Damle N S, Seevers R H, Schwendner S W, Counsell R E
J Pharm Sci. 1983 Aug;72(8):898-901. doi: 10.1002/jps.2600720814.
This paper describes the possible utility of plasma lipoproteins for the site-specific delivery of diagnostic agents. The class of lipoproteins known as chylomicrons was selected for this preliminary study, since they are known to be rapidly metabolized and taken up by the liver. Cholesteryl iopanoate (II), an iodinated analogue of a normal constituent of the hydrophobic core of chylomicrons, was synthesized from cholesterol and iopanoic acid (I) and subsequently radiolabeled with ioidine-125. Whereas intravenous administration of II in physiological saline resulted in the appearance of approximately 31% of the dose in the liver at 0.5 hr, prior incorporation of II into chylomicrons resulted in an almost threefold (87%) increase in the liver accumulation of II in the same time period. A more gradual appearance of II in steroid-secreting tissues was consistent with the association of II with high-density lipoproteins following administration.
本文描述了血浆脂蛋白用于诊断剂位点特异性递送的潜在效用。在这项初步研究中选择了被称为乳糜微粒的脂蛋白类别，因为已知它们会被肝脏快速代谢和摄取。胆固醇碘番酸盐（II）是乳糜微粒疏水核心正常成分的碘化类似物，由胆固醇和碘番酸（I）合成，随后用碘-125进行放射性标记。在生理盐水中静脉注射II时，0.5小时后肝脏中约31%的剂量出现，而在将II预先掺入乳糜微粒后，同一时间段内II在肝脏中的积累几乎增加了两倍（87%）。给药后II在类固醇分泌组织中出现得更为缓慢，这与给药后II与高密度脂蛋白的结合一致。
