Issue 33, 2019

Nucleoside-lipid-based nanocarriers for methylene blue delivery: potential application as anti-malarial drug

Abstract

Nucleolipid supramolecular assemblies are promising Drug Delivery Systems (DDS), particularly for nucleic acids. Studies based on negatively and positively charged nucleolipids (diC16dT and DOTAU, respectively) demonstrated appropriate stability, safety, and purity profile to be used as DDS. Methylene Blue (MB) remains a good antimalarial drug candidate, and could be considered for the treatment of uncomplicated or severe malaria. However, the development of MB as an antimalarial drug has been hampered by a high dose regimen required to obtain a proper effect, and a short plasmatic half life. We demonstrated that nanoparticles formed by nucleolipid encapsulation of MB using diC16dT and DOTAU (MB-NPs) is an interesting approach to improve drug stability and delivery. MB-NPs displayed sizes, PDI, zeta values, and colloidal stability allowing a possible use in intravenous formulations. Nanoparticles partially protected MB from oxido-reduction reactions, thus preventing early degradation during storage, and allowing prolongated pharmacokinetic in plasma. MB-NPs' efficacy, tested in vitro on sensitive or multidrug resistant strains of Plasmodium falciparum, was statistically similar to MB alone, with a slightly lower IC50. This nucleolipid-based approach to protect drugs against degradation represents a new alternative tool to be considered for malaria treatment.

Graphical abstract: Nucleoside-lipid-based nanocarriers for methylene blue delivery: potential application as anti-malarial drug

Supplementary files

Article information

Article type
Paper
Submitted
05 Apr 2019
Accepted
29 May 2019
First published
17 Jun 2019
This article is Open Access
Creative Commons BY license

RSC Adv., 2019,9, 18844-18852

Nucleoside-lipid-based nanocarriers for methylene blue delivery: potential application as anti-malarial drug

K. Kowouvi, B. Alies, M. Gendrot, A. Gaubert, G. Vacher, K. Gaudin, J. Mosnier, B. Pradines, P. Barthelemy, L. Grislain and P. Millet, RSC Adv., 2019, 9, 18844 DOI: 10.1039/C9RA02576F

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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