Investigation on the relationship between the physicochemical properties of particles composed of a novel lipid A analog, E5531, and its pharmacokinetics

被引:0
|
作者
Asai, Y [1 ]
机构
[1] Eisai & Co Ltd, Formulat Res Lab, Gifu 5016195, Japan
关键词
lipid A; calcium ion; particle size; membrane fluidity; pharmacokinetics;
D O I
10.1163/1568552054194177
中图分类号
TQ [化学工业];
学科分类号
0817 ;
摘要
To obtain information on the effects of a divalent cation (Ca2+) on the membrane properties of the lipid A analog, E5531, the particle size, zeta potential, membrane fluidity and pharmacokinctices was investigated in rats after the addition of calcium ion. Within a molar ratio for [Ca2+]/[E5531] <= 3, the presence of Ca2+ increased the zeta potentials of the E5531 membrane, but had no effect on particle size. Ca2+ decreased membrane fluidity and the pharmacokinetics in rats. These effects of Ca2+ on the membrane properties of E5531 particles could be eliminated by the addition of EDTA.
引用
收藏
页码:413 / 418
页数:6
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