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 and are of eminent interest for biomedical applications, including gene transfection, tissue engineering, imaging, drug delivery. The well-known pharmacological activities of Ursolic and Oleanolic acids are limited by their small water solubility, non-specific cells 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 drugs release profiles of prepared materials were reported. The achieved water-soluble complexes harmonize a polycationic character and a buffer capacity which presuppose efficient cells penetration and increased residence time with a biodegradable cells respectful scaffold thus appearing a promising team of not toxic prodrugs for safe administration of Ursolic and Oleanolic acids.

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
2018

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 and are of eminent interest for biomedical applications, including gene transfection, tissue engineering, imaging, drug delivery. The well-known pharmacological activities of Ursolic and Oleanolic acids are limited by their small water solubility, non-specific cells 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 drugs release profiles of prepared materials were reported. The achieved water-soluble complexes harmonize a polycationic character and a buffer capacity which presuppose efficient cells penetration and increased residence time with a biodegradable cells respectful scaffold thus appearing a promising team of not toxic prodrugs for safe administration of Ursolic and Oleanolic acids.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11567/889434
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