title: Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery.
abstract: We report the synthesis and study of fluorocarbon (FC) modified polyethylenimine (PEI) for the purpose of siRNA delivery. Low-molecular-weight PEI (Mn = 600) was functionalized with fluorocarbon epoxides of varying length. All FC-modified samples with greater than 2.0 equiv of FC epoxide per PEI induced potent gene silencing in vitro. Compared to hydrocarbon (HC) analogues, the FC vectors showed greater general silencing efficacy, higher cell uptake, and reduced association with serum components. Collectively, the data suggest that modification of polyamines with FCs is a promising approach for the discovery of novel vectors for siRNA delivery.
authors.affiliation: Department of Chemistry, University of California , Irvine, California 92697, United States.
authors.forename: Mark E
authors.initials: ME
authors.lastname: Johnson
authors.affiliation: Department of Chemistry, University of California , Irvine, California 92697, United States.
authors.forename: Judy
authors.initials: J
authors.lastname: Shon
authors.affiliation: Department of Chemistry, University of California , Irvine, California 92697, United States.
authors.forename: Brian M
authors.initials: BM
authors.lastname: Guan
authors.affiliation: Department of Chemistry & Biochemistry, University of California, San Diego , La Jolla, California 92093, United States.
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Patterson
authors.affiliation: Department of Chemistry, University of California , Irvine, California 92697, United States.
authors.forename: Nathan J
authors.initials: NJ
authors.lastname: Oldenhuis
authors.affiliation: Department of Chemistry, University of California , Irvine, California 92697, United States.
authors.forename: Alexander C
authors.initials: AC
authors.lastname: Eldredge
authors.affiliation: Department of Chemistry & Biochemistry, University of California, San Diego , La Jolla, California 92093, United States.
authors.forename: Nathan C
authors.initials: NC
authors.lastname: Gianneschi
authors.affiliation: Department of Chemistry, University of California , Irvine, California 92697, United States.
authors.forename: Zhibin
authors.initials: Z
authors.lastname: Guan
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D005466:Fluorocarbons / Q000737:chemistry*; D020868:Gene Silencing; D057809:HEK293 Cells; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D008970:Molecular Weight; D041681:NIH 3T3 Cells; D009690:Nucleic Acid Conformation; D011094:Polyethyleneimine / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000737:chemistry* / Q000235:genetics
chemical_list: D004337:Drug Carriers; D005466:Fluorocarbons; D034741:RNA, Small Interfering; D011094:Polyethyleneimine