Co-delivery of buparvaquone and polymyxin B in a nanostructured lipid carrier for leishmaniasis treatment

L.M Monteiro, Raimar Löbenberg, Nikoletta Fotaki, Gabriel Lima Barros de Araujo, P.C Cotrim, Nádia Araci Bou-Chacra

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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; CC 50 583.4 ± 0.10, 203.1 ± 0.04 and 5.7 ± 0.06 μM; IC 50 229.0 ± 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.

Original languageEnglish
Pages (from-to)279-283
Number of pages5
JournalJournal of Global Antimicrobial Resistance
Early online date13 Jun 2019
Publication statusPublished - 1 Sept 2019

Bibliographical note

Copyright © 2019 International Society for Antimicrobial Chemotherapy. Published by Elsevier Ltd. All rights reserved.


  • Buparvaquone
  • Chitosan
  • Dextran
  • Leishmaniasis
  • Nanostructured lipid carrier
  • Polymyxin B

ASJC Scopus subject areas

  • Microbiology
  • Immunology and Allergy
  • Immunology
  • Microbiology (medical)


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