title: Efficient serum-resistant lipopolyplexes targeted to the folate receptor.
abstract: In this work, we have developed and evaluated a new targeted lipopolyplex (LPP), by combining polyethylenimine (PEI), 1,2-dioleoyl-3-(trimethylammonium) propane (DOTAP)/Chol liposomes, the plasmids pCMVLuc/pCMVIL-12, and the ligand folic acid (FA), able to transfect HeLa and B16-F10 cells in the presence of very high concentration of serum (60% FBS). These complexes (Fol-LPP) have a net positive surface charge. The combination of folic acid with lipopolyplexes also enhanced significantly the transfection activity of the therapeutic gene interleukin-12 (IL-12), without any significant cytotoxicity. The specificity of the folate receptor (FR)-mediated gene transfer was corroborated by employing a folate receptor deficient cell line (HepG2). This formulation improved gene delivery showed by conventional lipoplexes or polyplexes resulting an efficient, simple, and nontoxic method for gene delivery of therapeutic genes in vitro and very probably in vivo.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Navarra, Pamplona, Spain. kurbiola@alumni.unav.es
authors.forename: Koldo
authors.initials: K
authors.lastname: Urbiola
authors.forename: Leire
authors.initials: L
authors.lastname: García
authors.forename: Sara
authors.initials: S
authors.lastname: Zalba
authors.forename: María J
authors.initials: MJ
authors.lastname: Garrido
authors.forename: Conchita
authors.initials: C
authors.lastname: Tros de Ilarduya
mesh_terms: D000818:Animals; D001769:Blood; D045744:Cell Line, Tumor; D058973:Folate Receptors, GPI-Anchored / Q000187:drug effects*; D005492:Folic Acid / Q000737:chemistry; D006801:Humans; D018664:Interleukin-12 / Q000235:genetics / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry* / Q000494:pharmacology; D010316:Particle Size; D014162:Transfection
chemical_list: D058973:Folate Receptors, GPI-Anchored; D008055:Lipids; D018664:Interleukin-12; D005492:Folic Acid