title: Polyphosphonium polymers for siRNA delivery: an efficient and nontoxic alternative to polyammonium carriers.
abstract: A water-soluble polyphosphonium polymer was synthesized and directly compared with its ammonium analog in terms of siRNA delivery. The triethylphosphonium polymer shows transfection efficiency up to 65% with 100% cell viability, whereas the best result obtained for the ammonium analog reaches only 25% transfection with 85% cell viability. Moreover, the nature of the alkyl substituents on the phosphonium cations is shown to have an important influence on the transfection efficiency and toxicity of the polyplexes. The present results show that the use of positively charged phosphonium groups is a worthy choice to achieve a good balance between toxicity and transfection efficiency in gene delivery systems.
authors.affiliation: College of Chemistry, University of California, Berkeley, California 94720-1460, USA.
authors.forename: Cátia
authors.initials: C
authors.lastname: Ornelas-Megiatto
authors.forename: Peter R
authors.initials: PR
authors.lastname: Wich
authors.forename: Jean M J
authors.initials: JM
authors.lastname: Fréchet
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D016503:Drug Delivery Systems; D004353:Drug Evaluation, Preclinical; D006367:HeLa Cells; D006801:Humans; D008954:Models, Biological; D009943:Organophosphorus Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011108:Polymers / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000644:Quaternary Ammonium Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D034741:RNA, Small Interfering / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004337:Drug Carriers; D009943:Organophosphorus Compounds; D011108:Polymers; D000644:Quaternary Ammonium Compounds; D034741:RNA, Small Interfering