Sykes E, Woodburn K, Decker D, Kessel D
Department of Clinical Pathology, William Beaumont Hospital, Royal Oak, Michigan 48073.
Br J Cancer. 1994 Sep;70(3):401-4. doi: 10.1038/bjc.1994.317.
The clinical formulation of the anti-tumour agent Taxol involves the use of a mixture of ethanol and Cremophor EL. Gel electrophoresis and density-gradient ultracentrifugation were used to detect effects of Taxol infusions on serum lipoproteins. Use of the Cremophor vehicle results in a decrease in the electrophoretic mobility of serum lipoproteins along with the appearance of a lipoprotein dissociation product. These effects persist during a 24 h infusion and for at least 1.5 h afterwards, and can be reproduced in vitro using purified high-density lipoprotein (HDL) or low-density lipoprotein (LDL). In control serum, Taxol binds to albumin > HDL, but after serum is exposed to Cremophor EL in vitro or in vivo substantial binding of Taxol to the lipoprotein dissociation product(s) was observed. The latter could represent an important factor in taxol biodistribution.
抗肿瘤药物紫杉醇的临床制剂涉及使用乙醇和聚氧乙烯蓖麻油（Cremophor EL）的混合物。采用凝胶电泳和密度梯度超速离心法检测紫杉醇输注对血清脂蛋白的影响。使用聚氧乙烯蓖麻油载体导致血清脂蛋白的电泳迁移率降低，同时出现脂蛋白解离产物。这些效应在24小时输注期间以及之后至少1.5小时持续存在，并且使用纯化的高密度脂蛋白（HDL）或低密度脂蛋白（LDL）在体外可以重现。在对照血清中，紫杉醇与白蛋白的结合大于与HDL的结合，但在血清在体外或体内暴露于聚氧乙烯蓖麻油后，观察到紫杉醇与脂蛋白解离产物有大量结合。后者可能是紫杉醇生物分布的一个重要因素。
