Huo Shuaidong, Chen Shizhu, Gong Ningqiang, Liu Juan, Li Xianlei, Zhao Yuanyuan, Liang Xing-Jie
Laboratory of Controllable Nanopharmaceuticals, Chinese Academy of Sciences (CAS) Center for Excellence in Nanoscience, and CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology of China, No. 11 Beiyitiao, Zhongguancun, Beijing 100190, P. R. China.
University of Chinese Academy of Sciences , Beijing 100049, P. R. China.
Bioconjug Chem. 2017 Jan 18;28(1):239-243. doi: 10.1021/acs.bioconjchem.6b00488. Epub 2016 Oct 18.
Ultrasmall nanoparticles provide us with essential alternatives for designing more efficient nanocarriers for drug delivery. However, the fast clearance of ultrasmall nanoparticles limits their application to some extent. One of the most frequently used compound to slow the clearance of nanocarriers and nanodrugs is PEG, which is also approved by FDA. Nonetheless, few reports explored the effect of the PEGylation of ultrasmall nanoparticles on their behavior in vivo. Herein, we investigated the impact of different PEG grafting level of 2 nm core sized gold nanoparticles on their biological behavior in tumor-bearing mice. The results indicate that partial (∼50%) surface PEGylation could prolong the blood circulation and increase the tumor accumulation of ultrasmall nanoparticles to a maximum extent, which guide us to build more profitable small-sized nanocarriers for drug delivery.
超小纳米颗粒为我们设计更高效的药物递送纳米载体提供了重要的替代方案。然而，超小纳米颗粒的快速清除在一定程度上限制了它们的应用。聚乙二醇（PEG）是最常用于减缓纳米载体和纳米药物清除的化合物之一，它也获得了美国食品药品监督管理局（FDA）的批准。尽管如此，很少有报告探讨超小纳米颗粒的聚乙二醇化对其体内行为的影响。在此，我们研究了不同聚乙二醇接枝水平的2纳米核心尺寸金纳米颗粒对荷瘤小鼠体内生物学行为的影响。结果表明，部分（约50%）表面聚乙二醇化可以最大程度地延长超小纳米颗粒的血液循环并增加其在肿瘤中的积累，这指导我们构建更具效益的小型药物递送纳米载体。
