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用于皮肤再生的辅酶Q10负载微乳的局部递送

Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration.

作者信息

Ryu Kyeong-A, Park Phil June, Kim Seong-Bo, Bin Bum-Ho, Jang Dong-Jin, Kim Sung Tae

机构信息

Institute of Digital Anti-Aging Healthcare, Inje University, Gimhae 50834, Korea.

Department of Genetic Engineering, Sungkyunkwan University, Suwon-si, Gyeonggi-do 16499, Korea.

出版信息

Pharmaceutics. 2020 Apr 7;12(4):332. doi: 10.3390/pharmaceutics12040332.

DOI:10.3390/pharmaceutics12040332
PMID:32272811
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7238272/
Abstract

The aim of this study was to develop a coenzyme Q10 (CoQ10) microemulsion system with improved solubility, penetration, and wound healing efficacy. Based on the pseudo-ternary diagram, microemulsions containing isopropyl myristate (IPM), Cremophor EL, and Transcutol HP were selected and confirmed to be nanosized (<20 nm) and thermodynamically stable based on the dilution and thermodynamic stability tests. The CoQ10-loaded microemulsion with a surfactant/co-surfactant (S/CoS) ratio of 2:1 (w/w %) demonstrated a higher permeation efficacy compared to microemulsions with S/CoS ratio of 3:1 or 4:1 (w/w %). Additionally, the CoQ10-loaded microemulsion with an S/CoS ratio of 2:1 demonstrated a relatively rapid wound healing effect in keratinocytes and fibroblasts. Overall, these data suggest that a microemulsion based on IPM, Cremophor EL, and Transcutol HP could be an effective vehicle for the topical administration of CoQ10 and could be utilized for the application of other therapeutic agents that have difficulty in penetrating the skin.

摘要

本研究的目的是开发一种具有改善的溶解性、渗透性和伤口愈合功效的辅酶Q10（CoQ10）微乳体系。基于伪三元相图，选择了含有肉豆蔻酸异丙酯（IPM）、聚氧乙烯蓖麻油（Cremophor EL）和二乙二醇单乙基醚（Transcutol HP）的微乳，并根据稀释和热力学稳定性测试确认其为纳米尺寸（<20 nm）且热力学稳定。与表面活性剂/助表面活性剂（S/CoS）比例为3:1或4:1（w/w%）的微乳相比，S/CoS比例为2:1（w/w%）的负载CoQ10的微乳表现出更高的渗透功效。此外，S/CoS比例为2:1的负载CoQ10的微乳在角质形成细胞和成纤维细胞中表现出相对快速的伤口愈合效果。总体而言，这些数据表明，基于IPM、Cremophor EL和Transcutol HP的微乳可能是CoQ10局部给药的有效载体，并且可用于应用其他难以穿透皮肤的治疗剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/92a14ae214b4/pharmaceutics-12-00332-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/d1eaf6a75b53/pharmaceutics-12-00332-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/c4c2fa994d65/pharmaceutics-12-00332-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/f79557c1dbbb/pharmaceutics-12-00332-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/0fbc44277a02/pharmaceutics-12-00332-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/92a14ae214b4/pharmaceutics-12-00332-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/d1eaf6a75b53/pharmaceutics-12-00332-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/c4c2fa994d65/pharmaceutics-12-00332-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/f79557c1dbbb/pharmaceutics-12-00332-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/0fbc44277a02/pharmaceutics-12-00332-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa0c/7238272/92a14ae214b4/pharmaceutics-12-00332-g005.jpg

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[7]
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[10]
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本文引用的文献

[1]
Formation of Food Grade Microemulsion with Rice Glycosphingolipids to Enhance the Oral Absorption of Coenzyme Q10.

Foods. 2019-10-15

[2]
Scratch Wound Healing Assay.

Methods Mol Biol. 2020

[3]
Environmental Stressors on Skin Aging. Mechanistic Insights.

Front Pharmacol. 2019-7-9

[4]
Skin Penetration and Permeation Properties of Transcutol®-Neat or Diluted Mixtures.

AAPS PharmSciTech. 2018-11-12

[5]
Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation⁻Processing Aspects and Challenges.

Pharmaceutics. 2018-7-8

[6]
Drug delivery systems and materials for wound healing applications.

Adv Drug Deliv Rev. 2018-4-5

[7]
Microemulsion-based delivery of triamcinolone acetonide to posterior segment of eye using chitosan and butter oil as permeation enhancer: an in vitro and in vivo investigation.

J Microencapsul. 2018-1-22

[8]
Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals.

Drug Dev Ind Pharm. 2017-12-26

[9]
Optimization of nutraceutical coenzyme Q10 nanoemulsion with improved skin permeability and anti-wrinkle efficiency.

Drug Dev Ind Pharm. 2018-2

[10]
Topical Nano and Microemulsions for Skin Delivery.

Pharmaceutics. 2017-9-21

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