Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing

The excessive production of reactive oxygen species (ROS) causes harmful effects, including biomolecular damage and inflammation. ROS due to ultraviolet rays, blue light, and fine dust harm the skin, causing urban-related aging. Therefore, a strong antioxidant that relieves oxidative stress in the s...

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Main Authors: HeeSeon Yang, Sohyeon Yu, Jisu Kim, KumJu Baek, Young-Ran Lee, Hye Sun Lee, Won Il Choi, Daekyung Sung
Format: Article
Language:English
Published: MDPI AG 2022-02-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/14/3/521
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author HeeSeon Yang
Sohyeon Yu
Jisu Kim
KumJu Baek
Young-Ran Lee
Hye Sun Lee
Won Il Choi
Daekyung Sung
author_facet HeeSeon Yang
Sohyeon Yu
Jisu Kim
KumJu Baek
Young-Ran Lee
Hye Sun Lee
Won Il Choi
Daekyung Sung
author_sort HeeSeon Yang
collection DOAJ
description The excessive production of reactive oxygen species (ROS) causes harmful effects, including biomolecular damage and inflammation. ROS due to ultraviolet rays, blue light, and fine dust harm the skin, causing urban-related aging. Therefore, a strong antioxidant that relieves oxidative stress in the skin and removes ROS is required. Idebenone (IB) is a powerful antioxidant but is poorly soluble and thus has low solubility in water, resulting in low bioavailability. In this study, IB-loaded nanoparticles (IB@NPs) were synthesized by loading IB without an organic solvent into nanoparticles that can provide high loading efficiency and stability for solubilization. Indeed, the synthesized IB@NPs exhibited long-term stability through dynamic light scattering, methylene blue staining, and redispersion assays, and IB@NPs prepared with a 5 wt% IB loading content were found to be optimal. The antioxidant activity of IB@NPs evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay was significantly higher than that of unloaded IB. In addition, IB@NPs showed excellent biocompatibility, inhibited oxidative damage to mouse NIH-3T3 fibroblasts, and reduced intracellular ROS generation according to an in vitro DPPH antioxidant assay. Most notably, IB@NPs significantly promoted wound healing in vitro, as demonstrated by scratch assays. Therefore, as carriers with excellent stability, IB@NPs have potential cosmetic and pharmaceutical applications.
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spelling doaj.art-33a283ee18ed4928a412e242b7ddb9ba2023-11-30T21:56:04ZengMDPI AGPharmaceutics1999-49232022-02-0114352110.3390/pharmaceutics14030521Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound HealingHeeSeon Yang0Sohyeon Yu1Jisu Kim2KumJu Baek3Young-Ran Lee4Hye Sun Lee5Won Il Choi6Daekyung Sung7Center for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaThe excessive production of reactive oxygen species (ROS) causes harmful effects, including biomolecular damage and inflammation. ROS due to ultraviolet rays, blue light, and fine dust harm the skin, causing urban-related aging. Therefore, a strong antioxidant that relieves oxidative stress in the skin and removes ROS is required. Idebenone (IB) is a powerful antioxidant but is poorly soluble and thus has low solubility in water, resulting in low bioavailability. In this study, IB-loaded nanoparticles (IB@NPs) were synthesized by loading IB without an organic solvent into nanoparticles that can provide high loading efficiency and stability for solubilization. Indeed, the synthesized IB@NPs exhibited long-term stability through dynamic light scattering, methylene blue staining, and redispersion assays, and IB@NPs prepared with a 5 wt% IB loading content were found to be optimal. The antioxidant activity of IB@NPs evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay was significantly higher than that of unloaded IB. In addition, IB@NPs showed excellent biocompatibility, inhibited oxidative damage to mouse NIH-3T3 fibroblasts, and reduced intracellular ROS generation according to an in vitro DPPH antioxidant assay. Most notably, IB@NPs significantly promoted wound healing in vitro, as demonstrated by scratch assays. Therefore, as carriers with excellent stability, IB@NPs have potential cosmetic and pharmaceutical applications.https://www.mdpi.com/1999-4923/14/3/521idebenonePEG-40 hydrogenated castor oilnanoparticlesolubilizationantioxidant activitywound healing
spellingShingle HeeSeon Yang
Sohyeon Yu
Jisu Kim
KumJu Baek
Young-Ran Lee
Hye Sun Lee
Won Il Choi
Daekyung Sung
Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing
Pharmaceutics
idebenone
PEG-40 hydrogenated castor oil
nanoparticle
solubilization
antioxidant activity
wound healing
title Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing
title_full Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing
title_fullStr Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing
title_full_unstemmed Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing
title_short Facile Solvent-Free Preparation of Antioxidant Idebenone-Loaded Nanoparticles for Efficient Wound Healing
title_sort facile solvent free preparation of antioxidant idebenone loaded nanoparticles for efficient wound healing
topic idebenone
PEG-40 hydrogenated castor oil
nanoparticle
solubilization
antioxidant activity
wound healing
url https://www.mdpi.com/1999-4923/14/3/521
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