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基于聚集诱导发光荧光团的纳米诊疗剂用于靶向及影像引导的化疗-光热联合治疗。

Aggregation Induced Emission Fluorogens Based Nanotheranostics for Targeted and Imaging-Guided Chemo-Photothermal Combination Therapy.

机构信息

Department of Chemistry and Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education), Tsinghua University, Beijing, 100084, China.

Joint Center for Life Sciences, Tsinghua University-Peking University, Beijing, 100084, China.

出版信息

Small. 2016 Dec;12(47):6568-6575. doi: 10.1002/smll.201601473. Epub 2016 Aug 24.

Abstract

Nanotheranostics for biomedical imaging-guided cancer therapy have attracted increasing interest due to their capabilities of both precise tumor diagnosis and high therapeutic efficacy. Among the diverse imaging models, fluorescence imaging have been extensively researched for their high sensitivity, simple operation, and low cost. In this work, aggregation induced emission (AIE) fluorogens based targeted nanotheranostics are facilely fabricated via paclitaxel (PTX) induced assembly of proteins for the first time. Thanks to the unique fluorescence property of AIE fluorogens PhENH , the prepared theranostic nanoplatforms can emit bright fluorescence even after being incorporated with the photothermal therapy agent polypyrrole (PPy), which will often decrease or quench the emission of common fluorescence dyes. The target moiety of cyclic arginine-glycine-aspartic acid (cRGD) endows the nanotheranostics with outstanding targeting ability, which can further facilitate the targeted imaging and cancer treatment. As revealed by the in vitro and in vivo experiments, the prepared nanotheranostics human serum albumin-PhENH -PPy-PTX-cRGD shows impressive performance in the targeted fluorescence imaging even after intravenous injection for 48 h, and their combined chemo-photothermal therapy is also very effective. These results indicate that AIE fluorogens based nanotheranostics would find a promising prospect in further improved multimodal imaging and imaging guided cancer treatment.

摘要

基于纳米诊疗剂的生物医学影像引导癌症治疗近年来受到了广泛关注,因为它们不仅可以精确诊断肿瘤,还可以提高治疗效果。在各种成像模式中,荧光成像是研究最为广泛的一种,因为它具有灵敏度高、操作简单、成本低等优点。在这项工作中,我们首次通过紫杉醇(PTX)诱导蛋白质组装,制备了基于聚集诱导发光(AIE)荧光团的靶向纳米诊疗剂。由于 AIE 荧光团 PhENH 的独特荧光性质,制备的诊疗纳米平台即使与光热治疗剂聚吡咯(PPy)结合,也能发出明亮的荧光,而通常情况下,常见的荧光染料的发射会降低或猝灭。环精氨酸-甘氨酸-天冬氨酸(cRGD)的靶向部分赋予了纳米诊疗剂优异的靶向能力,进一步促进了靶向成像和癌症治疗。通过体外和体内实验表明,制备的人血清白蛋白-PhENH-PPy-PTX-cRGD 纳米诊疗剂在静脉注射 48 小时后仍具有出色的靶向荧光成像性能,其联合化疗-光热治疗也非常有效。这些结果表明,基于 AIE 荧光团的纳米诊疗剂在进一步提高多模态成像和影像引导癌症治疗方面具有广阔的应用前景。

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