Tumour homing and therapeutic effect of colloidal nanoparticles depend on the number of attached antibodies.
Tumour homing and therapeutic effect of colloidal nanoparticles depend on the number of attached antibodies.
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胶体纳米颗粒的肿瘤归巢和治疗效果取决于附着的抗体数量。
DOI：
10.1038/ncomms13818
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发表时间：
2016-12-19
影响因子：
16.6
通讯作者：
中科院分区：
文献类型：
--
作者：
纳米颗粒主动靶向肿瘤可以通过与特异性抗体结合来实现。在体外和体内使用皮下MCF-7乳腺癌小鼠模型和曲妥珠单抗功能化的金纳米颗粒证明了HER 2受体的特异性活性靶向。每个纳米颗粒附着的抗体数量以每个纳米颗粒与恰好一个或恰好两个抗体缀合的方式进行精确控制。正如预期的那样，在体外我们发现每个纳米颗粒连接两个而不是一个抗体的纳米颗粒的靶向效率适度增加。然而，体内数据表明，对于仅具有恰好一种抗体的纳米颗粒获得最佳效果。有迹象表明，这是基于规模效应。这些结果突出了精确控制纳米颗粒表面上的配体密度以优化主动靶向的重要性，并且更少的抗体可以表现出更大的效果。 将纳米颗粒靶向肿瘤的常见策略是与特异性抗体缀合，靶向癌细胞优先表达的蛋白质。在这里，作者表明，结合到纳米颗粒的抗体的数量影响体外和体内的靶向能力。
Active targeting of nanoparticles to tumours can be achieved by conjugation with specific antibodies. Specific active targeting of the HER2 receptor is demonstrated in vitro and in vivo with a subcutaneous MCF-7 breast cancer mouse model with trastuzumab-functionalized gold nanoparticles. The number of attached antibodies per nanoparticle was precisely controlled in a way that each nanoparticle was conjugated with either exactly one or exactly two antibodies. As expected, in vitro we found a moderate increase in targeting efficiency of nanoparticles with two instead of just one antibody attached per nanoparticle. However, the in vivo data demonstrate that best effect is obtained for nanoparticles with only exactly one antibody. There is indication that this is based on a size-related effect. These results highlight the importance of precisely controlling the ligand density on the nanoparticle surface for optimizing active targeting, and that less antibodies can exhibit more effect. A common strategy to target nanoparticles to tumours is conjugation with specific antibodies, targeting protein expressed preferentially by cancer cells. Here the authors show that the number of antibodies bound to the nanoparticle influences the targeting ability in vitro and in vivo.
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