The biodistribution of dendronized iron oxides, [email protected]_DOTAGA and melanin-targeting [email protected]_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [¹⁷⁷Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobiliary and urinary excretions. Little tumor uptake could be highlighted after intravenous injection probably as a consequence of the negatively charged DOTAGA-derivatized shell, which reduces the diffusion across the cells’ membrane. Planar scintigraphy images demonstrated a moderate specific tumor uptake of melanoma-targeted [¹⁷⁷Lu][email protected]_ICF_DOTAGA at 2 h post-intravenous injection (pi), and the highest tumor uptake of the control probe [¹⁷⁷Lu][email protected]_DOTAGA at 30 min pi, probably due to the enhanced permeability and retention effect. In addition, ex vivo confocal microscopy studies showed a high specific targeting of human melanoma samples impregnated with [email protected]_ICF_Alexa647_ DOTAGA.

中文翻译：

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静脉注射树突化纳米粒子后黑色素颗粒的主动靶向评价。

使用磁共振成像（MRI）和平面闪烁显像技术通过[ ¹⁷⁷ Lu] Lu放射标记在体内研究了树突化的铁氧化物[受电子邮件保护] _DOTAGA和靶向黑色素[受电子邮件保护] _ICF_DOTAGA的生物分布。MRI实验显示，树突状纳米颗粒（DPs）以及肝胆和尿液排泄物具有高对比度。静脉注射后几乎没有肿瘤吸收，这可能是由于带负电荷的DOTAGA衍生化的外壳导致的，该外壳减少了跨细胞膜的扩散。平面闪烁显像图像显示以黑色素瘤为靶标的中度特异性肿瘤摄取[ ¹⁷⁷静脉注射（pi）后2 h，Lu] [受电子邮件保护] _ICF_DOTAGA和对照探针的最高肿瘤吸收率[ ¹⁷⁷ Lu] pi在30分钟时达到最高的肿瘤吸收率，这可能是由于通透性和保留效果增强所致。此外，离体共聚焦显微镜研究表明，对以[电子邮件保护] _ICF_Alexa647_ DOTAGA浸渍的人黑素瘤样品具有高特异性。