Rapid determination of liposome-water partition coefficients (Klw) using liposome electrokinetic chromatography (LEKC)
Rapid determination of liposome-water partition coefficients (Klw) using liposome electrokinetic chromatography (LEKC)
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DOI：
10.1002/jps.10119
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发表时间：
2002-07-01
影响因子：
3.8
通讯作者：
Khaledi, MG
中科院分区：
文献类型：
--
作者：
Burns, ST;Khaledi, MG
脂质体电动色谱 (LEKC) 提供了一种简单便捷的方法来确定脂质体-水分配系数 K-lw。 LEKC 是一种毛细管电泳 (CE) 技术，其中脂质体被掺入缓冲溶液中并充当伪固定相，为溶质提供相互作用位点。 LEKC 中溶质的保留因子与 K-lw 成正比。本文介绍如何使用 LEKC 来确定 K-lw。对于中性和带电溶质。报告了一组中性芳香族化合物、β-阻滞剂和其他药物的 K-lw 值。此外，还证明了两种定量结构划分关系 (QSPR) 对于 K-lw 估计的有用性。一是脂质体水与辛醇-水分配系数（P-ow）之间的对数线性关系。另一种是线性溶剂化能关系（LSER）。两个 QSPR 计算出的 K-lw 值与观测值以及彼此之间非常一致。 (C) 2002 Wiley-Liss, Inc. 和美国制药协会。
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.