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

Author: Asai Yasuyuki  

Publisher: VSP

ISSN: 1568-5527

Source: Advanced Powder Technology, Vol.16, Iss.4, 2005-08, pp. : 413-418

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

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Abstract

To obtain information on the effects of a divalent cation (Ca2+) on the membrane properties of the lipid A analog, E5531, the particle size,  potential, membrane fluidity and pharmacokinetices was investigated in rats after the addition of calcium ion. Within a molar ratio for [Ca2+]/[E5531]  3, the presence of Ca2+ increased the  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.