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Glycosylated liposomes against Helicobacter pylori: Behavior in acidic conditions
Authors:Pierre-Louis Bardonnet  Vincent Faivre  Paul Boullanger  Françoise Falson
Institution:a Laboratoire de Pharmacie Galénique Industrielle, ISPB - Université Lyon I, 8 Avenue Rockefeller, 69373 Lyon cedex 08, France
b Pharmapeptides, Campus Universitaire - Parc d’Affaires International, 74166 Archamps, France
c UMR CNRS 8612 - IFR 141, Université Paris-Sud XI, 5 rue J.B. Clément, 92296 Châtenay-Malabry, France
d ICBMS, Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, Chimie Organique 2 - Glycochimie, 43 boulevard du 11 novembre 1918, Villeurbanne F-69622, France; CNRS, UMR 5246, Villeurbanne F-69622, France; Université de Lyon, Lyon F-69622, France; Université Lyon 1, Lyon F-69622, France; INSA-Lyon, Villeurbanne F-69622, France; CPE Lyon, Villeurbanne F-69616, France
Abstract:Helicobacter pylori was isolated in 1982 and confirmed as a gastric pathogenic agent at the end of the 1980s. The present work deals with liposomes formulations in which are incorporated cholesteryl tetraethylene glycol oside as model ligands for H. pylori adhesins. This study is devoted to the behavior of liposomes in gastric conditions. The glycosylated vesicles are stable and the pH of the internal aqueous compartment remains close to 4 even through more acidic conditions are imposed to the external phase (pH 1.2-2). Such a pH gradient depends essentially on the nature of phospholipids used and is not extensively affected by the incorporation of the targeting agent. These aspects are particularly important to the development of liposome formulations against H. pylori, bacteria sensitive to antibiotics which are unstable in very acidic conditions.
Keywords:Liposome  Proton diffusion  Helicobacter pylori  pH  Glycolipid  Targeting
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