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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Main Authors: Zhengqi Dong, Xiangtao Wang, Mingyue Wang, Rui Wang, Zheng Meng, Xiaotong Wang, Bo Yu, Meihua Han, Yifei Guo
Format: Article
Language:English
Published: MDPI AG 2022-06-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/27/12/3736
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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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