纳米载体的生物分布分析通常使用光学成像进行。虽然荧光染料可以与传输体，例如有机阴离子转运肽（OATPs）相互作用，但它们对生物分布的影响很少被研究。因此，本研究比较了四种近红外荧光染料（AF750、IRDye750、Cy7和DY-750）和染色的基于聚N-(2-羟基丙基)甲基丙烯酰胺（dye-pHPMAs）纳米载体在A431肿瘤携带小鼠中的肿瘤细胞摄取和生物分布。疏水性染料（Cy7、DY-750）的肿瘤细胞摄取量高于亲水性染料（AF750、IRDye750），并且是被动介导的但与OATPs无关。游离染料的消除取决于其疏水性，并且肿瘤摄取与血液循环时间相关。染色-pHPMAs循环时间更长，在肿瘤中的积累比游离染料更强。染料标记显著影响了纳米载体的肿瘤积累和生物分布。因此，需要低干扰的染料和进一步探索染料标签，以实现尽可能不偏的结果。在我们的评估中，AF750和IRDye750最适合标记亲水性纳米载体。版权所有© 2023 Elsevier Inc.。保留所有权利。

Biodistribution analyses of nanocarriers are often performed with optical imaging. Though dye tags can interact with transporters, e.g., organic anion transporting polypeptides (OATPs), their influence on biodistribution was hardly studied. Therefore, this study compared tumor cell uptake and biodistribution (in A431 tumor-bearing mice) of four near-infrared fluorescent dyes (AF750, IRDye750, Cy7, DY-750) and dye-labeled poly(N-(2-hydroxypropyl)methacrylamide)-based nanocarriers (dye-pHPMAs). Tumor cell uptake of hydrophobic dyes (Cy7, DY-750) was higher than that of hydrophilic dyes (AF750, IRDye750), and was actively mediated but not related to OATPs. Free dyes' elimination depended on their hydrophobicity, and tumor uptake correlated with blood circulation times. Dye-pHPMAs circulated longer and accumulated stronger in tumors than free dyes. Dye labeling significantly influenced nanocarriers' tumor accumulation and biodistribution. Therefore, low-interference dyes and further exploration of dye tags are required to achieve the most unbiased results possible. In our assessment, AF750 and IRDye750 best qualified for labeling hydrophilic nanocarriers.Copyright © 2023 Elsevier Inc. All rights reserved.