title: Cationic switchable lipids: pH-triggered molecular switch for siRNA delivery.
abstract: A pH-sensitive molecular switch able to change its conformation upon protonation at endosomal pH values is embedded into the structure of cationic lipidoid materials, thus conferring endosomal escape properties. Involvement of the conformational switch in the endosomal escape process was confirmed and leading material identified was able to induce efficient gene knockdown both in vitro and in vivo. The lipid nanoparticles reported here are promising for therapeutic applications and this work could serve as a template for future design of stimulus-responsive (ionic, redox, light) molecular switch for drug and gene delivery.
authors.affiliation: Faculty of Pharmacy, University of Montreal, P.O. Box 6128, Downtown Station, Montreal, QC, Canada. jeanne.leblond-chain@umontreal.ca.
authors.forename: W
authors.initials: W
authors.lastname: Viricel
authors.forename: S
authors.initials: S
authors.lastname: Poirier
authors.forename: A
authors.initials: A
authors.lastname: Mbarek
authors.forename: R M
authors.initials: RM
authors.lastname: Derbali
authors.forename: G
authors.initials: G
authors.lastname: Mayer
authors.forename: J
authors.initials: J
authors.lastname: Leblond
mesh_terms: D000818:Animals; D002412:Cations; D055785:Gene Knockdown Techniques; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008055:Lipids / Q000737:chemistry*; D008297:Male; D051379:Mice; D053758:Nanoparticles; D034741:RNA, Small Interfering / Q000008:administration & dosage* / Q000235:genetics
chemical_list: D002412:Cations; D008055:Lipids; D034741:RNA, Small Interfering