title: Fluorinated phosphatidylcholine-based liposomes: H+/Na+ permeability, active doxorubicin encapsulation and stability, in human serum.
abstract: The active encapsulation of doxorubicin (DOX) into fluorinated liposomes, the stability of these liposomes with respect to encapsulated DOX release in buffer and in human serum, and their H+/Na+ membrane permeability have been investigated and compared to those of their conventional hydrogenated analogues. These fluorinated liposomes are made from highly fluorinated phosphatidylcholines and contain a fluorinated core within their membrane. We found that the presence of this fluorinated core is not a barrier for the active encapsulation of DOX. Efficient (> 90%) and stable loading could be achieved using a transmembrane ammonium sulfate or even, in the absence of Na+, a transmembrane pH gradient. The higher H+/Na+ permeability found for the fluorinated membranes, as compared to conventional ones, is responsible for the lower stability observed for the DOX-loaded fluorinated liposomes when incubated in a physiological buffer (PBS) or in human serum. It is also noticeable that the retention of DOX is increased in human serum and for the liposomes whose membranes are in a gel or in a semi-fluid semi-gel state at 37 degrees C.
authors.affiliation: Laboratoire de Chimie Moléculaire, URA 426 au CNRS, Faculté des Sciences, Université de Nice-Sophia Antipolis, Nice, France.
authors.forename: F
authors.initials: F
authors.lastname: Frézard
authors.forename: C
authors.initials: C
authors.lastname: Santaella
authors.forename: M J
authors.initials: MJ
authors.lastname: Montisci
authors.forename: P
authors.initials: P
authors.lastname: Vierling
authors.forename: J G
authors.initials: JG
authors.lastname: Riess
mesh_terms: D004317:Doxorubicin / Q000008:administration & dosage / Q000097:blood; D004337:Drug Carriers; D004355:Drug Stability; D005461:Fluorine; D006801:Humans; D006859:Hydrogen / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000737:chemistry*; D010539:Permeability; D010713:Phosphatidylcholines / Q000737:chemistry*; D012964:Sodium / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D010713:Phosphatidylcholines; D005461:Fluorine; D006859:Hydrogen; D004317:Doxorubicin; D012964:Sodium