Chemical hydrolysis of DOTAP and DOPE in a liposomal environment

In this study the hydrolysis kinetics of 1,2-dipalmitoyl- sn-glycero-3-phosphocholine (DPPC), 1,2-dioleoyl- sn-glycero-3-phosphoethanolamine (DOPE) and 1,2-dioleoyltrimethylammoniumpropane (DOTAP) in net neutral DPPC–DOPE (3:1, mol/mol) and cationic DOTAP–DOPE (1:1, mol/mol) liposomes are described....

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Bibliographic Details
Published in:Journal of controlled release 2002-02, Vol.79 (1), p.299-303
Main Authors: Vernooij, E.A.A.M, Kettenes-van den Bosch, J.J, Underberg, W.J.M, Crommelin, D.J.A
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cationic liposomes
DOPE
DOTAP
Drug Carriers - pharmacokinetics
Fatty Acids, Monounsaturated - metabolism
Fatty Acids, Monounsaturated - pharmacokinetics
Fluorescent Dyes - metabolism
Fluorescent Dyes - pharmacokinetics
General pharmacology
Hydrolysis
Liposomes - pharmacokinetics
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Phosphatidylethanolamines - metabolism
Phosphatidylethanolamines - pharmacokinetics
Phospholipids
Quaternary Ammonium Compounds - metabolism
Quaternary Ammonium Compounds - pharmacokinetics
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Summary:In this study the hydrolysis kinetics of 1,2-dipalmitoyl- sn-glycero-3-phosphocholine (DPPC), 1,2-dioleoyl- sn-glycero-3-phosphoethanolamine (DOPE) and 1,2-dioleoyltrimethylammoniumpropane (DOTAP) in net neutral DPPC–DOPE (3:1, mol/mol) and cationic DOTAP–DOPE (1:1, mol/mol) liposomes are described. The log k obs–pH profile for DOTAP–DOPE liposomes differs markedly from earlier observed hydrolysis profiles: the slope approaches zero in the acidic region and +1 in the alkaline region. The concept of amine-influenced hydrolysis is introduced to explain the lack of pH dependency in the acidic region of the log k obs–pH profiles.
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(01)00534-X