Abstract
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 language | English |
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Pages (from-to) | 279-283 |
Number of pages | 5 |
Journal | Journal of Global Antimicrobial Resistance |
Volume | 18 |
Early online date | 13 Jun 2019 |
DOIs | |
Publication status | Published - 1 Sept 2019 |
Bibliographical note
Copyright © 2019 International Society for Antimicrobial Chemotherapy. Published by Elsevier Ltd. All rights reserved.Keywords
- Buparvaquone
- Chitosan
- Dextran
- Leishmaniasis
- Nanostructured lipid carrier
- Polymyxin B
ASJC Scopus subject areas
- Microbiology
- Immunology and Allergy
- Immunology
- Microbiology (medical)