Woodburn K, Kessel D
Department of Pharmacology, Wayne State University School of Medicine, Detroit, MI 48201.
J Photochem Photobiol B. 1994 Mar;22(3):197-201. doi: 10.1016/1011-1344(93)06968-9.
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 non-ionic 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.
聚氧乙烯蓖麻油（CRM）是一种非离子型两亲性乳化剂，已被用作多种疏水药物的肠胃外给药载体。在浓度高于0.4毫克/毫升时，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）稍敏感一些。另外两种非离子型去污剂吐温X-100和吐温80也观察到了同样的现象。超速离心实验表明，CRM会改变HDL的密度，产生一种比重与LDL大致相同的产物。将用CRM增溶的中卟啉给予小鼠后，与这种新的HDL种类结合的卟啉会迅速清除。这种现象可能解释了一些报告，这些报告表明CRM可促进光敏剂向肿瘤组织的分布。
