Impact of interfacial cholesterol-anchored polyethylene glycol on sterol-rich non-phospholipid liposomes

Autor: Michel Lafleur, Alejandro Nieto Orellana, Jean-Pierre Benoit, Zhong-Kai Cui, Katarina Edwards, Guillaume Bastiat
Přispěvatelé: Department of Physical and Analytical Chemistry, Uppsala University, Micro et Nanomédecines Biomimétiques (MINT), Université d'Angers (UA)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS)-Université Bretagne Loire (UBL), Micro et Nanomédecines Translationnelles (MINT), Université d'Angers (UA)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Ingénierie de la vectorisation particulaire, Université d'Angers (UA)-Institut National de la Santé et de la Recherche Médicale (INSERM), Center for Self-Assembled Chemical Structures (CSACS), Center for Self-Assembled Chemical Structures
Jazyk: angličtina
Rok vydání: 2014
Předmět:
Polyethylene glycol
Phospholipid
Palmitic Acid
02 engineering and technology
Pharmaco-kinetics
Physical Chemistry
Permeability
Analytical Chemistry
Polyethylene Glycols
Biomaterials
Rats
Sprague-Dawley
03 medical and health sciences
chemistry.chemical_compound
Colloid and Surface Chemistry
Palmitic acid
Amphiphile
PEG ratio
polycyclic compounds
Analytisk kemi
Animals
[CHIM]Chemical Sciences
ComputingMilieux_MISCELLANEOUS
030304 developmental biology
Fysikalisk kemi
0303 health sciences
Liposome
Active loading
Chromatography
Antibiotics
Antineoplastic
Cholesterol
technology
industry
and agriculture
[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences
021001 nanoscience & nanotechnology
Sterol
Surfaces
Coatings and Films
Electronic
Optical and Magnetic Materials
Calcein
chemistry
Doxorubicin
Nanovectors
Liposomes
lipids (amino acids
peptides
and proteins)
0210 nano-technology
Zdroj: Journal of Colloid and Interface Science
Journal of Colloid and Interface Science, Elsevier, 2014, 428, pp.111-120. ⟨10.1016/j.jcis.2014.04.031⟩
ISSN: 0021-9797
1095-7103
DOI: 10.1016/j.jcis.2014.04.031⟩
Popis: Hypothesis 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. Experiments 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. Findings 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.
Databáze: OpenAIRE
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