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dc.contributorSistema FMUSP-HC: Faculdade de Medicina da Universidade de São Paulo (FMUSP) e Hospital das Clínicas da FMUSP-
dc.contributor.authorMONTEIRO, Lis Marie-
dc.contributor.authorLOBENBERG, Raimar-
dc.contributor.authorBARBOSA, Eduardo Jose-
dc.contributor.authorARAUJO, Gabriel Lima Barros de-
dc.contributor.authorSATO, Paula Keiko-
dc.contributor.authorKANASHIRO, Edite-
dc.contributor.authorELIODORO, Raissa H. de Araujo-
dc.contributor.authorROCHA, Mussya-
dc.contributor.authorFREITAS, Vera Lucia Teixeira de-
dc.contributor.authorFOTAKI, Nikoletta-
dc.contributor.authorBOU-CHACRA, Nadia Araci-
dc.identifier.citationEUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, v.169, article ID 106097, 11p, 2022-
dc.description.abstractLeishmaniasis, 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 the severe adverse effects of the drugs, which are administered parenterally. Buparvaquone (BPQ) showed in vitro activity against leishmania parasites; nevertheless, it has failed in vivo tests due to its low aqueous solubility. Though, lipid nanoparticles can overcome this holdback. In this study we tested the hypothesis whether BPQ-NLC shows in vivo activity against L. infantum. Two optimized formulations were prepared (V1: 173.9 +/- 1.6 nm, 0.5 mg of BPQ/mL; V2: 232.4 +/- 1.6 nm, 1.3 mg of BPQ/mL), both showed increased solubility up to 73.00-fold, and dissolution up to 83.29%, while for the free drug it was only 2.89%. Cytotoxicity test showed their biocompatibility (CC50 >554.4 mu M). Besides, the V1 dose of 0.3 mg/kg/day for 10 days reduced the parasite burden in 83.4% +/- 18.2% (p <0.05) in the liver. BPQ-NLC showed similar leishmanicidal activity compared to miltefosine. Therefore, BPQ-NLC is a promising addition to the limited therapeutic arsenal suitable for leishmaniasis oral administration treatment.eng
dc.description.sponsorshipSao Paulo Research Support Foundation (FAPESP) [2018/16028-5]-
dc.description.sponsorshipCoordenacao de Aperfeicoamento de Pessoal de Nivel Superior Brazil (CAPES) [001]-
dc.relation.ispartofEuropean Journal of Pharmaceutical Sciences-
dc.subjectNanostructured lipid carriereng
dc.subjectNeglected diseaseseng
dc.subject.otherl. infantumeng
dc.titleOral administration of buparvaquone nanostructured lipid carrier enables in vivo activity against Leishmania infantumeng
dc.rights.holderCopyright ELSEVIEReng
dc.subject.wosPharmacology & Pharmacyeng
dc.type.categoryoriginal articleeng
dc.type.versionpublishedVersioneng, Lis Marie:Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Prof Lineu Prestes Av 580,Cidade Univ, BR-05508000 Sao Paulo, SP, Brazil-, Raimar:Univ Alberta, Fac Pharm & Pharmaceut Sci, 8613-114St NW, Edmonton, AB T6G 2H7, Canada-, Eduardo Jose:Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Prof Lineu Prestes Av 580,Cidade Univ, BR-05508000 Sao Paulo, SP, Brazil-, Gabriel Lima Barros de:Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Prof Lineu Prestes Av 580,Cidade Univ, BR-05508000 Sao Paulo, SP, Brazil-, Nikoletta:Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England-, Nadia Araci:Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Prof Lineu Prestes Av 580,Cidade Univ, BR-05508000 Sao Paulo, SP, Brazil-
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Artigos e Materiais de Revistas Científicas - FM/MIP
Departamento de Moléstias Infecciosas e Parasitárias - FM/MIP

Artigos e Materiais de Revistas Científicas - IMT
Instituto de Medicina Tropical - IMT

Artigos e Materiais de Revistas Científicas - LIM/46
LIM/46 - Laboratório de Parasitologia Médica

Artigos e Materiais de Revistas Científicas - LIM/48
LIM/48 - Laboratório de Imunologia

Artigos e Materiais de Revistas Científicas - ODS/03
ODS/03 - Saúde e bem-estar

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