Berberine-Loaded Liposomes for the Treatment of Leishmania infantum-Infected BALB/c Mice

Berberine (BER)—an anti-inflammatory quaternary isoquinoline alkaloid extracted from plants—has been reported to have a variety of biologic properties, including antileishmanial activity. This work addresses the preparation of BER-loaded liposomes with the aim to prevent its rapid liver metabolism a...

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Detalles Bibliográficos
Autores: Calvo-Bacaicoa, A. (Alba)|||/items/8557046e-51a2-45a9-b289-9b6e0b1648d3, Moreno, E. (Esther)|||/items/e9c6c350-8b74-4554-86fd-4a8a7ff563a4, Larrea-Leoz, E. (Esther)|||/items/37a0521f-3293-4001-85d1-bc71241d8a83, Sanmartin-Grijalba, C. (Carmen)|||/items/d36bd105-ab64-427d-9745-5812cf5e7af7, Irache-Garreta, J.M. (Juan Manuel)|||/items/c7cbbe9e-faeb-47e1-b7e8-2d956ca50173, Espuelas, S. (Socorro)|||/items/b57c05de-0bc4-4fcf-ae1e-c9b2fb92964c
Tipo de recurso: artículo
Fecha de publicación:2020
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/65575
Acceso en línea:https://hdl.handle.net/10171/65575
Access Level:acceso abierto
Palabra clave:Berberine
Liposomes
Visceral leishmaniasis
Leishmania infantum
Descripción
Sumario:Berberine (BER)—an anti-inflammatory quaternary isoquinoline alkaloid extracted from plants—has been reported to have a variety of biologic properties, including antileishmanial activity. This work addresses the preparation of BER-loaded liposomes with the aim to prevent its rapid liver metabolism and improve the drug selective delivery to the infected organs in visceral leishmaniasis (VL). BER liposomes (LP-BER) displayed a mean size of 120 nm, negative Z-potential of −38 mV and loaded 6 nmol/µmol lipid. In vitro, the loading of BER in liposomes enhanced its selectivity index more than 7-fold by decreasing its cytotoxicity to macrophages. In mice, LP-BER enhanced drug accumulation in the liver and the spleen. Consequently, the liposomal delivery of the drug reduced parasite burden in the liver and spleen by three and one logarithms (99.2 and 93.5%), whereas the free drug only decreased the infection in the liver by 1-log. The organ drug concentrations—far from IC50 values— indicate that BER immunomodulatory activity or drug metabolites also contribute to the efficacy. Although LP-BER decreased 10-fold—an extremely rapid clearance of the free drug in mice—the value remains very high. Moreover, LP-BER reduced plasma triglycerides levels.

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