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Formulations for natural and peptide nucleic acids based on cationic polymeric submicron particles

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Abstract

This article describes the production and characterization of cationic submicron particles constituted with Eudragit RS 100, plus different cationic surfactants, such as dioctadecyl-dimethyl-ammonium bromide (DDAB18) and diisobutyphenoxyethyl-dimethylbenzyl ammonium chloride (DEBDA), as a transport and delivery system for DNA/DNA and DNA/peptide nucleic acid (PNA) hybrids and PNA-DNA chimeras. Submicron particles could offer advantages over other delivery systems because they maintain unaltered physicochemical properties for long time periods, allowing long-term storage, and are suitable for industrial production. Submicron particles were characterized in terms of size, size distribution, morphology, and zeta potential. Moreover, the in vitro activity and ability of submicron particles to complex different types of nucleic acids were described. Finally, the ability of submicron particles to deliver functional genes to cells cultured in vitro was determined by a luciferase activity assay, demonstrating that submicron particles possess superior transfection efficiency with respect to commercially available, liposome-based transfection kits.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy

    Rita Cortesi

  2. Department of Biochemistry and Molecular Biology, University of Ferrara, Ferrara, Italy

    Carlo Mischiati, Monica Borgatti, Laura Breda & Roberto Gambari

  3. Institute of Biostructure and Bioimaging, CNR, Napoli, Italy

    Alessandra Romanelli, Michele Saviano & Carlo Pedone

  4. Laboratory for the Development of Pharmacological and Pharmacogenomic Therapy of Thalassemia, Biotechnology Centre, University of Ferrara, Italy

    Roberto Gambari

  5. Department of Pharmaceutical Chemistry and Technology, University of Perugia Dipartimento di Chimica e Tecnologia del Farmaco, via del Liceo, 06100, Perugia, Italy

    Claudio Nastruzzi (Associated Professor in Pharmaceutics)

Authors
  1. Rita Cortesi
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  2. Carlo Mischiati
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  3. Monica Borgatti
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  4. Laura Breda
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  5. Alessandra Romanelli
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  6. Michele Saviano
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  7. Carlo Pedone
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  8. Roberto Gambari
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  9. Claudio Nastruzzi
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Corresponding author

Correspondence to Claudio Nastruzzi.

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Published: January 20, 2003

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Cortesi, R., Mischiati, C., Borgatti, M. et al. Formulations for natural and peptide nucleic acids based on cationic polymeric submicron particles. AAPS J 6, 2 (2004). https://doi.org/10.1208/ps060102

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  • DOI: https://doi.org/10.1208/ps060102

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