Oral administration of buparvaquone nanostructured lipid carrier enables in vivo activity against Leishmania infantum

• DOI: 10.1016/j.ejps.2021.106097
• Publication Date: 2021-12-12T18:36:45Z
• Authors: Lis Marie Monteiro; Raimar Löbenberg; Eduardo José Barbosa; Gabriel Lima Barr...; Paula Keiko Sato; Edite Kanashiro; Raissa H. de Arau...; Mussya Rocha; Vera Lúcia Teixei...; Nikoletta Fotaki; Nádia Araci Bou-C...
• Keywords: Miltefosine; Antiprotozoal

Leishmaniasis, a neglected tropical disease, is prevalent in 98 countries with the occurrence of 1.3 million new cases annually. The conventional therapy for visceral leishmaniasis requires hospitalization due to severe adverse effects drugs, which are administered parenterally. Buparvaquone (BPQ) showed vitro activity against leishmania parasites; nevertheless, it has failed vivo tests its low aqueous solubility. Though, lipid nanoparticles can overcome this holdback. In study we tested hypothesis whether BPQ-NLC shows L. infantum. Two optimized formulations were prepared (V1: 173.9 ± 1.6 nm, 0.5 mg BPQ/mL; V2: 232.4 BPQ/mL), both increased solubility up 73.00-fold, and dissolution 83.29%, while free drug was only 2.89%. Cytotoxicity test their biocompatibility (CC50 >554.4 µM). Besides, V1 dose 0.3 mg/kg/day 10 days reduced parasite burden 83.4% ±18.2% (p <0.05) liver. similar leishmanicidal compared miltefosine. Therefore, promising addition limited therapeutic arsenal suitable oral administration treatment.