Ruan Zheng, Zhao Yangyang, Yuan Pan, Liu Le, Wang Yucai, Yan Lifeng
Hefei National Laboratory for Physical Sciences at the Microscale, CAS Key Laboratory of Soft Matter Chemistry, and Department of Chemical Physics, iCHEM, University of Science and Technology of China, China.
J Mater Chem B. 2018 Feb 7;6(5):753-762. doi: 10.1039/c7tb02924a. Epub 2018 Jan 18.
Drug-free biocompatible nanoparticles with photosensitizers as both diagnostic and therapy agents represent an emerging approach for imaging-guided photodynamic therapy (PDT). Here, a NSH-active boron-dipyrromethene (BODIPY) derivative with a bromine substituted (BODIPY-Br, for simplicity, BDP-Br) photosensitizer was synthesized; it showed a high ability of generating reactive oxygen species (ROS) upon irradiation for PDT and near infrared fluorescence imaging ability. Then, a simple PEGylated BDP-Br (PEG-BDP) as a kind of macro photosensitizer was prepared which showed superior cellular uptake ability, high efficiency of imaging, and curing with PDT therapy in vitro and in vivo. After administration with a 4T1 orthotopic tumor model, the resultant PEG-BDP showed prolonged blood circulation and preferential tumor accumulation compared with free BDP-Br molecules. Once accumulated in tumor tissues, therapeutic effects of PEG-BDP could significantly suppress primary tumor growth and has no evident side effects at a weak irradiation energy as low as 35 mW cm for 20 minutes. The designation of this simple structure macro photosensitizer agent provides new avenues for efficient imaging-guided cancer PDT.
以光敏剂作为诊断和治疗剂的无药物生物相容性纳米颗粒代表了一种用于成像引导光动力疗法（PDT）的新兴方法。在此，合成了一种具有溴取代的NSH活性硼二吡咯亚甲基（BODIPY）衍生物（BODIPY-Br，为简便起见，简称BDP-Br）光敏剂；它在光照下表现出高产生活性氧（ROS）用于PDT的能力以及近红外荧光成像能力。然后，制备了一种简单的聚乙二醇化BDP-Br（PEG-BDP）作为一种大分子光敏剂，其在体外和体内均表现出优异的细胞摄取能力、高效成像能力以及PDT治疗的治愈能力。在用4T1原位肿瘤模型给药后，与游离的BDP-Br分子相比，所得的PEG-BDP显示出延长的血液循环和优先的肿瘤蓄积。一旦在肿瘤组织中蓄积，PEG-BDP的治疗效果可显著抑制原发性肿瘤生长，并且在低至35 mW/cm²的弱照射能量下照射20分钟时没有明显的副作用。这种简单结构大分子光敏剂的设计为高效成像引导的癌症PDT提供了新途径。
