Do albendazole-loaded lipid nanocapsules enhance the bioavailability of albendazole in the brain of healthy mice?

•ABZ was detected in brain after oral administration as suspension or lipid nanocapsules (ABZ-LNCs).•ABZ-NCLs increased the brain availability of ABZ/ABZ-SO, in relation to ABZ suspension.•ABZ-NCLs have potential usefulness for the neurocysticercosis treatment. Neurocysticercosis is a neglected trop...

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Veröffentlicht in:Acta tropica 2020-01, Vol.201, p.105215, Article 105215
Hauptverfasser: Fabbri, Julia, Espinosa, Juan Pablo, Pensel, Patricia Eugenia, Medici, Sandra Karina, Gamboa, Gabriela Ullio, Benoit, Jean Pierre, Elissondo, María Celina
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Sprache:eng
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Zusammenfassung:•ABZ was detected in brain after oral administration as suspension or lipid nanocapsules (ABZ-LNCs).•ABZ-NCLs increased the brain availability of ABZ/ABZ-SO, in relation to ABZ suspension.•ABZ-NCLs have potential usefulness for the neurocysticercosis treatment. Neurocysticercosis is a neglected tropical disease that affects the central nervous system and is the most common cause of human epilepsy acquired in developing countries. Therapeutic failures attributed to medical management of neurocysticercosis with albendazole (ABZ) have been primarily linked to the poor drug absorption rate resulting in low drug level in plasma and brain tissue. The aim of the current work was to characterize and compare the brain pharmacokinetic behavior of ABZ formulated as a suspension or lipid nanocapsules (ABZ-LNCs) in healthy mice. The relative availability in brain tissue of the active metabolite ABZ sulphoxide increased 183% when ABZ was administered as LNCs, in relation to ABZ suspension. The parent drug was also detected for a short period of time. The bioavailability of ABZ in ABZ-LNCs treated mice increased more than 2 fold compared with ABZ suspension group. The enhanced drug brain exposure observed after administration of ABZ-LNCs to healthy mice has potential usefulness for the treatment of human neurocysticercosis. [Display omitted]
ISSN:0001-706X
1873-6254
DOI:10.1016/j.actatropica.2019.105215