Kinetics Membrane Disruption Due to Drug Interactions of Chlorpromazine Hydrochloride

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• 作者：Matthew R. Nussio ; Matthew J. Sykes ; John O. Miners ; Joseph G. Shapter
• 刊名：Langmuir
• 出版年：2009
• 出版时间：January 20, 2009
• 年：2009
• 卷：25
• 期：2
• 页码：1086-1090
• 全文大小：190K
• 年卷期：v.25,no.2(January 20, 2009)
• ISSN：1520-5827

文摘

Drug−membrane interactions assume considerable importance in pharmacokinetics and drug metabolism. Here, we present the interaction of chlorpromazine hydrochloride (CPZ) with supported phospholipid bilayers. It was demonstrated that CPZ binds rapidly to phospholipid bilayers, disturbing the molecular ordering of the phospholipids. These interactions were observed to follow first order kinetics, with an activation energy of 420 kJ mol⁻¹. Time-dependent membrane disruption was also observed for the interaction with CPZ, such that holes appeared in the phospholipid bilayer after the interaction of CPZ. For this process of membrane disruption, “lag-burst” kinetics was demonstrated.