Enhanced antisense effect of modified PNAs delivered through functional PMMA microspheres

Laura Chiarantini, Aurora Cerasi, Enrico Millo, Katia Sparnacci, Michele Laus, Massimo Riccio, Spartaco Santi, Marco Ballestri, Silvia Spaccasassi, Luisa Tondelli

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)83-91
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume324
Issue number1
DOIs
Publication statusPublished - Oct 31 2006

Keywords

  • Antisense therapy
  • Ciclooxigenase-2 (COX-2)
  • Core-shell microspheres
  • Macrophages
  • Peptide nucleic acids (PNA)
  • PMMA microspheres

ASJC Scopus subject areas

  • Pharmaceutical Science

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