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Oral administration of buparvaquone nanostructured lipid carrier enables in vivo activity against Leishmania infantum.
Monteiro, Lis Marie; Löbenberg, Raimar; Barbosa, Eduardo José; de Araujo, Gabriel Lima Barros; Sato, Paula Keiko; Kanashiro, Edite; de Araujo Eliodoro, Raissa H; Rocha, Mussya; de Freitas, Vera Lúcia Teixeira; Fotaki, Nikoletta; Bou-Chacra, Nádia Araci.
Afiliação
  • Monteiro LM; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av, 580, Cidade Universitária, 05508-000 São Paulo, SP, Brazil.
  • Löbenberg R; Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, 8613 - 114St NW, T6G 2H7, Edmonton, AB, Canada.
  • Barbosa EJ; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av, 580, Cidade Universitária, 05508-000 São Paulo, SP, Brazil. Electronic address: eduardo.jose.barbosa@usp.br.
  • de Araujo GLB; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av, 580, Cidade Universitária, 05508-000 São Paulo, SP, Brazil.
  • Sato PK; Laboratory of Medical Investigation in Immunology (LIM48), Hospital das Clínicas, Faculdade de Medicina FMUSP, Universidade de São Paulo, Av. Dr. Eneas Carvalho de Aguiar, 470, IMT2, térreo, 05403-000, São Paulo, SP, Brazil.
  • Kanashiro E; Laboratory of Medical Investigation in Immunology (LIM48), Hospital das Clínicas, Faculdade de Medicina FMUSP, Universidade de São Paulo, Av. Dr. Eneas Carvalho de Aguiar, 470, IMT2, térreo, 05403-000, São Paulo, SP, Brazil; Seroepidemiology, Cellular, and Molecular Immunology Laboratory - Institute
  • de Araujo Eliodoro RH; Laboratory of Medical Investigation in Immunology (LIM48), Hospital das Clínicas, Faculdade de Medicina FMUSP, Universidade de São Paulo, Av. Dr. Eneas Carvalho de Aguiar, 470, IMT2, térreo, 05403-000, São Paulo, SP, Brazil.
  • Rocha M; Laboratory of Medical Investigation in Immunology (LIM48), Hospital das Clínicas, Faculdade de Medicina FMUSP, Universidade de São Paulo, Av. Dr. Eneas Carvalho de Aguiar, 470, IMT2, térreo, 05403-000, São Paulo, SP, Brazil.
  • de Freitas VLT; Laboratory of Medical Investigation in Immunology (LIM48), Hospital das Clínicas, Faculdade de Medicina FMUSP, Universidade de São Paulo, Av. Dr. Eneas Carvalho de Aguiar, 470, IMT2, térreo, 05403-000, São Paulo, SP, Brazil.
  • Fotaki N; Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom.
  • Bou-Chacra NA; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Professor Lineu Prestes Av, 580, Cidade Universitária, 05508-000 São Paulo, SP, Brazil. Electronic address: chacra@usp.br.
Eur J Pharm Sci ; 169: 106097, 2022 Feb 01.
Article em En | MEDLINE | ID: mdl-34910988
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 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 µM). 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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Leishmania infantum / Antiprotozoários Idioma: En Revista: Eur J Pharm Sci Assunto da revista: FARMACIA / FARMACOLOGIA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Leishmania infantum / Antiprotozoários Idioma: En Revista: Eur J Pharm Sci Assunto da revista: FARMACIA / FARMACOLOGIA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda