Kibat P, Stricker H
Institut für Pharmazeutische Technologie und Biopharmazie, Universität Heidelberg.
Arzneimittelforschung. 1988 Oct;38(10):1472-8.
Carboxyfluorescein (CF) and fluorescein dilaurate (FDL) have been encapsulated in either small or large multilamellar liposomes of various lipid composition. Cholesterol (CH)-free liposomes showed relatively rapid CF release when dispersed in buffer, plasma or whole blood. The same behaviour was seen with liposomes which contained a lipid whose phase transition temperature was less than 37 degrees C. The CH-free preparations also showed marked aggregation in plasma. After i.v. application to rabbits the elimination of liposomal CF was found to depend upon the typ of phospholipid present, the CH content, the surface charge and vesicle size. The lipophilic substance FDL was lost from circulation more rapidly than the hydrophilic CF. All of the measured plasma levels indicated an open two-compartment model, i.e. with two exits. The calculated microconstants provide information about the distribution kinetics.
羧基荧光素（CF）和二月桂酸荧光素（FDL）已被包封于具有不同脂质组成的小或大多层脂质体中。不含胆固醇（CH）的脂质体分散在缓冲液、血浆或全血中时显示出相对较快的CF释放。含有相变温度低于37℃脂质的脂质体也观察到相同的行为。不含CH的制剂在血浆中也显示出明显的聚集。静脉注射给兔子后，发现脂质体CF的消除取决于所存在的磷脂类型、CH含量、表面电荷和囊泡大小。亲脂性物质FDL从循环中消失的速度比亲水性CF更快。所有测得的血浆水平均表明为开放二室模型，即有两个出口。计算出的微常数提供了有关分布动力学的信息。
