Self-assembled PEG-IR-780-C13 micelle as a targeting, safe and highly-effective photothermal agent for in vivo imaging and cancer therapy
Self-assembled PEG-IR-780-C13 micelle as a targeting, safe and highly-effective photothermal agent for in vivo imaging and cancer therapy
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自组装 PEG-IR-780-C13 胶束作为体内成像和癌症治疗的靶向、安全、高效光热剂
DOI：
10.1016/j.biomaterials.2015.01.069
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发表时间：
2015-05-01
期刊：
影响因子：
14
通讯作者：
Hu, Yiqiao
中科院分区：
文献类型：
--
作者：
Yuan, Ahu;Qiu, Xuefeng;Hu, Yiqiao
IR-780是一种代表性的疏水近红外荧光染料，能够在体外和体内进行荧光成像和光热治疗。然而，在所有药学上可接受的溶剂中的不溶性限制了其进一步的生物学应用。为了增加溶解度，我们开发了一种新的自组装IR-780胶束（PEG-IR-780-C13）的基础上的IR-780的结构修饰。简言之，在IR-780的一侧上修饰亲水性PEG（2000），并且将另一侧上的疏水性碳链从0延伸至C16（额外的C13碳链）。该改性提供了更好的自组装能力、改善的水溶性和更高的稳定性。此外，PEG-IR-780-C13胶束在静脉注射后特异性靶向肿瘤，可用于肿瘤成像。体外细胞活力测定和体内光热治疗实验表明，PEG-IR-7803胶束与808 nm激光照射相结合可以有效地消融CT-26细胞或Cf-26异种移植肿瘤。更重要的是，在静脉内施用治疗剂量的所产生的胶束后，没有观察到显著的毒性。总的来说，我们的胶束可能具有最小的安全性问题，同时显示出优异的治疗效果，因此可能是一种新的光热剂，在临床应用中有潜在的用途。(C)2015爱思唯尔有限公司版权所有。
IR-780, a representative hydrophobic near-infrared (NIR) fluorescence dye, is capable of fluorescently imaging and photothermal therapy in vitro and in vivo. However, insolubility in all pharmaceutically acceptable solvents limits its further biological applications. To increase solubility, we developed a novel self-assembled IR-780 containing micelle (PEG-IR-780-C13) based on the structural modification of IR-780. Briefly, a hydrophilic PEG(2000) was modified on the one side of IR-780, and the hydrophobic carbon chain on the other side was extended from 0 to C16 (additional C13 carbon chain). The modification provides a better self-assemble capability, improved water solubility and higher stability. In addition, PEG-IR-780-C13 micelles are specifically targeted to the tumor after intravenous injection and can be used for tumor imaging. The in vitro cell viability assays and in vivo photothermal therapy experiments indicated that CT-26 cells or Cf-26 xenograft tumors can be effectively ablated by combining PEG-IR-7803 micelles with 808 nm laser irradiation. More importantly, no significant toxicity can be observed after intravenous administration of the therapeutic dose of generated micelles. Overall, our micelles may have the least safety concern while showing excellent treatment efficacy, and thus may be a new photothermal agent potentially useful in clinical applications. (C) 2015 Elsevier Ltd. All rights reserved.