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Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion

Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)–SD. The SDs of AG and the carrier materi...

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Autores principales: Zhao, Guowei, Zeng, Qingyun, Zhang, Shoude, Zhong, Youquan, Wang, Changhao, Chen, Yashao, Ou, Liquan, Liao, Zhenggen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409804/
https://www.ncbi.nlm.nih.gov/pubmed/30744157
http://dx.doi.org/10.3390/pharmaceutics11020074
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author Zhao, Guowei
Zeng, Qingyun
Zhang, Shoude
Zhong, Youquan
Wang, Changhao
Chen, Yashao
Ou, Liquan
Liao, Zhenggen
author_facet Zhao, Guowei
Zeng, Qingyun
Zhang, Shoude
Zhong, Youquan
Wang, Changhao
Chen, Yashao
Ou, Liquan
Liao, Zhenggen
author_sort Zhao, Guowei
collection PubMed
description Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)–SD. The SDs of AG and the carrier materials, polyethylene glycol (PEG) and PEG grafted with carbon chains of different length (grafted PEG), have been prepared by spray-drying and vacuum-drying methods. In AG–SDs prepared by the different preparation methods with the same polymer as carrier material, the intermolecular interaction, 5% weight-loss temperature, the melting temperature (T(m)), surface morphology, crystallinity, and dissolution behavior have significant differences. In the AG–SDs prepared by the same spray-drying method with different grafted PEG as carrier material, T(m), surface morphology, crystallinity, and dissolution behavior had little difference. In the AG–SDs prepared by the same vacuum-drying method with different grafted PEG as carrier material, the crystallinity and T(m) decreased, and the dissolution rate of AG increased with the increase of grafted PEG lipophilicity. The preparation method has an important effect on the properties of SD. The increase of carrier material lipophilicity is beneficial to the thermal stability of SD, the decrease of crystallinity and the increase of dissolution rate of a poorly water-soluble drug in the SD.
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spelling pubmed-64098042019-03-29 Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion Zhao, Guowei Zeng, Qingyun Zhang, Shoude Zhong, Youquan Wang, Changhao Chen, Yashao Ou, Liquan Liao, Zhenggen Pharmaceutics Article Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)–SD. The SDs of AG and the carrier materials, polyethylene glycol (PEG) and PEG grafted with carbon chains of different length (grafted PEG), have been prepared by spray-drying and vacuum-drying methods. In AG–SDs prepared by the different preparation methods with the same polymer as carrier material, the intermolecular interaction, 5% weight-loss temperature, the melting temperature (T(m)), surface morphology, crystallinity, and dissolution behavior have significant differences. In the AG–SDs prepared by the same spray-drying method with different grafted PEG as carrier material, T(m), surface morphology, crystallinity, and dissolution behavior had little difference. In the AG–SDs prepared by the same vacuum-drying method with different grafted PEG as carrier material, the crystallinity and T(m) decreased, and the dissolution rate of AG increased with the increase of grafted PEG lipophilicity. The preparation method has an important effect on the properties of SD. The increase of carrier material lipophilicity is beneficial to the thermal stability of SD, the decrease of crystallinity and the increase of dissolution rate of a poorly water-soluble drug in the SD. MDPI 2019-02-10 /pmc/articles/PMC6409804/ /pubmed/30744157 http://dx.doi.org/10.3390/pharmaceutics11020074 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Zhao, Guowei
Zeng, Qingyun
Zhang, Shoude
Zhong, Youquan
Wang, Changhao
Chen, Yashao
Ou, Liquan
Liao, Zhenggen
Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion
title Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion
title_full Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion
title_fullStr Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion
title_full_unstemmed Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion
title_short Effect of Carrier Lipophilicity and Preparation Method on the Properties of Andrographolide–Solid Dispersion
title_sort effect of carrier lipophilicity and preparation method on the properties of andrographolide–solid dispersion
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6409804/
https://www.ncbi.nlm.nih.gov/pubmed/30744157
http://dx.doi.org/10.3390/pharmaceutics11020074
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