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微量热法和 Zeta 电位研究药物与脂质体的结合。

Microcalorimetric and zeta potential study on binding of drugs on liposomes.

机构信息

Aalto University, School of Science and Technology, Department of Chemistry, PO Box 16100, FI-00076 Aalto, Finland.

出版信息

Colloids Surf B Biointerfaces. 2010 Jul 1;78(2):275-82. doi: 10.1016/j.colsurfb.2010.03.017. Epub 2010 Mar 27.

Abstract

In this work, isothermal titration calorimetry (ITC) combined with zeta potential measurements was used to study the binding and partitioning of three beta-blockers, alprenolol, labetalol and propranolol, and the local anaesthetic tetracaine into liposomes. The thermodynamic parameters of enthalpy, entropy, the Gibbs energy and the binding constant were determined using the one site model. Furthermore, the binding constants corrected for the electrostatic contribution were used to assess the partition coefficients for the drugs. Also, the effect of the concentration, ionic strength, temperature and membrane curvature on the interaction was included in the evaluation.

摘要

在这项工作中,使用等温热力学滴定法(ITC)结合动电电势测量法来研究三种β受体阻滞剂(阿普洛尔、拉贝洛尔和普萘洛尔)和局部麻醉剂(盐酸丁卡因)与脂质体的结合和分配。使用单点模型确定了焓、熵、吉布斯自由能和结合常数的热力学参数。此外,还使用校正静电贡献的结合常数来评估药物的分配系数。此外,还包括浓度、离子强度、温度和膜曲率对相互作用的影响的评估。

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