State Key Laboratory of Chemical Resource Engineering, Beijing Laboratory of Biomedical Materials, Beijing University of Chemical Technology, China.
Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety Institute of High Energy Physics, Chinese Academy of Sciences, China.
Angew Chem Int Ed Engl. 2018 Aug 27;57(35):11384-11388. doi: 10.1002/anie.201807602. Epub 2018 Aug 1.
Fluorescent dyes with multi-functionality are of great interest for photo-based cancer theranostics. However, their low singlet oxygen quantum yield impedes their potential applications for photodynamic therapy (PDT). Now, a molecular self-assembly strategy is presented for a nanodrug with a remarkably enhanced photodynamic effect based on a dye-chemodrug conjugate. The self-assembled nanodrug possesses an increased intersystem crossing rate owing to the aggregation of dye, leading to a distinct singlet oxygen quantum yield (Φ( O )). Subsequently, upon red light irradiation, the generated singlet oxygen reduces the size of the nanodrug from 90 to 10 nm, which facilitates deep tumor penetration of the nanodrug and release of chemodrug. The nanodrug achieved in situ tumor imaging and potent tumor inhibition by deep chemo-PDT. Our work verifies a facile and effective self-assembly strategy to construct nanodrugs with enhanced performance for cancer theranostics.
具有多功能的荧光染料在基于光的癌症诊治中非常有吸引力。然而，它们的单线态氧量子产率低，阻碍了它们在光动力疗法（PDT）中的潜在应用。现在，提出了一种基于染料-化疗药物偶联物的纳米药物的分子自组装策略，以显著提高光动力效应。由于染料的聚集，自组装纳米药物具有增加的系间穿越速率，导致明显的单线态氧量子产率（Φ（O））。随后，在红光照射下，生成的单线态氧将纳米药物的尺寸从 90nm 减小到 10nm，这有利于纳米药物的深层肿瘤穿透和化疗药物的释放。纳米药物通过深部化学 PDT 实现了原位肿瘤成像和有效的肿瘤抑制。我们的工作验证了一种简单有效的自组装策略，用于构建具有增强癌症诊治性能的纳米药物。
