Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough
Naringenin (NRG) is a natural compound with several biological activities; however, its bioavailability is limited owing to poor aqueous solubility. In this study, NRG nanoparticles (NPs) were prepared using the wet media milling method. To obtain NRG NPs with a small particle size and high drug-loa...
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MDPI AG
2022-06-01
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author | Zhengqi Dong Xiangtao Wang Mingyue Wang Rui Wang Zheng Meng Xiaotong Wang Bo Yu Meihua Han Yifei Guo |
author_facet | Zhengqi Dong Xiangtao Wang Mingyue Wang Rui Wang Zheng Meng Xiaotong Wang Bo Yu Meihua Han Yifei Guo |
author_sort | Zhengqi Dong |
collection | DOAJ |
description | Naringenin (NRG) is a natural compound with several biological activities; however, its bioavailability is limited owing to poor aqueous solubility. In this study, NRG nanoparticles (NPs) were prepared using the wet media milling method. To obtain NRG NPs with a small particle size and high drug-loading content, the preparation conditions, including stirring time, temperature, stirring speed, and milling media amount, were optimized. The NRG (30 mg) and D-α-tocopherol polyethylene glycol succinate (10 mg) were wet-milled in deionized water (2 mL) with 10 g of zirconia beads via stirring at 50 °C for 2 h at a stirring speed of 300 rpm. As a result, the NRG NPs, with sheet-like morphology and a diameter of approximately 182.2 nm, were successfully prepared. The NRG NPs were stable in the gastrointestinal system and were released effectively after entering the blood circulation. In vivo experiments indicated that the NRG NPs have good antitussive effects. The cough inhibition rate after the administration of the NRG NPs was 66.7%, cough frequency was three times lower, and the potential period was 1.8 times longer than that in the blank model group. In addition, the enzyme biomarkers and histological analysis results revealed that the NRG NPs can effectively regulate the inflammatory and oxidative stress response. In conclusion, the NRG NPs exhibited good oral bioavailability and promoted antitussive and anti-inflammatory effects. |
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spelling | doaj.art-6a9568feedc34cfcb38e57f2a994e8b32023-11-23T18:10:21ZengMDPI AGMolecules1420-30492022-06-012712373610.3390/molecules27123736Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious CoughZhengqi Dong0Xiangtao Wang1Mingyue Wang2Rui Wang3Zheng Meng4Xiaotong Wang5Bo Yu6Meihua Han7Yifei Guo8Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaCollege of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin 150040, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaInstitute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, ChinaNaringenin (NRG) is a natural compound with several biological activities; however, its bioavailability is limited owing to poor aqueous solubility. In this study, NRG nanoparticles (NPs) were prepared using the wet media milling method. To obtain NRG NPs with a small particle size and high drug-loading content, the preparation conditions, including stirring time, temperature, stirring speed, and milling media amount, were optimized. The NRG (30 mg) and D-α-tocopherol polyethylene glycol succinate (10 mg) were wet-milled in deionized water (2 mL) with 10 g of zirconia beads via stirring at 50 °C for 2 h at a stirring speed of 300 rpm. As a result, the NRG NPs, with sheet-like morphology and a diameter of approximately 182.2 nm, were successfully prepared. The NRG NPs were stable in the gastrointestinal system and were released effectively after entering the blood circulation. In vivo experiments indicated that the NRG NPs have good antitussive effects. The cough inhibition rate after the administration of the NRG NPs was 66.7%, cough frequency was three times lower, and the potential period was 1.8 times longer than that in the blank model group. In addition, the enzyme biomarkers and histological analysis results revealed that the NRG NPs can effectively regulate the inflammatory and oxidative stress response. In conclusion, the NRG NPs exhibited good oral bioavailability and promoted antitussive and anti-inflammatory effects.https://www.mdpi.com/1420-3049/27/12/3736naringeninnanoparticleantitussive effectantioxidant effectanti-inflammatory effect |
spellingShingle | Zhengqi Dong Xiangtao Wang Mingyue Wang Rui Wang Zheng Meng Xiaotong Wang Bo Yu Meihua Han Yifei Guo Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough Molecules naringenin nanoparticle antitussive effect antioxidant effect anti-inflammatory effect |
title | Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough |
title_full | Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough |
title_fullStr | Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough |
title_full_unstemmed | Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough |
title_short | Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough |
title_sort | optimization of naringenin nanoparticles to improve the antitussive effects on post infectious cough |
topic | naringenin nanoparticle antitussive effect antioxidant effect anti-inflammatory effect |
url | https://www.mdpi.com/1420-3049/27/12/3736 |
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