Meglumine Antimoniate-Loaded Aqueous-Core PLA Nanocapsules: Old Drug, New Formulation against Leishmania-Related Diseases.

Abstract

Leishmaniasis is a human and animal disease endemic in tropical and subtropical areas treated by means of pentavalent antimony as first-line approach. Unfortunately, the formulations available on the market are characterized by significant side effects and a total remission of the disease is difficult to be obtained. The aim of this investigation is to describe the development and characterization of aqueous-core poly-l-lactide (PLA) nanocapsules containing glucantime (meglumine antimoniate, MA) with the aim of increasing the pharmacological efficacy of the active compound. The polymeric systems characterized by a mean diameter of ≈300 nm exert a great interaction with murine macrophages. MA-loaded PLA nanocapsules show a great antileishmanial activity on mice infected with Leishmania infantum with respect to the free drug, favoring a decrease of the administration times. The biodistribution profiles demonstrate a lower renal accumulation of MA after its nanoencapsulation and a significant increase of its plasmatic half-life. The parasite load evaluated by immunohistochemistry shows a significant decrease in liver, spleen, and kidneys when mice are treated with MA-loaded PLA nanocapsules especially after 45 days. The obtained results demonstrate the potential application of MA-loaded PLA nanocapsules as novel nanomedicine for the treatment of leishmaniasis.

• Authors: Donato Cosco, Federica Bruno, Germano Castelli, Roberto Puleio, Sonia Bonacci, Antonio Procopio, Domenico Britti, Massimo Fresta, Fabrizio Vitale, Donatella Paolino
• Journal: Macromolecular bioscience (Macromol Biosci) Vol. 21 Issue 7 Pg. e2100046 (07 2021) ISSN: 1616-5195 [Electronic] Germany
• PMID: 34117834 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2021 Wiley-VCH GmbH.

Chemical References

• Nanocapsules
• Organometallic Compounds
• Polyesters
• poly(lactide)
• Meglumine
• Meglumine Antimoniate

Topics

• Animals
• Leishmania infantum
• Meglumine (chemistry, pharmacology, therapeutic use)
• Meglumine Antimoniate (pharmacology)
• Mice
• Mice, Inbred BALB C
• Nanocapsules
• Organometallic Compounds (chemistry)
• Polyesters (pharmacology)
• Tissue Distribution