Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders
Excessive melanin deposition in the skin leads to various skin pigmentation diseases, such as chloasma and age spots. The deposition is induced by several factors, including tyrosinase activities and ultraviolet-induced oxidative stress. Herein, we propose a multi-component, multi-pathway drug combi...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-08-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/15/15/3296 |
| _version_ | 1797586131161710592 |
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| author | Chenxin Yan Mengzhen Xing Suohui Zhang Yunhua Gao |
| author_facet | Chenxin Yan Mengzhen Xing Suohui Zhang Yunhua Gao |
| author_sort | Chenxin Yan |
| collection | DOAJ |
| description | Excessive melanin deposition in the skin leads to various skin pigmentation diseases, such as chloasma and age spots. The deposition is induced by several factors, including tyrosinase activities and ultraviolet-induced oxidative stress. Herein, we propose a multi-component, multi-pathway drug combination, with glabridin, 3-O-ethyl-L-ascorbic acid, and tranexamic acid employed as, respectively, a tyrosinase inhibitor, an antioxidant, and a melanin transmission inhibitor. Considering the poor skin permeability associated with topical application, dissolving microneedles (MNs) prepared with hyaluronic acid/poly(vinyl alcohol)/poly(vinylpyrrolidone) were developed to load the drug combination. The drug-loaded microneedles (DMNs) presented outstanding skin insertion, dissolution, and drug delivery properties. In vitro experiments confirmed that DMNs loaded with active ingredients had significant antioxidant and inhibitory effects on tyrosinase activity. Furthermore, the production of melanin both in melanoma cells (B16-F10) and in zebrafish was directly reduced after using DMNs. Clinical studies demonstrated the DMNs’ safety and showed that they have the ability to effectively reduce chloasma and age spots. This study indicated that a complex DMN based on a multifunctional combination is a valuable depigmentation product worthy of clinical application. |
| first_indexed | 2024-03-11T00:18:56Z |
| format | Article |
| id | doaj.art-ef4246be219b4624be1c746b3f13dac2 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-11T00:18:56Z |
| publishDate | 2023-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-ef4246be219b4624be1c746b3f13dac22023-11-18T23:29:13ZengMDPI AGPolymers2073-43602023-08-011515329610.3390/polym15153296Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation DisordersChenxin Yan0Mengzhen Xing1Suohui Zhang2Yunhua Gao3Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaKey Laboratory of New Material Research Institute, Department of Acupuncture-Moxibustion and Tuina, Shandong University of Traditional Chinese Medicine, Jinan 250355, ChinaKey Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaKey Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaExcessive melanin deposition in the skin leads to various skin pigmentation diseases, such as chloasma and age spots. The deposition is induced by several factors, including tyrosinase activities and ultraviolet-induced oxidative stress. Herein, we propose a multi-component, multi-pathway drug combination, with glabridin, 3-O-ethyl-L-ascorbic acid, and tranexamic acid employed as, respectively, a tyrosinase inhibitor, an antioxidant, and a melanin transmission inhibitor. Considering the poor skin permeability associated with topical application, dissolving microneedles (MNs) prepared with hyaluronic acid/poly(vinyl alcohol)/poly(vinylpyrrolidone) were developed to load the drug combination. The drug-loaded microneedles (DMNs) presented outstanding skin insertion, dissolution, and drug delivery properties. In vitro experiments confirmed that DMNs loaded with active ingredients had significant antioxidant and inhibitory effects on tyrosinase activity. Furthermore, the production of melanin both in melanoma cells (B16-F10) and in zebrafish was directly reduced after using DMNs. Clinical studies demonstrated the DMNs’ safety and showed that they have the ability to effectively reduce chloasma and age spots. This study indicated that a complex DMN based on a multifunctional combination is a valuable depigmentation product worthy of clinical application.https://www.mdpi.com/2073-4360/15/15/3296glabridin3-O-Ethyl-L-ascorbic acidtranexamic acidmicroneedlespigmentationmultifunctional drug |
| spellingShingle | Chenxin Yan Mengzhen Xing Suohui Zhang Yunhua Gao Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders Polymers glabridin 3-O-Ethyl-L-ascorbic acid tranexamic acid microneedles pigmentation multifunctional drug |
| title | Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders |
| title_full | Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders |
| title_fullStr | Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders |
| title_full_unstemmed | Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders |
| title_short | Clinical Development and Evaluation of a Multi-Component Dissolving Microneedle Patch for Skin Pigmentation Disorders |
| title_sort | clinical development and evaluation of a multi component dissolving microneedle patch for skin pigmentation disorders |
| topic | glabridin 3-O-Ethyl-L-ascorbic acid tranexamic acid microneedles pigmentation multifunctional drug |
| url | https://www.mdpi.com/2073-4360/15/15/3296 |
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