Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment
Ascorbic acid (AA) is a water-soluble vitamin that is found at high concentrations in normal skin. The important and well-known benefits of using AA in skin health include the stimulation of collagen synthesis and the assistance of protection against photo-oxidative damages. To maintain stability an...
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doaj-ee5df54d54f345fe9ee2dcd2d085df2b2021-06-01T00:20:46ZengMDPI AGCosmetics2079-92842021-05-018383810.3390/cosmetics8020038Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity AssessmentNatsumi Doi0Yoshifumi Yamada1Misaki Toyoshima2Yuki Kondo3Koichi Nakaoji4Kazuhiko Hamada5Masaaki Tatsuka6Department of Life Sciences, Faculty of Life and Environmental Sciences, Prefectural University of Hiroshima, Shoubara, Hiroshima 727-0023, JapanResearch & Development Division, PIAS Corporation, Kobe, Hyogo 651-2241, JapanResearch & Development Division, PIAS Corporation, Kobe, Hyogo 651-2241, JapanResearch & Development Division, PIAS Corporation, Kobe, Hyogo 651-2241, JapanResearch & Development Division, PIAS Corporation, Kobe, Hyogo 651-2241, JapanResearch & Development Division, PIAS Corporation, Kobe, Hyogo 651-2241, JapanDepartment of Life Sciences, Faculty of Life and Environmental Sciences, Prefectural University of Hiroshima, Shoubara, Hiroshima 727-0023, JapanAscorbic acid (AA) is a water-soluble vitamin that is found at high concentrations in normal skin. The important and well-known benefits of using AA in skin health include the stimulation of collagen synthesis and the assistance of protection against photo-oxidative damages. To maintain stability and improve drug delivery to the active site, a variety of AA derivatives have been chemically synthesized. Among these compounds, we focus here on a lipophilic derivative, 3-<i>O</i>-cetyl ascorbic acid (3-CetylAA), which remains poorly characterized for cosmetic applications. Uptake analysis in three healthy human volunteers’ skin was conducted using a serial tape-stripping technique detecting 3-CetylAA (on average, 128 ± 27 pmol per µg) in the stratum corneum after a 5-h topical treatment when treated with 25 mM 3-CetylAA-containing cream for 13 days twice daily and continuously. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) imaging of vertical cryosections of pig skin revealed the presence of 3-CetylAA in the epidermal layer after topical treatment with 3-CetylAA-containing cream. In sun-exposed human skin, 3-CetylAA improved the texture after treatment with 25 mM 3-CetylAA-containing cream for 4 weeks or more when used twice daily or continuously. An in vitro transformation assay using BALB/c 3T3 A31-1-1 cells demonstrated that 10 µM 3-CetylAA, which is the same concentration exhibited in vitro biological activities in another lipophilic AA derivative, 2-<i>O</i>-octadecyl ascorbic acid, was non-carcinogenic and did not potentiate the UVC-induced transformation frequency when applied for 3 days after UVC irradiation. These results demonstrate that 3-CetylAA is a promising candidate as a lipophilic derivative of AA for cosmetic purposes.https://www.mdpi.com/2079-9284/8/2/383-<i>O</i>-cetyl ascorbic acidlipophilic derivativesun exposureskin carestratum corneumepidermis |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Natsumi Doi Yoshifumi Yamada Misaki Toyoshima Yuki Kondo Koichi Nakaoji Kazuhiko Hamada Masaaki Tatsuka |
spellingShingle |
Natsumi Doi Yoshifumi Yamada Misaki Toyoshima Yuki Kondo Koichi Nakaoji Kazuhiko Hamada Masaaki Tatsuka Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment Cosmetics 3-<i>O</i>-cetyl ascorbic acid lipophilic derivative sun exposure skin care stratum corneum epidermis |
author_facet |
Natsumi Doi Yoshifumi Yamada Misaki Toyoshima Yuki Kondo Koichi Nakaoji Kazuhiko Hamada Masaaki Tatsuka |
author_sort |
Natsumi Doi |
title |
Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment |
title_short |
Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment |
title_full |
Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment |
title_fullStr |
Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment |
title_full_unstemmed |
Facial Treatment with 3-<i>O</i>-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment |
title_sort |
facial treatment with 3-<i>o</i>-cetyl ascorbic acid for improvement of skin texture: uptake, effectiveness, and in vitro carcinogenicity assessment |
publisher |
MDPI AG |
series |
Cosmetics |
issn |
2079-9284 |
publishDate |
2021-05-01 |
description |
Ascorbic acid (AA) is a water-soluble vitamin that is found at high concentrations in normal skin. The important and well-known benefits of using AA in skin health include the stimulation of collagen synthesis and the assistance of protection against photo-oxidative damages. To maintain stability and improve drug delivery to the active site, a variety of AA derivatives have been chemically synthesized. Among these compounds, we focus here on a lipophilic derivative, 3-<i>O</i>-cetyl ascorbic acid (3-CetylAA), which remains poorly characterized for cosmetic applications. Uptake analysis in three healthy human volunteers’ skin was conducted using a serial tape-stripping technique detecting 3-CetylAA (on average, 128 ± 27 pmol per µg) in the stratum corneum after a 5-h topical treatment when treated with 25 mM 3-CetylAA-containing cream for 13 days twice daily and continuously. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) imaging of vertical cryosections of pig skin revealed the presence of 3-CetylAA in the epidermal layer after topical treatment with 3-CetylAA-containing cream. In sun-exposed human skin, 3-CetylAA improved the texture after treatment with 25 mM 3-CetylAA-containing cream for 4 weeks or more when used twice daily or continuously. An in vitro transformation assay using BALB/c 3T3 A31-1-1 cells demonstrated that 10 µM 3-CetylAA, which is the same concentration exhibited in vitro biological activities in another lipophilic AA derivative, 2-<i>O</i>-octadecyl ascorbic acid, was non-carcinogenic and did not potentiate the UVC-induced transformation frequency when applied for 3 days after UVC irradiation. These results demonstrate that 3-CetylAA is a promising candidate as a lipophilic derivative of AA for cosmetic purposes. |
topic |
3-<i>O</i>-cetyl ascorbic acid lipophilic derivative sun exposure skin care stratum corneum epidermis |
url |
https://www.mdpi.com/2079-9284/8/2/38 |
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