Document Detail

Effect of beta-sitosterol concentration and high pressure homogenization on the chlorhexidine release from vesicular gels.
MedLine Citation:
PMID:  16257155     Owner:  NLM     Status:  MEDLINE    
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.
E Farkas; R Schubert; R Zelkó
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Publication Detail:
Type:  Journal Article     Date:  2005-10-27
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  307     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2006 Jan 
Date Detail:
Created Date:  2005-12-12     Completed Date:  2006-04-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  51-5     Citation Subset:  IM    
Pharmaceutical Institute, Semmelweis University, Hogyes E. Street 7, 1092 Budapest, Hungary.
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MeSH Terms
Anti-Infective Agents, Local / chemistry*
Antilipemic Agents / chemistry*
Calorimetry, Differential Scanning
Chlorhexidine / chemistry*
Delayed-Action Preparations
Drug Compounding / methods*
Lipid Bilayers / chemistry
Microscopy, Electron, Transmission
Sitosterols / chemistry*
Reg. No./Substance:
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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