-Por NPs) have been synthesized and characterized. PDT with Lac-Por NPs exhibited tumor-specific cytotoxicity in lactose receptor-overexpressing HepG2 cells in vitro and in vivo. In summary, we designed and synthesized lactose conjugate porphyrins with enhanced water solubility and tumor selectivity. This work expands the application range of porphyrin-based photosensitizers for cancer treatment.