Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Proc Natl Acad Sci U S A. 2010 Jan 19;107(3):1235-40. doi: 10.1073/pnas.0914140107. Epub 2009 Dec 29.
PEGylated gold nanoparticles are decorated with various amounts of human transferrin (Tf) to give a series of Tf-targeted particles with near-constant size and electrokinetic potential. The effects of Tf content on nanoparticle tumor targeting were investigated in mice bearing s.c. Neuro2A tumors. Quantitative biodistributions of the nanoparticles 24 h after i.v. tail-vein injections show that the nanoparticle accumulations in the tumors and other organs are independent of Tf. However, the nanoparticle localizations within a particular organ are influenced by the Tf content. In tumor tissue, the content of targeting ligands significantly influences the number of nanoparticles localized within the cancer cells. In liver tissue, high Tf content leads to small amounts of the nanoparticles residing in hepatocytes, whereas most nanoparticles remain in nonparenchymal cells. These results suggest that targeted nanoparticles can provide greater intracellular delivery of therapeutic agents to the cancer cells within solid tumors than their nontargeted analogs.
聚乙二醇化金纳米粒子被各种数量的人转铁蛋白（Tf）修饰，得到一系列具有近恒定尺寸和电动电势的 Tf 靶向粒子。在皮下Neuro2A 肿瘤小鼠中研究了 Tf 含量对纳米粒子肿瘤靶向的影响。静脉尾静脉注射后 24 小时的纳米粒子定量生物分布表明，肿瘤和其他器官中的纳米粒子积累与 Tf 无关。然而，纳米粒子在特定器官内的定位受 Tf 含量的影响。在肿瘤组织中，靶向配体的含量显著影响定位于癌细胞内的纳米粒子数量。在肝组织中，高 Tf 含量导致少量纳米粒子驻留在肝细胞中，而大多数纳米粒子仍存在于非实质细胞中。这些结果表明，与非靶向类似物相比，靶向纳米粒子可以为实体瘤中的癌细胞提供更多的治疗剂的细胞内递送。
