Synthesis of Water-soluble, Polyester-based Dendrimer Prodrugs for Exploiting Therapeutic Properties of Two Triterpenoid Acids

  • Silvana Alfei
  • Gaby Brice Taptue
  • Silvia Catena
  • Angela Bisio
Article
  • 11 Downloads

Abstract

Dendrimers are macromolecules characterized by high controlled size, shape and architecture, presence of inner cavities able to accommodate small molecules and many peripheral functional groups to bind target entities. They are of eminent interest for biomedical applications, including gene transfection, tissue engineering, imaging, and drug delivery. The well-known pharmacological activities of ursolic and oleanolic acids are limited by their small water solubility, non-specific cell distribution, low bioavailability, poor pharmacokinetics, and their direct administration could result in the release of thrombi. To overcome such problems, in this paper we described their physical incorporation inside amino acids-modified polyester-based dendrimers which made them highly water-soluble. IR, NMR, zeta potential, mean size of particles, buffer capacity and drug release profiles of prepared materials were reported. The achieved water-soluble complexes harmonize a polycationic character and a buffer capacity which presuppose efficient cell penetration and increased residence time with a biodegradable cell respectful scaffold, thus appearing as a promising team of not toxic prodrugs for safe administration of ursolic and oleanolic acids.

Keywords

Polyester-based amino acids-modified dendrimers Physical encapsulation Water-soluble dendriplexes Buffer capacity NMR investigations 

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Notes

Acknowledgements

The authors are very thankful to Mr Gagliardo Osvaldo for Elemental Analysis and to University of Genova.

Supplementary material

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Synthesis of Water-soluble, Polyester-based Dendrimer Prodrugs for Exploiting Therapeutic Properties of Two Triterpenoid Acids

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Copyright information

© Chinese Chemical Society, Institute of Chemistry, Chinese Academy of Sciences and Springer-Verlag GmbH Germany, part of Springer Nature 2018

Authors and Affiliations

  • Silvana Alfei
    • 1
  • Gaby Brice Taptue
    • 1
  • Silvia Catena
    • 1
  • Angela Bisio
    • 1
  1. 1.Dipartimento di Farmacia, Sezione di Chimica e Tecnologie Farmaceutiche e AlimentariUniversità di GenovaGenovaItaly

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