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

摘要

To obtain information on the effects of a divalent cation (Ca~(2+)) on the membrane properties of the lipid A analog,E5531,the particle size,f potential,membrane fluidity and pharmacokinetices was investigated in rats after the addition of calcium ion.Within a molar ratio for [Ca~(2+)]/[E5531] <= 3,the presence of Ca~(2+) increased the f potentials of the E5531 membrane,but had no effect on particle size.Ca~(2+) decreased membrane fluidity and the pharmacokinetics in rats.These effects of Ca~(2+) on the membrane properties of E5531 particles could be eliminated by the addition of EDTA.