AI Article Synopsis

  • This study focused on creating and testing a modified nanostructured lipid carrier (NLC) that uses chitosan and dextran to co-deliver two drugs, buparvaquone (BPQ) and polymyxin B (PB), for treating leishmaniasis.
  • The NLC was developed through high-pressure homogenization, with PB attached via electrostatic interactions, and its effectiveness was tested in mouse cells and against Leishmania infantum.
  • Results showed that the modified NLCs had better leishmanicidal activity compared to free BPQ, indicating that this formulation could effectively improve leishmaniasis treatment by targeting macrophages more efficiently.

Article 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 583.4 ± 0.10, 203.1 ± 0.04 and 5.7 ± 0.06 μM; IC 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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Source
http://dx.doi.org/10.1016/j.jgar.2019.06.006DOI Listing

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Article Synopsis
  • This study focused on creating and testing a modified nanostructured lipid carrier (NLC) that uses chitosan and dextran to co-deliver two drugs, buparvaquone (BPQ) and polymyxin B (PB), for treating leishmaniasis.
  • The NLC was developed through high-pressure homogenization, with PB attached via electrostatic interactions, and its effectiveness was tested in mouse cells and against Leishmania infantum.
  • Results showed that the modified NLCs had better leishmanicidal activity compared to free BPQ, indicating that this formulation could effectively improve leishmaniasis treatment by targeting macrophages more efficiently.
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