Department of Pharmaceutical Technology, University of Regensburg, Universitätsstr. 31, 93053 Regensburg, Germany.
Small. 2012 Nov 5;8(21):3368-75. doi: 10.1002/smll.201200733. Epub 2012 Aug 8.
Renal nanoparticle passage opens the door for targeting new cells like podocytes, which constitute the exterior part of the renal filter. When cyclo(RGDfC)-modified Qdots are tested on isolated primary podocytes for selective binding to the αvβ3 integrin receptor a highly cell- and receptor-specific binding can be observed. In displacement experiments with free cyclo(RGDfC) IC(50) values of 150 nM for αvβ3 integrin over-expressing U87-MG cells and 60 nM for podocytes are measured. Confocal microscopy shows a cellular Qdot uptake into vesicle-like structures. Our ex vivo study gives clear evidence that, after renal filtration, nanoparticles can be targeted to podocyte integrin receptors in the future. This could be a highly promising approach for future therapy and diagnostics of podocyte-associated diseases.
肾脏纳米颗粒通道为靶向新的细胞（如足细胞）打开了大门，足细胞构成了肾脏滤器的外部部分。当用环（RGDfC）修饰的 Qdot 对分离的原代足细胞进行测试以选择性结合 αvβ3 整联蛋白受体时，可以观察到高度细胞和受体特异性结合。在使用游离环（RGDfC）的置换实验中，U87-MG 细胞中 αvβ3 整联蛋白的 IC50 值为 150 nM，而足细胞的 IC50 值为 60 nM。共焦显微镜显示细胞内 Qdot 被摄取到囊泡样结构中。我们的离体研究清楚地表明，在肾脏过滤后，未来可以将纳米颗粒靶向到足细胞整联蛋白受体。这可能是未来治疗和诊断与足细胞相关疾病的一种很有前途的方法。
