title: Enhanced transfection rates of small-interfering RNA using dioleylglutamide-based magnetic lipoplexes.
abstract: Magnetic force-guided delivery (magnetofection) has been studied as a new modality for introducing small-interfering RNA (siRNA) into target cells, but its delivery efficiency needs to be improved. Here, we report that magnetofection of N,N''-dioleylglutamide (DG)-based magnetic lipoplexes can substantially enhance the cellular delivery rates of siRNA. The siRNA was triply complexed with DG-based cationic liposomes and cationic iron-oxide nanoparticles. The formation of siRNA-containing magnetic lipoplexes was confirmed by gel retardation, sizes, and zeta potential values. Fluorescence microscopy and flow cytometry of fluorescent marker-labeled siRNA revealed that the DG-based magnetic lipoplexes conferred a higher cellular delivery rate of siRNA than DG-based lipoplexes or Lipofectamine 2000. In addition to the enhanced delivery of siRNA, the DG-based magnetic lipoplexes showed lack of cytotoxicity. We then tested the application of these magnetic lipoplexes for the cellular delivery of anticancer siRNA. Cancer cell lines magnetofected with DG-based magnetic lipoplexes containing Mcl1-specific siRNA (siMcl1) showed much lower viability than the groups treated with DG-based lipoplexes or Lipofectamine 2000, indicating that our magnetofection strategy conferred greater siMcl1-induced anticancer activity. These results suggest that DG-based magnetic lipoplexes are promising candidates for enhancing the efficiency of magnetic field-guided siRNA delivery.
authors.affiliation: Department of Molecular Medicine and Biopharmaceutical Sciences, Graduate School of Convergence Science and Technology, Seoul National University, Seoul, South Korea.
authors.forename: Soondong
authors.initials: S
authors.lastname: Lee
authors.forename: Gayong
authors.initials: G
authors.lastname: Shim
authors.forename: Sunil
authors.initials: S
authors.lastname: Kim
authors.forename: Young Bong
authors.initials: YB
authors.lastname: Kim
authors.forename: Chan-Wha
authors.initials: CW
authors.lastname: Kim
authors.forename: Youngro
authors.initials: Y
authors.lastname: Byun
authors.forename: Yu-Kyoung
authors.initials: YK
authors.lastname: Oh
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival; D005973:Glutamine / Q000031:analogs & derivatives* / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D055666:Lipopeptides / Q000737:chemistry*; D008081:Liposomes; D058185:Magnetite Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D064549:Myeloid Cell Leukemia Sequence 1 Protein; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000235:genetics; D034741:RNA, Small Interfering / Q000008:administration & dosage* / Q000737:chemistry; D014162:Transfection / Q000379:methods*
chemical_list: D055666:Lipopeptides; D008081:Liposomes; D058185:Magnetite Nanoparticles; D064549:Myeloid Cell Leukemia Sequence 1 Protein; C547520:N,N'-dioleylglutamide; D019253:Proto-Oncogene Proteins c-bcl-2; D034741:RNA, Small Interfering; D005973:Glutamine