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

doi:10.1016/j.ijpharm.2006.07.007

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

Istituti Ortopedici Rizzoli

Research output: Contribution to journal › Article › peer-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 language	English
Pages (from-to)	83-91
Number of pages	9
Journal	International Journal of Pharmaceutics
Volume	324
Issue number	1
DOIs	https://doi.org/10.1016/j.ijpharm.2006.07.007
Publication status	Published - 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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10.1016/j.ijpharm.2006.07.007

Cite this

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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.",

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AU - Chiarantini, Laura

AU - Cerasi, Aurora

AU - Millo, Enrico

AU - Sparnacci, Katia

AU - Laus, Michele

AU - Riccio, Massimo

AU - Santi, Spartaco

AU - Ballestri, Marco

AU - Spaccasassi, Silvia

AU - Tondelli, Luisa

PY - 2006/10/31

Y1 - 2006/10/31

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KW - Antisense therapy

KW - Ciclooxigenase-2 (COX-2)

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KW - PMMA microspheres

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Enhanced antisense effect of modified PNAs delivered through functional PMMA microspheres

Abstract

Keywords

ASJC Scopus subject areas

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