Photodynamic therapy (PDT) has a successful track record in cancer. . Urea is a naturally occurring metabolite in the human body. Some studies have shown that it can inhibit the proliferation of tumor cells and cause oxidative stress. In order to explore the application of urea in enhancing the PDT effect, we synthesized a new photosensitizer (BODIPY-I-35) with good phototherapeutic effect and encapsulated it in liposomes. Compared with free BODIPY-I-35, water-soluble nanoliposomes (LipoBOD) produced a huge redshift (> 122 nm) of fluorescence emission in solution. When LipoBOD was irradiated with 808 nm laser (1 W/cm) for 10 min, the temperature contrast increased by 20 °C, which was 4 times higher than free BODIPY-I-35. Confocal microscopy showed appreciable accumulation of LipoBOD in HeLa cells. In addition, when LipoBOD was incubated with urea in HeLa cells, we found that urea not only obviously enhanced the production of ROS, but also increased the apoptosis of HeLa cells. The synergistic effect of LipoBOD (20 μg/mL, at BODIPY-I-35-eq) with urea (250 mM) showed significantly higher phototoxicity than LipoBOD alone. Low dose can reduce the cell viability to 10%. Therefore, we have obtained an effective method of using urea to enhance the PDT effect.
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