title: PEGylated and non-PEGylated siRNA lipoplexes formulated with cholesteryl cytofectins promote efficient luciferase knockdown in HeLa tat luc cells.
abstract: Delivery of small interfering RNAs (siRNAs) remains a major challenge in their development for therapeutic applications, and cationic liposomes are being actively investigated for this purpose. Six liposome formulations containing the cytofectins 3β[N-(N ',N '-dimethylaminopropane)-carbamoyl] cholesterol (Chol-T) or 3β[N-(N ',N ',-dimethylaminopropylsuccinamidohydrazido)-carbamoyl] cholesterol (MS09) and varying amounts of distearoylphosphatidylethanolamine poly(ethylene glycol)2000, were prepared. Lipoplexes formed with siRNA were characterized by gel retardation analysis and cryo-electron microscopy. All lipoplexes exhibited low cytotoxicity in the HeLa tat luc cell line while Chol-T lipoplexes, containing anti-luciferase siRNA, achieved 93.4% knockdown of the luciferase transcript at 30 nM siRNA. Poly(ethylene glycol)2000 incorporation only marginally reduced knockdown efficiency.
authors.affiliation: Non-viral Gene Delivery Laboratory, Discipline of Biochemistry, University of KwaZulu-Natal, Durban, South Africa.
authors.forename: Aliscia
authors.initials: A
authors.lastname: Daniels
authors.forename: Moganavelli
authors.initials: M
authors.lastname: Singh
authors.forename: Mario
authors.initials: M
authors.lastname: Ariatti
mesh_terms: D002412:Cations; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology; D016503:Drug Delivery Systems; D055785:Gene Knockdown Techniques; D006367:HeLa Cells; D006801:Humans; D006834:Hydrazines / Q000737:chemistry* / Q000494:pharmacology; D008081:Liposomes / Q000737:chemistry / Q000494:pharmacology; D008156:Luciferases / Q000235:genetics*; D011092:Polyethylene Glycols / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D002412:Cations; D006834:Hydrazines; D008081:Liposomes; D034741:RNA, Small Interfering; C514134:cytofectin; D011092:Polyethylene Glycols; D002784:Cholesterol; D008156:Luciferases