| Effect of beta-sitosterol concentration and high pressure homogenization on the chlorhexidine release from vesicular gels. | |
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MedLine Citation:
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PMID: 16257155 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Previous studies have confirmed that the phase transition of vesicular gels of hydrogenated phospholipids to the less ordered fluid vesicular state was induced by the increase of the beta-sitosterol ratio in the whole gel system and consequently in the lipid bilayer. The purpose of the present study was to evaluate the influence of the beta-sitosterol portion in the lipid bilayer and the effect of high pressure homogenization on the structural characteristics of the prepared gel systems. In addition the influence of beta-sitosterol on the consequent chlorhexidine release from the obtained vesicles and liposomes was also examined. Lipid mixtures were prepared from different molar ratios of lecithin:sterol components (90:10-65:35 mol%). The obtained mixtures were hydrated with the aqueous solution of chlorhexidine digluconate in order to achieve a 30% (w/w) final concentration of the lipid mixtures and a 4% (w/w) concentration of the drug. One portion of the resultant multilamellar vesicles was homogenized by using high pressure. To characterize the homogenized and non-homogenized systems, transmission electron microscopy of the freeze-fractured samples and differential scanning calorimetry (DSC) were carried out. A vertical type diffusion cell was applied to determine the amount of released chlorhexidine digluconate. Along with the increase in beta-sitosterol concentration, the fluidity of the membrane as well as its permeability also increased. The increased permeability--caused by the higher beta-sitosterol concentration--and the high pressure homogenization, which increased the dispersity and therefore the surface area, enabled a higher amount of chlorhexidine to be released. The increase of drug release was more pronounced in the case of samples prepared with high pressure homogenization. |
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Authors:
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E Farkas; R Schubert; R Zelkó |
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Publication Detail:
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Type: Journal Article Date: 2005-10-27 |
Journal Detail:
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Title: International journal of pharmaceutics Volume: 307 ISSN: 0378-5173 ISO Abbreviation: Int J Pharm Publication Date: 2006 Jan |
Date Detail:
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Created Date: 2005-12-12 Completed Date: 2006-04-13 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7804127 Medline TA: Int J Pharm Country: Netherlands |
Other Details:
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Languages: eng Pagination: 51-5 Citation Subset: IM |
Affiliation:
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Pharmaceutical Institute, Semmelweis University, Hogyes E. Street 7, 1092 Budapest, Hungary. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Infective Agents, Local
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chemistry* Antilipemic Agents / chemistry* Calorimetry, Differential Scanning Chlorhexidine / chemistry* Delayed-Action Preparations Drug Compounding / methods* Gels Lipid Bilayers / chemistry Liposomes* Microscopy, Electron, Transmission Sitosterols / chemistry* |
| Chemical | |
Reg. No./Substance:
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0/Anti-Infective Agents, Local; 0/Antilipemic Agents; 0/Delayed-Action Preparations; 0/Gels; 0/Lipid Bilayers; 0/Liposomes; 0/Sitosterols; 55-56-1/Chlorhexidine; 5779-62-4/sitosterol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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