Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive

The purpose of this study was to optimize the preparation method of injectable Octreotide microspheres. To explore the correlation between the solvent system and the general properties of microspheres to reduce burst release and enable them to be used for portal hypertension. Octreotide microspheres...

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Autores principales: Han, Bing, Tang, Huan, Liang, Qiming, Zhu, Ming, Xie, Yizhuo, Chen, Jinglin, Li, Qianwen, Jia, Juan, Li, Yan, Ren, Zhihui, Cong, Dengli, Yu, Xiaofeng, Sui, Dayun, Pei, Jin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2021
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Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8032347/
https://www.ncbi.nlm.nih.gov/pubmed/33825592
http://dx.doi.org/10.1080/10717544.2021.1898702
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author Han, Bing
Tang, Huan
Liang, Qiming
Zhu, Ming
Xie, Yizhuo
Chen, Jinglin
Li, Qianwen
Jia, Juan
Li, Yan
Ren, Zhihui
Cong, Dengli
Yu, Xiaofeng
Sui, Dayun
Pei, Jin
author_facet Han, Bing
Tang, Huan
Liang, Qiming
Zhu, Ming
Xie, Yizhuo
Chen, Jinglin
Li, Qianwen
Jia, Juan
Li, Yan
Ren, Zhihui
Cong, Dengli
Yu, Xiaofeng
Sui, Dayun
Pei, Jin
author_sort Han, Bing
collection PubMed
description The purpose of this study was to optimize the preparation method of injectable Octreotide microspheres. To explore the correlation between the solvent system and the general properties of microspheres to reduce burst release and enable them to be used for portal hypertension. Octreotide microspheres were prepared by modified double emulsion solution evaporation method after optimizing preparation conditions. The results showed that Octreotide microspheres had a particle size of 57.48 ± 15.24 μm, and the initial release was significantly reduced. In vitro release and in vivo pharmacokinetic data indicated that Octreotide was released stably within 1200 h. The effects on portal vein pressure, liver tissue morphology and other related indexes were observed after administration. As obvious results, injection of Octreotide microspheres could significantly reduce portal vein pressure and reduce the portal vein lumen area in experimental cirrhotic portal hypertensive rats. The optimized Octreotide PLGA microsphere preparation has been proved to have a good effect on PHT in vivo after detecting aminotransferase (AST) and alanine aminotransferase (ALT) activity, liver tissue hydroxyproline (Hyp) content, serum and liver tissue malondialdehyde (MDA) levels, plasma prostacyclin (PGI(2)) levels, and liver tissue tumor necrosis factor (TNFα) content. In addition, serum and liver tissue superoxide dismutase (SOD) activity and liver tissue glutathione (GSH) content, plasma thromboxane (TXA(2)), serum nitric oxide (NO), liver tissue nitric oxide synthase (NOS), and plasma and liver tissue endothelin (ET) were significantly increased.
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spelling pubmed-80323472021-04-21 Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive Han, Bing Tang, Huan Liang, Qiming Zhu, Ming Xie, Yizhuo Chen, Jinglin Li, Qianwen Jia, Juan Li, Yan Ren, Zhihui Cong, Dengli Yu, Xiaofeng Sui, Dayun Pei, Jin Drug Deliv Research Article The purpose of this study was to optimize the preparation method of injectable Octreotide microspheres. To explore the correlation between the solvent system and the general properties of microspheres to reduce burst release and enable them to be used for portal hypertension. Octreotide microspheres were prepared by modified double emulsion solution evaporation method after optimizing preparation conditions. The results showed that Octreotide microspheres had a particle size of 57.48 ± 15.24 μm, and the initial release was significantly reduced. In vitro release and in vivo pharmacokinetic data indicated that Octreotide was released stably within 1200 h. The effects on portal vein pressure, liver tissue morphology and other related indexes were observed after administration. As obvious results, injection of Octreotide microspheres could significantly reduce portal vein pressure and reduce the portal vein lumen area in experimental cirrhotic portal hypertensive rats. The optimized Octreotide PLGA microsphere preparation has been proved to have a good effect on PHT in vivo after detecting aminotransferase (AST) and alanine aminotransferase (ALT) activity, liver tissue hydroxyproline (Hyp) content, serum and liver tissue malondialdehyde (MDA) levels, plasma prostacyclin (PGI(2)) levels, and liver tissue tumor necrosis factor (TNFα) content. In addition, serum and liver tissue superoxide dismutase (SOD) activity and liver tissue glutathione (GSH) content, plasma thromboxane (TXA(2)), serum nitric oxide (NO), liver tissue nitric oxide synthase (NOS), and plasma and liver tissue endothelin (ET) were significantly increased. Taylor & Francis 2021-04-07 /pmc/articles/PMC8032347/ /pubmed/33825592 http://dx.doi.org/10.1080/10717544.2021.1898702 Text en © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by-nc/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial License (http://creativecommons.org/licenses/by-nc/4.0/ (https://creativecommons.org/licenses/by-nc/4.0/) ), which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Han, Bing
Tang, Huan
Liang, Qiming
Zhu, Ming
Xie, Yizhuo
Chen, Jinglin
Li, Qianwen
Jia, Juan
Li, Yan
Ren, Zhihui
Cong, Dengli
Yu, Xiaofeng
Sui, Dayun
Pei, Jin
Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
title Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
title_full Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
title_fullStr Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
title_full_unstemmed Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
title_short Preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
title_sort preparation of long-acting microspheres loaded with octreotide for the treatment of portal hypertensive
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8032347/
https://www.ncbi.nlm.nih.gov/pubmed/33825592
http://dx.doi.org/10.1080/10717544.2021.1898702
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