Computed tomography (CT) with contrast plays an important role as a clinical diagnostic tool but still has a limited diagnostic range. In this work, we developed a novel injectable iodine-based small molecule CT contrast agent, even can be used for bile duct diagnostics. The bile duct diagnosable CT contrast agent (BDICA) is synthesized with 5-amino-2,4,6-triiodoisophthaloyl dichloride (ATIPC), tromethamine and lactobionic acid (LBA) for asialoglycoprotein receptor (ASGPR) targeted delivery via receptor-mediated endocytosis and transport to the bile canaliculi. Specific binding to the ASGPRs was confirmed by in vitro cellular uptake in HepG2 cells (ASGPR positive) and HCT 116 cells (ASGPR negative). Compared to iohexol, BDICA has equal in vivo distribution and a 13-fold iodine increase in content was observed in bile juice after BDICA injection. The radiopaque contrast effect in the bile duct has been clearly shown in in vivo CT scans. Furthermore, within 36 h, 91.3% of the BDICA was eliminated without organ damage, which verified the overall safety of the contrast agent. BDICA not only provides sufficient contrast images similar to iohexol, but also provides superior images of the bile duct. Based on recent studies, it has been shown that BDICA is a promising, safe and effective contrast agent for CT imaging of the organs and soft tissues, including the bile duct.

对比计算机断层扫描（CT）作为临床诊断工具发挥着重要作用，但诊断范围仍然有限。在这项工作中，我们开发了一种新型的可注射的基于碘的小分子CT造影剂，甚至可以用于胆管诊断。胆管可诊断的CT造影剂（BDICA）与5-氨基-2,4,6-三碘间苯二甲酰二氯（ATIPC），氨丁三醇和乳糖酸（LBA）合成，通过受体介导的内吞作用靶向去唾液酸糖蛋白受体（ASGPR）。运输到胆小管。通过在HepG2细胞（ASGPR阳性）和HCT 116细胞（ASGPR阴性）中进行体外细胞摄取，证实了与ASGPR的特异性结合。与碘海醇相比，BDICA在体内具有相等的作用BDICA注射后胆汁中的碘分布和碘含量增加了13倍。体内CT扫描清楚地显示了胆管中的不透射线的对比效果。此外，在36小时内，消除了91.3％的BDICA，而没有器官损伤，这证明了造影剂的整体安全性。BDICA不仅可以提供类似于碘海醇的足够对比度图像，而且还可以提供胆管的出色图像。基于最近的研究，已经表明，BDICA是用于器官和软组织（包括胆管）的CT成像的有希望，安全和有效的造影剂。