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Rationally designed hyaluronic acid-based nano-complexes for pentamidine delivery.

Abstract
Nanoparticles of polymeric complexes made of hyaluronic acid and polyarginine were investigated for the encapsulation of the cationic hydrophilic drug pentamidine isethionate. The interaction between the anionic hyaluronic acid and the cationic pentamidine resulting in the formation of polyelectrolyte complexes was firstly studied. Then, nanoparticles made of hyaluronic acid and polyarginine loaded with pentamidine were developed. These drug delivery systems consist of a monodisperse population of negatively charged pentamidine-loaded nanoparticles with a high drug encapsulation rate (80%). Such high encapsulation efficiency coming from ion exchange was confirmed by measurements of the counterion isethionate released from pentamidine during nanoparticles formation. Besides, freeze-dried pentamidine-loaded nanoparticles kept their integrity after their reconstitution in water. In vitro studies on human lung (A549) and breast (MDA-MB-231) cancer cell lines showed that pentamidine-loaded nanoparticles were more cytotoxic in comparison to the free drug, suggesting an enhanced internalization of encapsulated drug by cancer cells.
AuthorsFlavia Carton, Yves Chevalier, Letizia Nicoletti, Małgorzata Tarnowska, Barbara Stella, Silvia Arpicco, Manuela Malatesta, Lars Petter Jordheim, Stéphanie Briançon, Giovanna Lollo
JournalInternational journal of pharmaceutics (Int J Pharm) Vol. 568 Pg. 118526 (Sep 10 2019) ISSN: 1873-3476 [Electronic] Netherlands
PMID31323370 (Publication Type: Journal Article)
CopyrightCopyright © 2019. Published by Elsevier B.V.
Chemical References
  • Antineoplastic Agents
  • Peptides
  • polyarginine
  • Pentamidine
  • Hyaluronic Acid
Topics
  • Antineoplastic Agents (administration & dosage, chemistry)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Drug Delivery Systems
  • Drug Liberation
  • Drug Stability
  • Freeze Drying
  • Humans
  • Hyaluronic Acid (administration & dosage, chemistry)
  • Nanoparticles (administration & dosage, chemistry)
  • Pentamidine (administration & dosage, chemistry)
  • Peptides (administration & dosage, chemistry)
  • Solubility

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