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Co-delivery of buparvaquone and polymyxin B in a nanostructured lipid carrier for leishmaniasis treatment.
Monteiro, Lis Marie; Löbenberg, Raimar; Fotaki, Nikoletta; de Araújo, Gabriel Lima Barros; Cotrim, Paulo Cesar; Bou-Chacra, Nádia.
Afiliação
  • Monteiro LM; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.
  • Löbenberg R; Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, AB, Canada.
  • Fotaki N; Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, United Kingdom.
  • de Araújo GLB; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.
  • Cotrim PC; Seroepidemiology, Cellular and Molecular Immunology Laboratory - Institute of Tropical Medicine, University of São Paulo, São Paulo, Brazil.
  • Bou-Chacra N; Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil. Electronic address: chacra@usp.br.
J Glob Antimicrob Resist ; 18: 279-283, 2019 09.
Article em En | MEDLINE | ID: mdl-31202979
OBJECTIVES: This study aimed to describe the preparation and in vitro evaluation of a surface-modified nanostructured lipid carrier (NLC) using chitosan and dextran for co-delivery of buparvaquone (BPQ) and polymyxin B (PB) against leishmaniasis. METHODS: The NLC was prepared using high-pressure homogenisation. Polymyxin B binding and surface modification with biopolymers were achieved by electrostatic interaction. In vitro cytotoxicity was assessed in mouse peritoneal macrophages, and leishmanicidal activity in amastigotes of Leishmania infantum. RESULTS: The performance attributes of BPQ-NLC, BPQ-NLC-PB[A-] (anionic) and BPQ-NLC-PB[C+] (cationic) were respectively: Z-average 173.9 ± 1.6, 183.8 ± 4.5 and 208.8 ± 2.6 nm; zeta potential -19.6 ± 1.5, -20.1 ± 1.1 and 31.1 ± 0.8 mV; CC50 583.4 ± 0.10, 203.1 ± 0.04 and 5.7 ± 0.06 µM; IC50 229.0 ± 0.04, 145.7 ± 0.04 and 150.5 ± 0.02 nM. The NLC in vitro leishmanicidal activity showed up to 3.1-fold increase when compared with free BPQ (P < 0.05, α = 0.05). CONCLUSIONS: The developed NLC proved to be a promising formulation with which to overcome the drawbacks of current leishmaniasis treatment by the co-delivery of two alternative drugs and a macrophage targeting modified surface.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Polimixina B / Leishmaniose / Naftoquinonas / Sistemas de Liberação de Medicamentos / Nanoestruturas / Lipídeos / Antibacterianos Idioma: En Revista: J Glob Antimicrob Resist Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
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XML
PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Polimixina B / Leishmaniose / Naftoquinonas / Sistemas de Liberação de Medicamentos / Nanoestruturas / Lipídeos / Antibacterianos Idioma: En Revista: J Glob Antimicrob Resist Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda