Document Detail


Lipid model membranes for drug interaction study.
MedLine Citation:
PMID:  16598469     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The present work shows a structural study on the process of incorporation of a hydrophobic drug, Ellipticine (ELPT), into lipid model membranes for drug targeting purpose. The ELPT is an alkaloid that showed an anti-proliferation activity against several types of tumor cells and against the HIV1 virus. We used the zwitterionic lipid dipalmitoyl phosphatidylcholine (DPPC) and four different anionic lipids: cardiolipin (CL), dipalmitoyl phosphatidic acid (DPPA), dipalmitoyl phosphatidylglycerol (DPPG) and dipalmitoyl phosphatidylserine (DPPS), both spread on a Langmuir monolayer and deposited on a solid substrate to mimic a model membrane and study the interaction with the drug ELPT. X-ray reflectivity results pointed toward an increase in drug loading efficiency up to 13.5% mol/mol of ELPT into mixed systems DPPC/CL. This increase in loading efficiency was also accompanied by a slight distortion in the stacking of the bilayers less evidenced after optimization of the molar ratio between the co-lipids. Grazing incidence X-ray diffraction measurements revealed an in-plane lattice distortion due to the presence of hydrocarbon chain backbone ordering in pure systems of DPPC doped with ELPT. The same was not observed in mixed membranes with DPPC/CL and DPPC/DPPA.
Authors:
L P Cavalcanti; O Konovalov; I L Torriani
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-04-06
Journal Detail:
Title:  European biophysics journal : EBJ     Volume:  35     ISSN:  0175-7571     ISO Abbreviation:  Eur. Biophys. J.     Publication Date:  2006 May 
Date Detail:
Created Date:  2006-04-28     Completed Date:  2006-12-26     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8409413     Medline TA:  Eur Biophys J     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  431-8     Citation Subset:  IM    
Affiliation:
European Synchrotron Radiation Facility (ESRF), Grenoble Cedex, France. cavalcanti@esrf.fr
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MeSH Terms
Descriptor/Qualifier:
Computer Simulation
Drug Delivery Systems / methods*
Drug Design*
Ellipticines / chemistry*
Lipid Bilayers / chemistry*
Membrane Fluidity*
Models, Chemical*
Models, Molecular
Phospholipids / chemistry*
Chemical
Reg. No./Substance:
0/Ellipticines; 0/Lipid Bilayers; 0/Phospholipids; 519-23-3/ellipticine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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