THE ALTERATION OF PLASMA-LIPOPROTEINS BY CREMOPHOR EL
THE ALTERATION OF PLASMA-LIPOPROTEINS BY CREMOPHOR EL
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DOI：
10.1016/1011-1344(93)06968-9
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发表时间：
1994-03-01
影响因子：
5.4
通讯作者：
KESSEL, D
中科院分区：
文献类型：
--
作者：
WOODBURN, K;KESSEL, D
Cremophor EL（CRM）是一种非离子型两亲乳化剂，已被用作许多疏水性药物的胃肠外载体。当浓度超过0.4 mg ml（-1）时，CRM会改变脂蛋白，从而降低其电泳迁移率;在这方面，高密度脂蛋白（HDL）比低密度脂蛋白（LDL）更敏感。用Triton X-100和Tween-80（两种其它非离子洗涤剂）观察到相同的现象。超离心实验表明，CRM改变了HDL的密度，导致产物具有与LDL大致相同的比重。给小鼠施用用CRM溶解的中卟啉导致与这种新的HDL种类结合的卟啉的快速清除。这种现象可以解释的报告表明，CRM促进光敏剂的肿瘤组织的分布。
Cremophor EL (CRM) is a non-ionic amphipathic emulsifier which has been used as a parenteral vehicle for many hydrophobic drugs. At concentrations above 0.4 mg ml(-1), CRM alters lipoproteins so as to reduce their electrophoretic mobility; high density lipoprotein (HDL) is somewhat more sensitive than low density lipoprotein (LDL) in this regard. The same phenomenon was observed with Triton X-100 and Tween-80, two other nonionic detergents. Ultracentrifugation experiments show that CRM alters the density of HDL resulting in a product with approximately the same specific gravity as LDL. Administration of mesoporphyrin solubilized with CRM to the mouse resulted in a rapid clearance of porphyrin bound to this new HDL species. Such a phenomenon may account for reports which indicate that CRM promotes the distribution of photosensitizing agents to neoplastic tissues.