Rapid determination of liposome-water partition coefficients (Klw) using liposome electrokinetic chromatography (LEKC)

被引:84
作者
Burns, ST [1 ]
Khaledi, MG [1 ]
机构
[1] N Carolina State Univ, Dept Chem, Raleigh, NC 27696 USA
关键词
LEKC; liposome-water partition coefficients; octanol-water partition coefficients;
D O I
10.1002/jps.10119
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Liposome Electrokinetic Chromatography (LEKC) provides a simple and facile approach for determining liposome-water partition coefficients, K-lw. LEKC is a Capillary Electrophoresis (CE) technique where liposomes are incorporated into a buffer solution and act as a pseudostationary phase providing sites of interaction for solutes. The retention factors of solutes in LEKC are directly proportional to K-lw. This article describes how LEKC can be used to determine K-lw. for both neutral and charged solutes. The K-lw values for a group of neutral aromatic compounds, beta-blockers, and other drugs are reported. In addition, the usefulness of two quantitative structure partition relationships (QSPR) for estimation of K-lw is demonstrated. One is the logarithmic linear relationship between liposome water and octanol-water partition coefficients (P-ow). The other is the Linear Solvation Energy Relationship (LSER). The calculated K-lw, values from the two QSPR agree nicely with the observed values and with one another. (C) 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association.
引用
收藏
页码:1601 / 1612
页数:12
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