Jiangsu Key Laboratory of Neuropsychiatric Diseases, College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China.
J Mater Chem B. 2022 Apr 20;10(16):3016-3022. doi: 10.1039/d2tb00176d.
Organic photosensitizers are of great interest in cancer diagnosis and treatments such as fluorescence imaging, photodynamic therapy (PDT), and photothermal therapy (PTT). However, their poor aqueous solubility, inadequate photostability and unsatisfactory photophysical parameters limit their clinical application. Herein, we report the construction of liposome encapsulating cyanine dye Cypate (Lipo-Cy) with enhanced nonradiative transition for efficient cancer therapy. After being loaded in liposomes, Cypate molecules are spatially confined within the hydrophobic lipid bilayer, thereby causing much better stability, higher photothermal conversion efficiency, and increased singlet oxygen quantum yield than free Cypate enhanced nonradiative transition through π-π aggregation. Lipo-Cy further enhanced the cellular uptake of Cypate, as well as preferable tumor accumulation and retention, leading to abundant intracellular singlet oxygen and potent hyperthermia at the tumor for effective PTT synergized PDT, even at dosages 10 times less than free Cypate. The Lipo-Cy exhibited superior anticancer efficiency, showing great prospects for clinical translation.
有机光敏剂在癌症诊断和治疗中（如荧光成像、光动力疗法（PDT）和光热疗法（PTT））具有重要的应用价值。然而，它们较差的水溶性、不足的光稳定性和不理想的光物理参数限制了其临床应用。在此，我们报告了一种囊泡包裹花菁染料 Cypate（Lipo-Cy）的构建，以增强非辐射跃迁，从而实现高效的癌症治疗。在被装载到囊泡中后，Cypate 分子在疏水性脂质双层内受到空间限制，从而导致比游离 Cypate 更好的稳定性、更高的光热转换效率和增加的单线态氧量子产率——通过π-π 聚集增强非辐射跃迁。Lipo-Cy 进一步增强了 Cypate 的细胞摄取，以及更好的肿瘤积累和保留，导致丰富的细胞内单线态氧和有效的高热治疗协同 PDT，即使在剂量比游离 Cypate 低 10 倍的情况下也是如此。Lipo-Cy 表现出优异的抗癌效率，具有很大的临床转化前景。
