Anticancer efficacy of photodynamic therapy with hematoporphyrin-modified, doxorubicin-loaded nanoparticles in liver cancer

• We developed novel nanoparticles (HP-NPs) to improve the therapeutic effect of PDT.
• The in vitro phototoxicity was enhanced in HP-NPs compared with free HP.
• The in vivo anticancer efficacy was markedly improved by HP-NPs-based PDT.
• HP-NPs represent a potentially effective co-delivery system of HP and DOX.

Photodynamic therapy (PDT) in combination with chemotherapy has great potential for cancer treatment. However, there have been very few attempts to developing cancer-targeted co-delivered systems of photosensitizers and anticancer drugs.We developed hematoporphyrin (HP)-modified doxorubicin (DOX)-loaded nanoparticles (HP-NPs) to improve the therapeutic effect of PDT in treating liver cancer.HP is not only a ligand for low density lipoprotein (LDL) receptors on the hepatoma cells but also a well-known photosensitizer for PDT. In vitro phototoxicity in HepG2 (human hepatocellular carcinoma) cells and in vivo anticancer efficacy in HepG2 tumor-bearing mice of free HP and HP-NPs were evaluated.The in vitro phototoxicity in HepG2 cells determined by MTT assay, annexin V-FITC staining and FACS analysis was enhanced in HP-NPs compared with free HP. Furthermore, compared with free HP-based PDT, in vivo anticancer efficacy in HepG2 tumor-bearing mice was markedly improved by HP-NPs-based PDT. Moreover, in both cases, the therapeutic effect was increased according to the irradiation time and number of PDT sessions.In conclusion, the HP-NPs prepared in this study represent a potentially effective co-delivery system of photosensitizer (HP) and anticancer drug (DOX) which improved the effects of PDT in liver cancer.