Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging
Retinoids, one of the most robust bioactive materials, have been widely used to improve various dermatological and pathological conditions. The body has an endogenous mechanism that modulates the exogenous retinoid above physiological concentrations, which limits the bioavailability or pharmacologic...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/11/2412 |
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| author | Seongsu Kang Hyejin Lee Seung-Hyun Jun Sun-Gyoo Park Nae-Gyu Kang |
| author_facet | Seongsu Kang Hyejin Lee Seung-Hyun Jun Sun-Gyoo Park Nae-Gyu Kang |
| author_sort | Seongsu Kang |
| collection | DOAJ |
| description | Retinoids, one of the most robust bioactive materials, have been widely used to improve various dermatological and pathological conditions. The body has an endogenous mechanism that modulates the exogenous retinoid above physiological concentrations, which limits the bioavailability or pharmacological efficacy of retinoids. Considering that most retinoids trigger extensive irritation in users, it is necessary to enhance the pharmacological efficacy of retinoids, thereby achieving a higher efficacy at a lower dosage. Here, we present approaches for enhancing the efficacy of retinol by enhancing retinoid-induced RAR gamma (RAR-γ) activity and inhibiting the hydroxylation of retinoic acid. Using both in vitro and ex vivo experiments, retinoid boosters were demonstrated to enhance pharmacological efficacy. A small pilot study was conducted to investigate the efficacy for improvement of facial wrinkles, whose results revealed that these boosters could enhance the pharmacological efficacy of topical applications of both retinol and retinoic acid for cosmetic use. These results promote not only a higher compliance among retinoids users, but also provide significant insights into the mechanisms underlying the action of retinoids. |
| first_indexed | 2024-03-09T18:44:45Z |
| format | Article |
| id | doaj.art-226c24c013b6436cad50b6289f5232ca |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T18:44:45Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-226c24c013b6436cad50b6289f5232ca2023-11-24T06:21:50ZengMDPI AGPharmaceutics1999-49232022-11-011411241210.3390/pharmaceutics14112412Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-AgingSeongsu Kang0Hyejin Lee1Seung-Hyun Jun2Sun-Gyoo Park3Nae-Gyu Kang4LG Household and Health Care R&D Center, Seoul 07795, KoreaLG Household and Health Care R&D Center, Seoul 07795, KoreaLG Household and Health Care R&D Center, Seoul 07795, KoreaLG Household and Health Care R&D Center, Seoul 07795, KoreaLG Household and Health Care R&D Center, Seoul 07795, KoreaRetinoids, one of the most robust bioactive materials, have been widely used to improve various dermatological and pathological conditions. The body has an endogenous mechanism that modulates the exogenous retinoid above physiological concentrations, which limits the bioavailability or pharmacological efficacy of retinoids. Considering that most retinoids trigger extensive irritation in users, it is necessary to enhance the pharmacological efficacy of retinoids, thereby achieving a higher efficacy at a lower dosage. Here, we present approaches for enhancing the efficacy of retinol by enhancing retinoid-induced RAR gamma (RAR-γ) activity and inhibiting the hydroxylation of retinoic acid. Using both in vitro and ex vivo experiments, retinoid boosters were demonstrated to enhance pharmacological efficacy. A small pilot study was conducted to investigate the efficacy for improvement of facial wrinkles, whose results revealed that these boosters could enhance the pharmacological efficacy of topical applications of both retinol and retinoic acid for cosmetic use. These results promote not only a higher compliance among retinoids users, but also provide significant insights into the mechanisms underlying the action of retinoids.https://www.mdpi.com/1999-4923/14/11/2412retinolretinoidcosmeticsphotoagingretinoic acid receptorhydroxylation |
| spellingShingle | Seongsu Kang Hyejin Lee Seung-Hyun Jun Sun-Gyoo Park Nae-Gyu Kang Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging Pharmaceutics retinol retinoid cosmetics photoaging retinoic acid receptor hydroxylation |
| title | Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging |
| title_full | Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging |
| title_fullStr | Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging |
| title_full_unstemmed | Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging |
| title_short | Enhancement of Efficacy of Retinoids through Enhancing Retinoid-Induced RAR Activity and Inhibiting Hydroxylation of Retinoic Acid, and Its Clinical Efficacy on Photo-Aging |
| title_sort | enhancement of efficacy of retinoids through enhancing retinoid induced rar activity and inhibiting hydroxylation of retinoic acid and its clinical efficacy on photo aging |
| topic | retinol retinoid cosmetics photoaging retinoic acid receptor hydroxylation |
| url | https://www.mdpi.com/1999-4923/14/11/2412 |
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