Tang Qianyun, Si Weili, Huang Chuhan, Ding Kaikai, Huang Wei, Chen Peng, Zhang Qi, Dong Xiaochen
Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Jiangsu National Synergetic Innovation Center for Advanced Materials (SICAM), Nanjing Tech University (NanjingTech), Nanjing 211816, P. R. China.
J Mater Chem B. 2017 Feb 28;5(8):1566-1573. doi: 10.1039/c6tb02979e. Epub 2017 Feb 3.
Developing biocompatible, near infrared absorbing, and multi-functional photosensitizers is crucial for effective cancer phototherapy. In this contribution, a BF chelate of [4-iodo-5-(4-bromophenyl)-3-(4-methoxyphenyl)-1H-pyrrol-2-yl][4-iodo-5-(4-bromophenyl)-3-(4-methoxyphenyl)pyrrol-2-ylidene]amine (IABDP) with high singlet oxygen generation efficiency (∼92%) has been designed and synthesized. Soluble and near infrared absorbing nanoparticles (NPs) can be simply obtained from the self-assembly of IABDP molecules, which have a high photothermal conversion efficiency (∼37.9%). Under irradiation of a broadband Xenon lamp, IABBDP NPs are able to serve as common photosensitizers for photothermal imaging (PTI) and photoacoustic imaging (PAI) guided simultaneous photodynamic therapy (PDT) and photothermal therapy (PTT). Compared to the usual combined strategies that require two distinct photosensitizers and two excitation sources, the IABBDP NP based approach is simplified considerably, and hence is more convenient, reliable, and cost effective. Both in vitro and in vivo studies confirm the good biosafety and prominent anti-tumor phototoxicity of IABDP NPs. Finally, we demonstrate that the imaging guided synergistic dual modal phototherapy enabled by IABDP NPs can essentially inhibit tumor growth (87.2% inhibition) in mice without causing considerable side-effects, testifying the great potential of this multi-functional organic photosensitizer for clinical use.
开发具有生物相容性、近红外吸收和多功能的光敏剂对于有效的癌症光疗至关重要。在本研究中，设计并合成了一种[4-碘-5-(4-溴苯基)-3-(4-甲氧基苯基)-1H-吡咯-2-基][4-碘-5-(4-溴苯基)-3-(4-甲氧基苯基)吡咯-2-亚基]胺（IABDP）的硼氟螯合物，其单线态氧生成效率高（约92%）。通过IABDP分子的自组装可以简单地获得可溶且近红外吸收的纳米颗粒（NPs），其具有高光热转换效率（约37.9%）。在宽带氙灯照射下，IABBDP NPs能够作为常见的光敏剂用于光热成像（PTI）和光声成像（PAI）引导的同步光动力疗法（PDT）和光热疗法（PTT）。与通常需要两种不同光敏剂和两个激发源的联合策略相比，基于IABBDP NP的方法大大简化，因此更方便、可靠且具有成本效益。体外和体内研究均证实了IABDP NPs具有良好的生物安全性和显著的抗肿瘤光毒性。最后，我们证明由IABDP NPs实现的成像引导协同双模态光疗能够在小鼠中基本抑制肿瘤生长（抑制率为87.2%）且不会引起明显的副作用，证明了这种多功能有机光敏剂在临床应用中的巨大潜力。
