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Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis

This work aimed to design, develop, and characterize a lipid nanocarrier system for the selective delivery of rifabutin (RFB) to alveolar macrophages. Lipid nanoparticles, specifically nanostructured lipid carriers (NLC), were synthetized by the high-shear homogenization and ultrasonication techniqu...

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Autores principales: Pinheiro, Marina, Ribeiro, Ricardo, Vieira, Alexandre, Andrade, Fernanda, Reis, Salette
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4977088/
https://www.ncbi.nlm.nih.gov/pubmed/27536067
http://dx.doi.org/10.2147/DDDT.S104395
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author Pinheiro, Marina
Ribeiro, Ricardo
Vieira, Alexandre
Andrade, Fernanda
Reis, Salette
author_facet Pinheiro, Marina
Ribeiro, Ricardo
Vieira, Alexandre
Andrade, Fernanda
Reis, Salette
author_sort Pinheiro, Marina
collection PubMed
description This work aimed to design, develop, and characterize a lipid nanocarrier system for the selective delivery of rifabutin (RFB) to alveolar macrophages. Lipid nanoparticles, specifically nanostructured lipid carriers (NLC), were synthetized by the high-shear homogenization and ultrasonication techniques. These nanoparticles were designed to exhibit both passive and active targeting strategies to be efficiently internalized by the alveolar macrophages, traffic to the acidified phagosomes and phagolysosomes, and release bactericidal concentrations of the antituberculosis drug intracellularly. NLC that could entrap RFB were prepared, characterized, and further functionalized with mannose. Particles’ diameter, zeta potential, morphology, drug% entrapping efficiency, and drug release kinetics were evaluated. The mannose coating process was confirmed by Fourier transform infrared. Further, the cytotoxicity of the formulations was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay in A549, Calu-3, and Raw 264.7 cells. The diameter of NLC formulations was found to be in the range of 175–213 nm, and drug entrapping efficiency was found to be above 80%. In addition, high storage stability for the formulations was expected since they maintained the initial characteristics for 6 months. Moreover, the drug release was pH-sensitive, with a faster drug release at acidic pH than at neutral pH. These results pose a strong argument that the developed nanocarrier can be explored as a promising carrier for safer and more efficient management of tuberculosis by exploiting the pulmonary route of administration.
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spelling pubmed-49770882016-08-17 Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis Pinheiro, Marina Ribeiro, Ricardo Vieira, Alexandre Andrade, Fernanda Reis, Salette Drug Des Devel Ther Original Research This work aimed to design, develop, and characterize a lipid nanocarrier system for the selective delivery of rifabutin (RFB) to alveolar macrophages. Lipid nanoparticles, specifically nanostructured lipid carriers (NLC), were synthetized by the high-shear homogenization and ultrasonication techniques. These nanoparticles were designed to exhibit both passive and active targeting strategies to be efficiently internalized by the alveolar macrophages, traffic to the acidified phagosomes and phagolysosomes, and release bactericidal concentrations of the antituberculosis drug intracellularly. NLC that could entrap RFB were prepared, characterized, and further functionalized with mannose. Particles’ diameter, zeta potential, morphology, drug% entrapping efficiency, and drug release kinetics were evaluated. The mannose coating process was confirmed by Fourier transform infrared. Further, the cytotoxicity of the formulations was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay in A549, Calu-3, and Raw 264.7 cells. The diameter of NLC formulations was found to be in the range of 175–213 nm, and drug entrapping efficiency was found to be above 80%. In addition, high storage stability for the formulations was expected since they maintained the initial characteristics for 6 months. Moreover, the drug release was pH-sensitive, with a faster drug release at acidic pH than at neutral pH. These results pose a strong argument that the developed nanocarrier can be explored as a promising carrier for safer and more efficient management of tuberculosis by exploiting the pulmonary route of administration. Dove Medical Press 2016-08-02 /pmc/articles/PMC4977088/ /pubmed/27536067 http://dx.doi.org/10.2147/DDDT.S104395 Text en © 2016 Pinheiro et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Pinheiro, Marina
Ribeiro, Ricardo
Vieira, Alexandre
Andrade, Fernanda
Reis, Salette
Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
title Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
title_full Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
title_fullStr Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
title_full_unstemmed Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
title_short Design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
title_sort design of a nanostructured lipid carrier intended to improve the treatment of tuberculosis
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4977088/
https://www.ncbi.nlm.nih.gov/pubmed/27536067
http://dx.doi.org/10.2147/DDDT.S104395
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