title: Enhanced antisense effect of modified PNAs delivered through functional PMMA microspheres.
abstract: Peptide nucleic acids (PNA) are very promising antisense agents, but their in vivo application is often hampered by their low bioavailability, mainly due to their limited uptake through cellular and nuclear membranes. However, PNA chemical synthesis easily allows modification with functional structures able to improve the intrinsically low permeability and great interest is arising in finding specific and efficient delivery protocols. Polymeric core-shell microspheres with anionic functional groups on the surface were tested for their ability to reversibly bind lysine modified PNA sequences, whose antisense activity against COX-2 mRNA was already demonstrated in murine macrophages.
authors.affiliation: Institute of Biological Chemistry, University of Urbino, Italy. l.chiarantini@uniurb.it
authors.forename: Laura
authors.initials: L
authors.lastname: Chiarantini
authors.forename: Aurora
authors.initials: A
authors.lastname: Cerasi
authors.forename: Enrico
authors.initials: E
authors.lastname: Millo
authors.forename: Katia
authors.initials: K
authors.lastname: Sparnacci
authors.forename: Michele
authors.initials: M
authors.lastname: Laus
authors.forename: Massimo
authors.initials: M
authors.lastname: Riccio
authors.forename: Spartaco
authors.initials: S
authors.lastname: Santi
authors.forename: Marco
authors.initials: M
authors.lastname: Ballestri
authors.forename: Silvia
authors.initials: S
authors.lastname: Spaccasassi
authors.forename: Luisa
authors.initials: L
authors.lastname: Tondelli
mesh_terms: D000180:Acrylic Resins; D000818:Animals; D016375:Antisense Elements (Genetics); D001682:Biological Availability; D051546:Cyclooxygenase 2 / Q000096:biosynthesis / Q000235:genetics; D005079:Excipients; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D018613:Microscopy, Confocal; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D020135:Peptide Nucleic Acids / Q000008:administration & dosage* / Q000494:pharmacology* / Q000633:toxicity; D019904:Polymethyl Methacrylate; D012333:RNA, Messenger / Q000096:biosynthesis / Q000235:genetics; D013816:Thermodynamics
chemical_list: D000180:Acrylic Resins; D016375:Antisense Elements (Genetics); C446821:Eudragit L100-55; D005079:Excipients; D008070:Lipopolysaccharides; D020135:Peptide Nucleic Acids; D012333:RNA, Messenger; D019904:Polymethyl Methacrylate; D051546:Cyclooxygenase 2