Journal
LANGMUIR
Volume 25, Issue 2, Pages 1086-1090Publisher
AMER CHEMICAL SOC
DOI: 10.1021/la803288s
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Funding
- Australian Microscopy and Microanalysis Research Facitity (AMMRF)
- Flinders University
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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 similar to 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.
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