Meglumine Antimoniate-Loaded Aqueous-Core PLA Nanocapsules: Old Drug, New Formulation against Leishmania-Related Diseases.
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.
['Cosco|Donato|D|', 'Bruno|Federica|F|', 'Castelli|Germano|G|', 'Puleio|Roberto|R|', 'Bonacci|Sonia|S|', 'Procopio|Antonio|A|', 'Britti|Domenico|D|', 'Fresta|Massimo|M|', 'Vitale|Fabrizio|F|', 'Paolino|Donatella|D|https://orcid.org/0000-0002-5223-9879']
PLA nanocapsules leishmaniasis glucantime meglumine antimoniate