文摘
Photodynamic therapy (PDT) is hampered by poor water solubility and skin phototoxicity of photosensitizers (PSs). Incorporation of PSs into nanocarrier (Nano-PDT) has been designed to overcome these problems. However, self-quenching of PSs highly condensed in Nano-PDT significantly reduced singlet oxygen (<sup>1sup>O<sub>2sub>) generation, resulting in unsatisfactory PDT efficacy. Here, we developed a novel tripleffect Nano-PDT, which has a special core–shell nanostructure by synergistic integration of perfluorotributylamine (PFTBA) and human serum albumin (HSA) to improve PDT. It has three mechanisms to relight quenched PSs, thereby generating more <sup>1sup>O<sub>2sub>. First, PSs uniformly dispersed in the shell, preventing self-quenching caused by π–π stacking. Second, HSA as nanocarrier extends the triplet-state lifetimes of PSs, increasing the amount of <sup>1sup>O<sub>2sub>. Third, PFTBA as core dissolves and protects<sup>1sup> O<sub>2sub> to extend the duration time of action of <sup>1sup>O<sub>2sub>. Compared with PS-encapsulated Nano-PDT, the self-quenching of PSs in tripleffect Nano-PDT can be effectively overcome. The fluorescence and <sup>1sup>O<sub>2sub> generation of PS are increased by approximately 100-fold and 15-fold, respectively. After intravenous injection into tumor-bearing mice, the tumor growth is significantly inhibited, while the PS-encapsulated Nano-PDT has almost no effect. The novel tripleffect Nano-PDT may guide improvement of existing clinical PDT and future PDT design.