Department of Chemical and Biomolecular Engineering, National University of Singapore, Singapore, 117585, Singapore.
State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials, Ministry of Education, and College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
Small. 2017 Jan;13(3). doi: 10.1002/smll.201602807. Epub 2016 Nov 7.
A multifunctional theranostic platform based on conjugated polymer nanoparticles (CPNs) with tumor targeting, fluorescence detection, photodynamic therapy (PDT), and photothermal therapy (PTT) is developed for effective cancer imaging and therapy. Two conjugated polymers, poly[9,9-bis(2-(2-(2-methoxyethoxy)ethoxy)-ethyl)fluorenyldivinylene]-alt-4,7-(2,1,3-benzothiadiazole) with bright red emission and photosensitizing ability and poly[(4,4,9,9-tetrakis(4-(octyloxy)phenyl)-4,9-dihydro-s-indacenol-dithiophene-2,7-diyl)-alt-co-4,9-bis(thiophen-2-yl)-6,7-bis(4-(hexyloxy)phenyl)-thiadiazolo-quinoxaline] with strong near-infrared absorption and excellent photothermal conversion ability are co-loaded into one single CPN via encapsulation approach using lipid-polyethylene glycol as the matrix. The obtained co-loaded CPNs show sizes of around 30 nm with a high singlet oxygen quantum yield of 60.4% and an effective photothermal conversion efficiency of 47.6%. The CPN surface is further decorated with anti-HER2 affibody, which bestows the resultant anti-HER2-CPNs superior selectivity toward tumor cells with HER2 overexpression both in vitro and in vivo. Under light irradiation, the PDT and PTT show synergistic therapeutic efficacy, which provides new opportunities for the development of multifunctional biocompatible organic materials in cancer therapy.
一种基于共轭聚合物纳米粒子(CPN)的多功能治疗平台,具有肿瘤靶向、荧光检测、光动力治疗(PDT)和光热治疗(PTT)功能,可有效用于癌症成像和治疗。两种共轭聚合物,具有明亮红光发射和光敏能力的聚[9,9-双(2-(2-(2-甲氧基乙氧基)乙氧基)乙基)芴基二乙烯基]-alt-4,7-(2,1,3-苯并噻二唑)和具有强近红外吸收和优异光热转换能力的聚[(4,4,9,9-四(4-(辛氧基)苯基)-4,9-二氢-s-茚并[1,2-b]噻吩-2,7-二基)-alt-共-4,9-双(噻吩-2-基)-6,7-双(4-(己氧基)苯基)-噻二唑并喹喔啉]通过使用脂质-聚乙二醇作为基质的包封方法共负载到一个 CPN 中。所得共负载的 CPN 大小约为 30nm,具有 60.4%的高单线态氧量子产率和 47.6%的有效光热转换效率。CPN 表面进一步用抗 HER2 亲和体修饰,使所得的抗 HER2-CPN 对 HER2 过表达的肿瘤细胞具有优异的选择性,无论是在体外还是体内。在光照射下,PDT 和 PTT 显示出协同治疗效果,为开发多功能生物相容性有机材料在癌症治疗中的应用提供了新的机会。