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Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties

Emodin (1,3,8-trihydroxy-6-methylanthraquinone) has been identified to have the potential to improve lung fibrosis and lung cancer. To avoid the liver and kidney toxicities and the fast metabolism of emodin, emodin-loaded polylactic acid microspheres (ED-PLA-MS) were prepared and their characteristi...

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Autores principales: Chen, Xiaohong, Yang, Zifeng, Sun, Renshan, Mo, Ziyao, Jin, Guangyao, Wei, Fenghuan, Hu, Jianmin, Guan, Wenda, Zhong, Nanshan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4013625/
https://www.ncbi.nlm.nih.gov/pubmed/24733070
http://dx.doi.org/10.3390/ijms15046241
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author Chen, Xiaohong
Yang, Zifeng
Sun, Renshan
Mo, Ziyao
Jin, Guangyao
Wei, Fenghuan
Hu, Jianmin
Guan, Wenda
Zhong, Nanshan
author_facet Chen, Xiaohong
Yang, Zifeng
Sun, Renshan
Mo, Ziyao
Jin, Guangyao
Wei, Fenghuan
Hu, Jianmin
Guan, Wenda
Zhong, Nanshan
author_sort Chen, Xiaohong
collection PubMed
description Emodin (1,3,8-trihydroxy-6-methylanthraquinone) has been identified to have the potential to improve lung fibrosis and lung cancer. To avoid the liver and kidney toxicities and the fast metabolism of emodin, emodin-loaded polylactic acid microspheres (ED-PLA-MS) were prepared and their characteristics were studied. ED-PLA-MS were prepared by the organic phase dispersion-solvent diffusion method. By applying an orthogonal design, our results indicated that the optimal formulation was 12 mg/mL PLA, 0.5% gelatin, and an organic phase:glycerol ratio of 1:20. Using the optimal experimental conditions, the drug loading and encapsulation efficiencies were (19.0 ± 1.8)% and (62.2 ± 2.6)%, respectively. The average particle size was 9.7 ± 0.7 μm. In vitro studies indicated that the ED-PLA-MS demonstrated a well-sustained release efficacy. The microspheres delivered emodin, primarily to the lungs of mice, upon intravenous injection. It was also detected by microscopy that partial lung inflammation was observed in lung tissues and no pathological changes were found in other tissues of the ED-PLA-MS-treated animals. These results suggested that ED-PLA-MS are of potential value in treating lung diseases in animals.
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spelling pubmed-40136252014-05-08 Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties Chen, Xiaohong Yang, Zifeng Sun, Renshan Mo, Ziyao Jin, Guangyao Wei, Fenghuan Hu, Jianmin Guan, Wenda Zhong, Nanshan Int J Mol Sci Article Emodin (1,3,8-trihydroxy-6-methylanthraquinone) has been identified to have the potential to improve lung fibrosis and lung cancer. To avoid the liver and kidney toxicities and the fast metabolism of emodin, emodin-loaded polylactic acid microspheres (ED-PLA-MS) were prepared and their characteristics were studied. ED-PLA-MS were prepared by the organic phase dispersion-solvent diffusion method. By applying an orthogonal design, our results indicated that the optimal formulation was 12 mg/mL PLA, 0.5% gelatin, and an organic phase:glycerol ratio of 1:20. Using the optimal experimental conditions, the drug loading and encapsulation efficiencies were (19.0 ± 1.8)% and (62.2 ± 2.6)%, respectively. The average particle size was 9.7 ± 0.7 μm. In vitro studies indicated that the ED-PLA-MS demonstrated a well-sustained release efficacy. The microspheres delivered emodin, primarily to the lungs of mice, upon intravenous injection. It was also detected by microscopy that partial lung inflammation was observed in lung tissues and no pathological changes were found in other tissues of the ED-PLA-MS-treated animals. These results suggested that ED-PLA-MS are of potential value in treating lung diseases in animals. Molecular Diversity Preservation International (MDPI) 2014-04-11 /pmc/articles/PMC4013625/ /pubmed/24733070 http://dx.doi.org/10.3390/ijms15046241 Text en © 2014 by the authors; licensee MDPI, Basel, Switzerland http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Chen, Xiaohong
Yang, Zifeng
Sun, Renshan
Mo, Ziyao
Jin, Guangyao
Wei, Fenghuan
Hu, Jianmin
Guan, Wenda
Zhong, Nanshan
Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties
title Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties
title_full Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties
title_fullStr Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties
title_full_unstemmed Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties
title_short Preparation of Lung-Targeting, Emodin-Loaded Polylactic Acid Microspheres and Their Properties
title_sort preparation of lung-targeting, emodin-loaded polylactic acid microspheres and their properties
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4013625/
https://www.ncbi.nlm.nih.gov/pubmed/24733070
http://dx.doi.org/10.3390/ijms15046241
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