title: Anionic pH-Sensitive Lipoplexes.
abstract: To provide long circulating nanoparticles able to carry a gene to tumors, we have designed anionic pegylated lipoplexes which are pH sensitive. Anionic pegylated lipoplexes have been prepared from the combined formulation of cationic lipoplexes and pegylated anionic liposomes. The neutralization of the particle surface charge as a function of the pH was monitored by light scattering in order to determine the ratio between anionic and cationic lipids that would give pH sensitive complexes. This ratio has been optimized to form particles sensitive to pH change in the range 5.5-6.5. Compaction of DNA into these newly formed anionic complexes is checked by DNA accessibility to picogreen. The transfection efficiency and pH sensitive property of these formulations has been shown in vitro using bafilomycin, a vacuolar H+-ATPase inhibitor.
authors.affiliation: Chimie ParisTech, PSL Research University, Unité de Technologies Chimiques et Biologiques pour la Santé (UTCBS), F-75005 Paris, France. nathalie.mignet@parisdescartes.fr.|CNRS, UTCBS UMR 8258, F-75006, Paris, France. nathalie.mignet@parisdescartes.fr.|Université Paris Descartes, Sorbonne-Paris-Cité, UTCBS, F-75006, Paris, France. nathalie.mignet@parisdescartes.fr.|INSERM, UTCBS U 1022, F-75006, Paris, France. nathalie.mignet@parisdescartes.fr.
authors.forename: Nathalie
authors.initials: N
authors.lastname: Mignet
authors.affiliation: Chimie ParisTech, PSL Research University, Unité de Technologies Chimiques et Biologiques pour la Santé (UTCBS), F-75005 Paris, France.|CNRS, UTCBS UMR 8258, F-75006, Paris, France.|Université Paris Descartes, Sorbonne-Paris-Cité, UTCBS, F-75006, Paris, France.|INSERM, UTCBS U 1022, F-75006, Paris, France.
authors.forename: Daniel
authors.initials: D
authors.lastname: Scherman
mesh_terms: D000818:Animals; D000838:Anions; D002412:Cations; D045744:Cell Line, Tumor; D004247:DNA / Q000378:metabolism; D005453:Fluorescence; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000737:chemistry*; D051379:Mice; D011092:Polyethylene Glycols / Q000737:chemistry; D055672:Static Electricity; D014162:Transfection
chemical_list: D000838:Anions; D002412:Cations; D008081:Liposomes; D011092:Polyethylene Glycols; D004247:DNA
keywords: Anionic cholesterol; Anionic lipoplexes; Gene delivery to tumor; Pegylated lipoplexes; pH-sensitive lipoplexes