mPEG-icariin nanoparticles for treating myocardial ischaemia

Icariin (ICA), a major active ingredient from Chinese medicine, has unique pharmacological effects on ischaemic heart disease. However, its hydrophobic property limits its administration and leads to poor efficacy. This work aimed to change its hydrophobic property and improve the treatment efficacy...

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Main Authors: Yongqiang Zheng, Lingli Lu, Zhengli Yan, Sufang Jiang, Shanyi Yang, Yingzi Zhang, Kangwei Xu, Chunlian He, Xiaojun Tao, Qiufang Zhang
Format: Article
Language:English
Published: Taylor & Francis Group 2019-12-01
Series:Artificial Cells, Nanomedicine, and Biotechnology
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Online Access:https://www.tandfonline.com/doi/10.1080/21691401.2018.1554579
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author Yongqiang Zheng
Lingli Lu
Zhengli Yan
Sufang Jiang
Shanyi Yang
Yingzi Zhang
Kangwei Xu
Chunlian He
Xiaojun Tao
Qiufang Zhang
author_facet Yongqiang Zheng
Lingli Lu
Zhengli Yan
Sufang Jiang
Shanyi Yang
Yingzi Zhang
Kangwei Xu
Chunlian He
Xiaojun Tao
Qiufang Zhang
author_sort Yongqiang Zheng
collection DOAJ
description Icariin (ICA), a major active ingredient from Chinese medicine, has unique pharmacological effects on ischaemic heart disease. However, its hydrophobic property limits its administration and leads to poor efficacy. This work aimed to change its hydrophobic property and improve the treatment efficacy. We designed a new nano-drug to increase the ICA delivery. ICA was modified with hydrophilic polyethylene glycol monomethyl ether (mPEG) by a succinic anhydride linker to form a polyethylene glycol-icariin (mPEG-ICA) polymer. The structure of this polymer was identified by Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The content of ICA in the polymer was 32% as detected by ultraviolet spectrophotometry. mPEG-ICA nanoparticles, of 143.3 nm, were prepared by the dialysis method, and zeta potential was 0.439 mV by dynamic light scattering. The nanoparticles had a spherical shape on transmission electron microscopy. In media with pH 7.4 and 6.8, ICA release from mPEG-ICA nanoparticles after 72 h was about 0.78% and 64.05%, respectively, so the ICA release depended on the release media pH. On MTT and lactate dehydrogenase activity assay, mPEG-ICA nanoparticles could reduce cell damage induced by oxgen-glucose deprivation. Hoechst 33258 staining and TUNEL and AnnexinV-FITC/PI double staining showed that ICA nanoparticles could increase the activity of H9c2 cardiomyocytes under oxgen-glucose deprivation conditions by decreasing apoptosis. ICA modified by hydrophilic mPEG could improve its efficacy.
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series Artificial Cells, Nanomedicine, and Biotechnology
spelling doaj-art-dfc9a3269258465fb1faf7a4a0c0c6ca2025-08-20T03:51:08ZengTaylor & Francis GroupArtificial Cells, Nanomedicine, and Biotechnology2169-14012169-141X2019-12-0147179980910.1080/21691401.2018.1554579mPEG-icariin nanoparticles for treating myocardial ischaemiaYongqiang Zheng0Lingli Lu1Zhengli Yan2Sufang Jiang3Shanyi Yang4Yingzi Zhang5Kangwei Xu6Chunlian He7Xiaojun Tao8Qiufang Zhang9Department of Pharmacology, Laboratory of Chinese Herbal Pharmacology, Biomedical Research Institute, Hubei University of Medicine, Shiyan, Hubei, ChinaDepartment of Pharmacology, Laboratory of Chinese Herbal Pharmacology, Biomedical Research Institute, Hubei University of Medicine, Shiyan, Hubei, ChinaKey Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, ChinaKey Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, ChinaKey Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, ChinaKey Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, ChinaKey Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, ChinaKey Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, ChinaDepartment of Pharmacology, Laboratory of Chinese Herbal Pharmacology, Biomedical Research Institute, Hubei University of Medicine, Shiyan, Hubei, ChinaDepartment of Pharmacology, Laboratory of Chinese Herbal Pharmacology, Biomedical Research Institute, Hubei University of Medicine, Shiyan, Hubei, ChinaIcariin (ICA), a major active ingredient from Chinese medicine, has unique pharmacological effects on ischaemic heart disease. However, its hydrophobic property limits its administration and leads to poor efficacy. This work aimed to change its hydrophobic property and improve the treatment efficacy. We designed a new nano-drug to increase the ICA delivery. ICA was modified with hydrophilic polyethylene glycol monomethyl ether (mPEG) by a succinic anhydride linker to form a polyethylene glycol-icariin (mPEG-ICA) polymer. The structure of this polymer was identified by Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The content of ICA in the polymer was 32% as detected by ultraviolet spectrophotometry. mPEG-ICA nanoparticles, of 143.3 nm, were prepared by the dialysis method, and zeta potential was 0.439 mV by dynamic light scattering. The nanoparticles had a spherical shape on transmission electron microscopy. In media with pH 7.4 and 6.8, ICA release from mPEG-ICA nanoparticles after 72 h was about 0.78% and 64.05%, respectively, so the ICA release depended on the release media pH. On MTT and lactate dehydrogenase activity assay, mPEG-ICA nanoparticles could reduce cell damage induced by oxgen-glucose deprivation. Hoechst 33258 staining and TUNEL and AnnexinV-FITC/PI double staining showed that ICA nanoparticles could increase the activity of H9c2 cardiomyocytes under oxgen-glucose deprivation conditions by decreasing apoptosis. ICA modified by hydrophilic mPEG could improve its efficacy.https://www.tandfonline.com/doi/10.1080/21691401.2018.1554579Icariin (ICA)polyethylene glycol monomethyl ether (mPEG)fourier transform infrared spectroscopy (FTIR)nuclear magnetic resonance spectroscopy (1H-NMR)dynamic light scattering (DLS)
spellingShingle Yongqiang Zheng
Lingli Lu
Zhengli Yan
Sufang Jiang
Shanyi Yang
Yingzi Zhang
Kangwei Xu
Chunlian He
Xiaojun Tao
Qiufang Zhang
mPEG-icariin nanoparticles for treating myocardial ischaemia
Artificial Cells, Nanomedicine, and Biotechnology
Icariin (ICA)
polyethylene glycol monomethyl ether (mPEG)
fourier transform infrared spectroscopy (FTIR)
nuclear magnetic resonance spectroscopy (1H-NMR)
dynamic light scattering (DLS)
title mPEG-icariin nanoparticles for treating myocardial ischaemia
title_full mPEG-icariin nanoparticles for treating myocardial ischaemia
title_fullStr mPEG-icariin nanoparticles for treating myocardial ischaemia
title_full_unstemmed mPEG-icariin nanoparticles for treating myocardial ischaemia
title_short mPEG-icariin nanoparticles for treating myocardial ischaemia
title_sort mpeg icariin nanoparticles for treating myocardial ischaemia
topic Icariin (ICA)
polyethylene glycol monomethyl ether (mPEG)
fourier transform infrared spectroscopy (FTIR)
nuclear magnetic resonance spectroscopy (1H-NMR)
dynamic light scattering (DLS)
url https://www.tandfonline.com/doi/10.1080/21691401.2018.1554579
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