School of Applied Chemistry and Engineering, University of Science and Technology of China, Hefei 230026, P.R. China.
State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P.R. China.
Biomater Sci. 2022 Aug 24;10(17):4815-4821. doi: 10.1039/d2bm00670g.
The fabrication of a high-performance second near-infrared (NIR-II) biological window fluorophore is in urgent need for precise diagnosis and treatment of cancer. Nevertheless, the construction of phototherapeutic agents in the NIR-II region with excellent imaging performance and minimal side effects remains a big challenge due to the limited availability of core fluorophore candidates. In this study, a new NIR-II fluorescent probe, CB1, which is an aza-BODIPY core conjugated with bulky donors, was designed and synthesized. CB1 was further encapsulated in DSPE-PEG2000 to impart water solubility, which shows brighter NIR-II fluorescence and higher photostability than the clinically used indocyanine green (ICG). CB1 nanoparticles show deep tissue penetration and high imaging contrast . In addition, molecular conformation enables CB1 nanoparticles to exhibit good photothermal properties. Both and assessments confirm that CB1 nanoparticles could be utilized as distinguished theranostic agents for NIR-II fluorescence imaging and tumor growth inhibition with negligible side effects. Collectively, this work provides a promising approach for constructing a new platform for cancer diagnosis and therapy.
迫切需要制备高性能的第二代近红外二区（NIR-II）生物窗口荧光探针，以实现癌症的精准诊断和治疗。然而，由于可用的核心荧光团候选物有限，在 NIR-II 区域构建具有优异成像性能和最小副作用的光疗剂仍然是一个巨大的挑战。在这项研究中，设计并合成了一种新型的 NIR-II 荧光探针 CB1，它是一个带有大供体的氮杂-BODIPY 核心。CB1 进一步被包裹在 DSPE-PEG2000 中以赋予其水溶性，其表现出比临床使用的吲哚菁绿（ICG）更亮的 NIR-II 荧光和更高的光稳定性。CB1 纳米颗粒具有更深的组织穿透能力和更高的成像对比度。此外，分子构象使 CB1 纳米颗粒表现出良好的光热性能。和 评估均证实，CB1 纳米颗粒可用作新型 NIR-II 荧光成像和肿瘤生长抑制的治疗诊断试剂，且副作用可忽略不计。总之，这项工作为构建癌症诊断和治疗的新平台提供了一种有前途的方法。
