Zhen Shijie, Xu Zhe, Suo Meng, Zhang Teng, Lyu Meng, Li Tianwei, Zhang Tianfu, Li Meijing, Zhao Zujin, Tang Ben Zhong
Guangxi Key Laboratory of Electrochemical and Magneto-chemical Functional Materials, College of Chemistry and Bioengineering, Guilin University of Technology, Guilin, 541006, P. R. China.
Affiliated Cancer Hospital & Institute of Guangzhou Medical University, School of Biomedical Engineering, Guangzhou Medical University, Guangzhou, 510182, P. R. China.
Adv Mater. 2025 Jan;37(3):e2411133. doi: 10.1002/adma.202411133. Epub 2024 Nov 26.
Phototheranositcs has recently aroused extreme attention due to its exceptional advantages. However, the poor photothernostic efficiency, limited penetration depth, strong oxygen-dependence, and inevitable damage to normal tissue of conventional photothernostic materials severely hindered their total theranostic efficacy. Herein, a series of near-infrared second (NIR-II) photosensitizers (PSs) featuring aggregation-induced emission (AIE), NIR-II fluorescence imaging (FLI), type I photodynamic therapy (PDT) and mild-temperature photothermal therapy (PTT) are constructed through dual-strategy methods combining donor group engineering and fluorination engineering. Profiting from sufficient molecular rotors and high electronegativity of fluorine, the developed 2-(2-((5-(4-((4-(diphenylamino)phenyl)(phenyl)amino)phenyl)thiophen-2-yl)methylene)-5,6-difluoro-3-oxo-2,3-dihydro-1H-inden-1-ylidene)malononitrile (BTS-2F) and 2-(2-((5-(4-(bis(4-(diphenylamino)phenyl)amino)phenyl)thiophen-2-yl)methylene)-5,6-difluoro-3-oxo-2,3-dihydro-1H-inden-1-ylidene)malononitrile (TTS-2F) are endowed with NIR-II AIE property, high radical reactive oxygen species (ROS) generation ability and mild-temperature photothermal conversion. Through thin film hydration method, the prepared BTS-2F and TTS-2F loaded liposomes exhibit significant NIR-II FLI and improved type-I PDT/mild-temperature PTT therapy under laser irradiation both in vitro and orthotopic 4T1 mice models.
光诊疗学因其独特优势最近引起了极大关注。然而，传统光诊疗材料的光诊疗效率低、穿透深度有限、对氧依赖性强以及对正常组织不可避免的损伤严重阻碍了它们的整体诊疗效果。在此，通过结合供体基团工程和氟化工程的双策略方法构建了一系列具有聚集诱导发光（AIE）、近红外二区（NIR-II）荧光成像（FLI）、I型光动力疗法（PDT）和温和温度光热疗法（PTT）的近红外二区光敏剂（PSs）。得益于充足的分子转子和氟的高电负性，所开发的2-(2-((5-(4-((4-(二苯胺基)phenyl)(phenyl)amino)phenyl)thiophen-2-yl)methylene)-5,6-二氟-3-氧代-2,3-二氢-1H-茚-1-亚基)丙二腈（BTS-2F）和2-(2-((5-(4-(双(4-(二苯胺基)phenyl)amino)phenyl)thiophen-2-yl)methylene)-5,6-二氟-3-氧代-2,3-二氢-1H-茚-1-亚基)丙二腈（TTS-2F）具有NIR-II AIE特性、高自由基活性氧（ROS）生成能力和温和温度光热转换。通过薄膜水化法，制备的负载BTS-2F和TTS-2F的脂质体在体外和原位4T1小鼠模型中激光照射下均表现出显著的NIR-II FLI以及改善的I型PDT/温和温度PTT治疗效果。
