title: Gantrez AN as a new polymer for the preparation of ligand-nanoparticle conjugates.
abstract: The aim of this study was to evaluate the feasibility and in vitro activity of ligand-conjugates based on the use of poly(methyl vinyl ether-co-maleic anhydride) (PVM/MA or Gantrez AN). Fluorescently labelled PVM/MA nanoparticles were prepared by desolvation and cross-linkage with 1,3-diaminopropane (DP). Conjugates were obtained by incubation between the carriers and Sambucus nigra agglutinin (SNA) for 1 h in an aqueous medium. The lectin binding to the surface of nanoparticles was increased by both increasing the bulk ligand concentration and decreasing the amount of cross-linker. However, a concentration of about 0.3-0.4 mg DP per mg polymer was necessary to obtain maximum agglutination activity. Under optimal conditions, the amount of fixed ligand was 46 microg/mg nanoparticle (binding efficiency of 86%); although the activity of SNA conjugates was 13.3 microg/mg particle. The activity of nanoparticles, measured by the association to Caco-2 monolayers, was higher when SNA was covalently bound onto their surface. The lectin-conjugate interaction was 6-fold higher than conventional nanoparticles. Moreover, energy-dependent mechanisms were only observed in SNA-PVM/MA particles. Finally, the decrease in association in the presence of lactose demonstrates that both SNA- and SNA-conjugate-binding was due to a true lectin-sugar interaction.
authors.affiliation: Centro Galénico, Universidad de Navarra, Apartado 177, C/Irunlarrea s/n, Pamplona, Spain.
authors.forename: P
authors.initials: P
authors.lastname: Arbós
authors.forename: M
authors.initials: M
authors.lastname: Wirth
authors.forename: M A
authors.initials: MA
authors.lastname: Arangoa
authors.forename: F
authors.initials: F
authors.lastname: Gabor
authors.forename: J M
authors.initials: JM
authors.lastname: Irache
mesh_terms: D000818:Animals; D018938:Caco-2 Cells; D002417:Cattle; D006801:Humans; D008024:Ligands; D008298:Maleates / Q000138:chemical synthesis* / Q000378:metabolism; D036103:Nanotechnology / Q000379:methods*; D037121:Plant Lectins / Q000378:metabolism; D011095:Polyethylenes / Q000378:metabolism; D011145:Polyvinyls / Q000138:chemical synthesis* / Q000378:metabolism; D054788:Ribosome Inactivating Proteins; D012710:Serum Albumin, Bovine / Q000378:metabolism
chemical_list: D008024:Ligands; D008298:Maleates; D037121:Plant Lectins; D011095:Polyethylenes; D011145:Polyvinyls; C050600:Sambucus nigra lectins; C058026:polyvinylmethoxyethylene-maleic anhydride copolymer; D012710:Serum Albumin, Bovine; C043105:poly(methyl vinyl ether-co-maleic anhydride); D054788:Ribosome Inactivating Proteins