| Lipid model membranes for drug interaction study. | |
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MedLine Citation:
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PMID: 16598469 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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L P Cavalcanti; O Konovalov; I L Torriani |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2006-04-06 |
Journal Detail:
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Title: European biophysics journal : EBJ Volume: 35 ISSN: 0175-7571 ISO Abbreviation: Eur. Biophys. J. Publication Date: 2006 May |
Date Detail:
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Created Date: 2006-04-28 Completed Date: 2006-12-26 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8409413 Medline TA: Eur Biophys J Country: Germany |
Other Details:
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Languages: eng Pagination: 431-8 Citation Subset: IM |
Affiliation:
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European Synchrotron Radiation Facility (ESRF), Grenoble Cedex, France. cavalcanti@esrf.fr |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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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