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A Self-Assembled “Albumin–Conjugate” Nanoprobe for Near Infrared Optical Imaging of Subcutaneous and Metastatic Tumors
ACS Applied Bio Materials ( IF 4.7 ) Pub Date : 2020-01-07 , DOI: 10.1021/acsabm.9b00839
Weiwei Wang 1 , Zhixiao Fang 1 , Xingming Zhang 2 , Haiyan Cai 1 , Yucheng Zhao 1 , Wenli Gu 2 , Xi Yang 3 , Yingli Wu 1
Affiliation  

The need for in situ accurate identification of tumor assisted real-time image-guided surgical resection calls for new near-infrared fluorescence agents with high tumor-sensitivity and excellent biocompatibility. Here, an albumin–conjugate nanoparticle system HSA-Er-RI-Cl was designed, synthesized, and applied in cancer imaging, which simultaneously achieved the EPR effect, hypoxia-targeting, and EGFR-targeting property. Our novel nanoprobe is composed of human serum albumin (HSA) and double-targeting small molecule conjugate (Er-RI-Cl): a hypoxia-targeting heptamethine carbocyanine dye (RI-Cl) conjugated with a clinic anti-EGFR antagonist (Erlotinib) by covalent bonding. This conjugate could bind to albumin proteins, forming albumin–conjugate complexes, and those complexes self-assemble into particles with diameters of approximately 100 nm in the aqueous solution. The tumor hypoxia and EGFR targeting specificity of HSA-Er-RI-Cl was, respectively, evaluated in vitro and in vivo. Using murine xenograft subcutaneous and brain metastatic tumor models, we demonstrated that HSA-Er-RI-Cl is a highly potent tumor-targeting NIR agent for noninvasive imaging with remarkable tumor localization and excellent pharmacokinetic properties.

中文翻译:

用于皮下和转移性肿瘤的近红外光学成像的自组装“白蛋白-共轭”纳米探针

并且这些配合物在水溶液中自组装成直径约为100 nm的颗粒。分别在体外和体内评估了HSA-Er-RI-Cl的肿瘤缺氧和EGFR靶向特异性。使用小鼠异种移植皮下和脑转移肿瘤模型,我们证明 HSA-Er-RI-Cl 是一种高效的肿瘤靶向 NIR 试剂,用于无创成像,具有显着的肿瘤定位和优异的药代动力学特性。
更新日期:2020-01-07
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