Department of Pharmacy, The Third Affiliated Hospital (The Affiliated Luohu Hospital) of Shenzhen University, Shenzhen 518001, China.
Department of Pharmaceutics, School of Pharmacy, Fujian Medical University, Fuzhou 350122, China.
ACS Appl Mater Interfaces. 2020 Sep 23;12(38):42551-42557. doi: 10.1021/acsami.0c12670. Epub 2020 Sep 14.
Because light exhibits excellent spatiotemporal resolution, photodynamic therapy (PDT) is becoming a promising method for cancer treatment. However, in a single photosensitizer (PS), it remains a big challenge to achieve all key properties including effective singlet oxygen (O) production under long-wavelength laser and bright near-infrared (NIR) emission without toxicity in the dark. In addition, clinically used traditional PSs encounter quenched fluorescence and decreased O production because of molecular aggregation in aqueous solution. To solve the aforementioned issues, quinoxalinone CN (QCN) with effective O generation under long-wavelength (530 nm) laser irradiation and aggregation-induced NIR emission is rationally designed by precise optimization of the quinoxalinone scaffold. After being encapsulated by an amphiphilic polymer (DSPE-PEG), the yielded nanoparticles exhibit highly efficient O production and stable NIR fluorescence located at 800 nm without obvious toxicity under the dark. Both and evaluation identify that QCN would be a promising PS for image-guided PDT of tumors.
由于光具有优异的时空分辨率，光动力疗法（PDT）正成为癌症治疗的一种有前途的方法。然而，在单一的光敏剂（PS）中，要实现所有关键特性，包括在长波长激光下有效产生单线态氧（O）和在黑暗中无毒性的明亮近红外（NIR）发射，仍然是一个巨大的挑战。此外，临床上使用的传统 PS 由于在水溶液中分子聚集而遇到荧光猝灭和 O 产量降低。为了解决上述问题，通过对喹喔啉酮支架的精确优化，合理设计了具有长波长（530nm）激光照射下有效 O 生成和聚集诱导的近红外发射的喹喔啉酮 CN（QCN）。被两亲聚合物（DSPE-PEG）包裹后，所得纳米颗粒在黑暗中表现出高效的 O 生成和位于 800nm 的稳定近红外荧光，无明显毒性。和评价都表明 QCN 将是一种有前途的用于肿瘤图像引导 PDT 的 PS。
