Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia
Atraric acid (AA) is a phenolic compound isolated from <i>Stereocaulon japonicum</i> that has demonstrated anti-androgen properties and was used to design an alternative formulation for the treatment of alopecia. This new topical formulation was designed using a solvent mixture system co...
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MDPI AG
2023-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/2/340 |
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| author | Sultan Pulat Laxman Subedi Prashant Pandey Suresh R. Bhosle Jae-Seoun Hur Jung-Hyun Shim Seung-Sik Cho Ki-Taek Kim Hyung-Ho Ha Hangun Kim Jin Woo Park |
| author_facet | Sultan Pulat Laxman Subedi Prashant Pandey Suresh R. Bhosle Jae-Seoun Hur Jung-Hyun Shim Seung-Sik Cho Ki-Taek Kim Hyung-Ho Ha Hangun Kim Jin Woo Park |
| author_sort | Sultan Pulat |
| collection | DOAJ |
| description | Atraric acid (AA) is a phenolic compound isolated from <i>Stereocaulon japonicum</i> that has demonstrated anti-androgen properties and was used to design an alternative formulation for the treatment of alopecia. This new topical formulation was designed using a solvent mixture system composed of ethanol as a volatile vehicle, oleic acid as a permeation enhancer, and water for skin hydration. The ideal topical AA formulation (AA–TF#15) exhibited an 8.77-fold higher human skin flux and a 570% increase in dermal drug deposition, compared to 1% (<i>w</i>/<i>w</i>) AA in ethanol. In addition, compared to other formulations, AA–TF#15 (1% [<i>w</i>/<i>w</i>] AA) activated keratinocytes and human dermal papilla cell proliferation at a concentration of 50 µM AA, which is equivalent to 50 µM minoxidil. Moreover, AA–TF#15 treatment produced a significant increase in hair regrowth by 58.0% and 41.9% compared to the 1% (<i>w</i>/<i>w</i>) minoxidil and oral finasteride (1 mg/kg)-treated mice. In addition, AA–TF#15 showed a higher expression level of aldehyde dehydrogenase 1, β-catenin, cyclin D1, and pyruvate kinase M2 proteins in the skin of AA–TF#15-treated mice compared to that of those treated with minoxidil and oral finasteride. These findings suggest AA–TF#15 is an effective formulation for the treatment of scalp androgenic alopecia. |
| first_indexed | 2024-03-11T08:17:56Z |
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| id | doaj.art-70768615e4f94ae582c1a9a49ca272c2 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T08:17:56Z |
| publishDate | 2023-01-01 |
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| series | Pharmaceutics |
| spelling | doaj.art-70768615e4f94ae582c1a9a49ca272c22023-11-16T22:38:36ZengMDPI AGPharmaceutics1999-49232023-01-0115234010.3390/pharmaceutics15020340Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic AlopeciaSultan Pulat0Laxman Subedi1Prashant Pandey2Suresh R. Bhosle3Jae-Seoun Hur4Jung-Hyun Shim5Seung-Sik Cho6Ki-Taek Kim7Hyung-Ho Ha8Hangun Kim9Jin Woo Park10College of Pharmacy, Sunchon National University, Sunchon-si 57922, Jeonnam, Republic of KoreaDepartment of Biomedicine, Health & Life Convergence Sciences, BK21 Four, Biomedical and Healthcare Research Institute, Mokpo National University, Muan-gun 58554, Jeonnam, Republic of KoreaDepartment of Biomedicine, Health & Life Convergence Sciences, BK21 Four, Biomedical and Healthcare Research Institute, Mokpo National University, Muan-gun 58554, Jeonnam, Republic of KoreaCollege of Pharmacy, Sunchon National University, Sunchon-si 57922, Jeonnam, Republic of KoreaKorean Lichen Research Institute, Sunchon National University, Sunchon-si 57922, Jeonnam, Republic of KoreaDepartment of Biomedicine, Health & Life Convergence Sciences, BK21 Four, Biomedical and Healthcare Research Institute, Mokpo National University, Muan-gun 58554, Jeonnam, Republic of KoreaDepartment of Biomedicine, Health & Life Convergence Sciences, BK21 Four, Biomedical and Healthcare Research Institute, Mokpo National University, Muan-gun 58554, Jeonnam, Republic of KoreaDepartment of Biomedicine, Health & Life Convergence Sciences, BK21 Four, Biomedical and Healthcare Research Institute, Mokpo National University, Muan-gun 58554, Jeonnam, Republic of KoreaCollege of Pharmacy, Sunchon National University, Sunchon-si 57922, Jeonnam, Republic of KoreaCollege of Pharmacy, Sunchon National University, Sunchon-si 57922, Jeonnam, Republic of KoreaDepartment of Biomedicine, Health & Life Convergence Sciences, BK21 Four, Biomedical and Healthcare Research Institute, Mokpo National University, Muan-gun 58554, Jeonnam, Republic of KoreaAtraric acid (AA) is a phenolic compound isolated from <i>Stereocaulon japonicum</i> that has demonstrated anti-androgen properties and was used to design an alternative formulation for the treatment of alopecia. This new topical formulation was designed using a solvent mixture system composed of ethanol as a volatile vehicle, oleic acid as a permeation enhancer, and water for skin hydration. The ideal topical AA formulation (AA–TF#15) exhibited an 8.77-fold higher human skin flux and a 570% increase in dermal drug deposition, compared to 1% (<i>w</i>/<i>w</i>) AA in ethanol. In addition, compared to other formulations, AA–TF#15 (1% [<i>w</i>/<i>w</i>] AA) activated keratinocytes and human dermal papilla cell proliferation at a concentration of 50 µM AA, which is equivalent to 50 µM minoxidil. Moreover, AA–TF#15 treatment produced a significant increase in hair regrowth by 58.0% and 41.9% compared to the 1% (<i>w</i>/<i>w</i>) minoxidil and oral finasteride (1 mg/kg)-treated mice. In addition, AA–TF#15 showed a higher expression level of aldehyde dehydrogenase 1, β-catenin, cyclin D1, and pyruvate kinase M2 proteins in the skin of AA–TF#15-treated mice compared to that of those treated with minoxidil and oral finasteride. These findings suggest AA–TF#15 is an effective formulation for the treatment of scalp androgenic alopecia.https://www.mdpi.com/1999-4923/15/2/340atraric acidtopical deliveryskin penetrationdermal papilla cell proliferationandrogenic alopeciahair regrowth |
| spellingShingle | Sultan Pulat Laxman Subedi Prashant Pandey Suresh R. Bhosle Jae-Seoun Hur Jung-Hyun Shim Seung-Sik Cho Ki-Taek Kim Hyung-Ho Ha Hangun Kim Jin Woo Park Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia Pharmaceutics atraric acid topical delivery skin penetration dermal papilla cell proliferation androgenic alopecia hair regrowth |
| title | Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia |
| title_full | Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia |
| title_fullStr | Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia |
| title_full_unstemmed | Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia |
| title_short | Topical Delivery of Atraric Acid Derived from <i>Stereocaulon japonicum</i> with Enhanced Skin Permeation and Hair Regrowth Activity for Androgenic Alopecia |
| title_sort | topical delivery of atraric acid derived from i stereocaulon japonicum i with enhanced skin permeation and hair regrowth activity for androgenic alopecia |
| topic | atraric acid topical delivery skin penetration dermal papilla cell proliferation androgenic alopecia hair regrowth |
| url | https://www.mdpi.com/1999-4923/15/2/340 |
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