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Impact of interfacial cholesterol-anchored polyethylene glycol on sterol-rich non-phospholipid liposomes
Department of Chemistry, Centre for Self-Assembled Chemical Structures (CSACS), Université de Montréal, Canada.
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Analytical Chemistry.
INSERM U1066, Micro et Nanomédecines Biomimétiques-MINT, France AND LUNAM Université, UMR-S1066, Angers F-49933, France.
INSERM U1066, Micro et Nanomédecines Biomimétiques-MINT, France AND LUNAM Université, UMR-S1066, Angers F-49933, France.
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2014 (English)In: Journal of Colloid and Interface Science, ISSN 0021-9797, E-ISSN 1095-7103, Vol. 428, 111-120 p.Article in journal (Refereed) Published
Abstract [en]


Liposomes made of single-chain amphiphiles and a large amount of sterols display several advantages including a limited permeability. In the present paper, we examine the possibility to prepare such non-phospholipid liposomes with interfacial polyethylene glycol (PEG) in order to improve their circulation in the blood stream. Cholesterol (Chol) was chosen as the PEG anchor.


The phase behavior of mixtures of palmitic acid (PA) and cholesterol including various proportions of PEGylated cholesterol (PEG-Chol) was characterized. In conditions leading to the formation of fluid bilayers, properties of the resulting liposomes were assessed.


Up to 20 mol% of PEGylated cholesterol could be introduced without significant perturbations in fluid bilayers made of PA and cholesterol. With 10 mol% PEG-Chol, PA/Chol/PEG-Chol liposomes showed a very limited permeability to calcein and doxorubicin. Doxorubicin could be actively loaded in PA/Chol/PEG-Chol liposomes with a high drug loading efficiency and a high drug to lipid ratio. Pharmaco-kinetic experiments in rats indicated that interfacial PEG reduced the clearance of PA/Chol liposomes compared to the naked ones. However the lifetime of these non-phospholipid liposomes in the blood circulation was considerably shorter than that observed for control PEGylated phospholipid liposomes, a phenomenon associated with the negative interfacial charge of the PA/Chol/PEG-Chol liposomes. 

Place, publisher, year, edition, pages
2014. Vol. 428, 111-120 p.
Keyword [en]
Liposomes, Cholesterol, Palmitic acid, Polyethylene glycol, Nanovectors, Permeability, Pharmaco-kinetics, Active loading
National Category
Analytical Chemistry Physical Chemistry
URN: urn:nbn:se:uu:diva-223793DOI: 10.1016/j.jcis.2014.04.031ISI: 000337860800016OAI: oai:DiVA.org:uu-223793DiVA: diva2:714123
Available from: 2014-04-25 Created: 2014-04-25 Last updated: 2014-07-25Bibliographically approved

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