Enhanced antisense effect of modified PNAs delivered through functional PMMA microspheres

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 structu...

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Bibliographic Details
Published in:International journal of pharmaceutics 2006-10, Vol.324 (1), p.83-91
Main Authors: Chiarantini, Laura, Cerasi, Aurora, Millo, Enrico, Sparnacci, Katia, Laus, Michele, Riccio, Massimo, Santi, Spartaco, Ballestri, Marco, Spaccasassi, Silvia, Tondelli, Luisa
Format: Article
Language:English
Subjects:
Acrylic Resins
Animals
Antisense Elements (Genetics)
Antisense therapy
Biological and medical sciences
Biological Availability
Ciclooxigenase-2 (COX-2)
Core-shell microspheres
Cyclooxygenase 2 - biosynthesis
Cyclooxygenase 2 - genetics
Excipients
General pharmacology
Hydrogen-Ion Concentration
In Vitro Techniques
Lipopolysaccharides - pharmacology
Macrophages
Macrophages - drug effects
Macrophages - metabolism
Medical sciences
Mice
Microscopy, Confocal
Microscopy, Electron, Scanning
Microspheres
Particle Size
Peptide nucleic acids (PNA)
Peptide Nucleic Acids - administration & dosage
Peptide Nucleic Acids - pharmacology
Peptide Nucleic Acids - toxicity
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
PMMA microspheres
Polymethyl Methacrylate
RNA, Messenger - biosynthesis
RNA, Messenger - genetics
Thermodynamics
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Description
Summary: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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2006.07.007