Cheng Qiang, Pang E, Zhou Zirong, Tang Yuanyu, Liu Chao, Wang Feng, Zhao Shaojing, Wang Benhua, He Dan, Song Xiangzhi, Lan Minhuan
College of Chemistry & Chemical Engineering, Central South University Changsha, Hunan 410083, P. R. China.
School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology Wuhan, Hubei 430074, P. R. China.
J Phys Chem Lett. 2025 Aug 14;16(32):8262-8271. doi: 10.1021/acs.jpclett.5c01550. Epub 2025 Aug 5.
A photosensitizer that exhibits high singlet oxygen (O) generation efficiency under moderate aggregation holds promise for combined photodynamic therapy (PDT) and chemotherapy. Here, we develop a phenoxazine-modified helical boron-dipyrromethene () and manipulate its aggregation state to enhance the O generation efficiency. It demonstrates that under the moderately aggregated state, affords the highest O generation capability with a quantum yield of 53%. This is due to the inhibition of nonradiative transition and the reduction of the energy gap between the lowest singlet state and the triplet excited state. This unique property enables to persist with excellent O production capability when assembled with a chemotherapeutic drug, such as tamoxifen (TAM). By finely regulating the molar ratio of TAM and to 3:7 to optimize molecular aggregation, the resulting nanoparticles (NPs) achieve a O quantum yield of 55%. Subsequently, these NPs are successfully applied in the combined PDT and chemotherapy of tumor mice. This study highlights the design and aggregation-state regulation of a photosensitizer for enhanced photodynamic activity, paving the way for the development of combined chemotherapy strategies.
一种在适度聚集状态下表现出高单线态氧（O）生成效率的光敏剂有望用于联合光动力疗法（PDT）和化疗。在此，我们开发了一种吩恶嗪修饰的螺旋硼二吡咯亚甲基（），并操纵其聚集状态以提高O生成效率。结果表明，在适度聚集状态下，具有最高的O生成能力，量子产率为53%。这是由于抑制了非辐射跃迁以及降低了最低单重态与三重激发态之间的能隙。这种独特的性质使得与化疗药物（如他莫昔芬（TAM））组装时能够保持优异的O生成能力。通过精细调节TAM与的摩尔比至3:7以优化分子聚集，所得纳米颗粒（NPs）实现了55%的O量子产率。随后，这些NPs成功应用于肿瘤小鼠的联合PDT和化疗。本研究突出了用于增强光动力活性的光敏剂的设计和聚集状态调节，为联合化疗策略的发展铺平了道路。
