Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation
Md Al-Amin, Jiafu Cao, Muhammad Naeem, Hasanul Banna, Min-Soo Kim, Yunjin Jung, Hae Young Chung, Hyung Ryong Moon, Jin-Wook Yoo College of Pharmacy, Pusan National University, Busan, South Korea Abstract: Hyperpigmentation caused by melanin overproduction is a major skin disorder in humans. Inhibiti...
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2016-12-01
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| Series: | Drug Design, Development and Therapy |
| Subjects: | |
| Online Access: | https://www.dovepress.com/increased-therapeutic-efficacy-of-a-newly-synthesized-tyrosinase-inhib-peer-reviewed-article-DDDT |
| _version_ | 1818348196547526656 |
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| author | Al-Amin M Cao J Naeem M Banna H Kim M Jung Y Chung HY Moon HR Yoo J |
| author_facet | Al-Amin M Cao J Naeem M Banna H Kim M Jung Y Chung HY Moon HR Yoo J |
| author_sort | Al-Amin M |
| collection | DOAJ |
| description | Md Al-Amin, Jiafu Cao, Muhammad Naeem, Hasanul Banna, Min-Soo Kim, Yunjin Jung, Hae Young Chung, Hyung Ryong Moon, Jin-Wook Yoo College of Pharmacy, Pusan National University, Busan, South Korea Abstract: Hyperpigmentation caused by melanin overproduction is a major skin disorder in humans. Inhibition of tyrosinase, a key regulator of melanin production, has been used as an effective strategy to treat hyperpigmentation. In this study, we investigated the use of solid lipid nanoparticles (SLNs) as a highly effective and nontoxic means to deliver a newly synthesized potent tyrosinase inhibitor, MHY498, and to target melanocytes through the skin. MHY498-loaded SLNs (MHY-SLNs) were prepared by an oil-in-water emulsion solvent-evaporation method, and their morphological and physicochemical properties were characterized. MHY-SLNs showed a prolonged drug-release profile and higher skin permeation than that of MHY solution. In an in vivo evaluation of antimelanogenic activity, MHY-SLNs showed a prominent inhibitory effect against ultraviolet B-induced melanogenesis, resulting in no change in the skin color of C57BL/6 mouse, compared with that observed in an MHY solution-treated group and an untreated control group. The antimelanogenic effect of MHY-SLNs was further confirmed through Fontana–Masson staining. Importantly, MHY-SLNs did not induce any toxic effects in the L929 cell line. Overall, these data indicate that MHY-SLNs show promise in the topical treatment of hyperpigmentation. Keywords: melanogenesis, hyperpigmentation, MHY498, solid lipid nanoparticles, skin delivery |
| first_indexed | 2024-12-13T17:46:13Z |
| format | Article |
| id | doaj.art-37c625a29ca54959866ab83d233730ef |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-13T17:46:13Z |
| publishDate | 2016-12-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-37c625a29ca54959866ab83d233730ef2022-12-21T23:36:37ZengDove Medical PressDrug Design, Development and Therapy1177-88812016-12-01Volume 103947395730303Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentationAl-Amin MCao JNaeem MBanna HKim MJung YChung HYMoon HRYoo JMd Al-Amin, Jiafu Cao, Muhammad Naeem, Hasanul Banna, Min-Soo Kim, Yunjin Jung, Hae Young Chung, Hyung Ryong Moon, Jin-Wook Yoo College of Pharmacy, Pusan National University, Busan, South Korea Abstract: Hyperpigmentation caused by melanin overproduction is a major skin disorder in humans. Inhibition of tyrosinase, a key regulator of melanin production, has been used as an effective strategy to treat hyperpigmentation. In this study, we investigated the use of solid lipid nanoparticles (SLNs) as a highly effective and nontoxic means to deliver a newly synthesized potent tyrosinase inhibitor, MHY498, and to target melanocytes through the skin. MHY498-loaded SLNs (MHY-SLNs) were prepared by an oil-in-water emulsion solvent-evaporation method, and their morphological and physicochemical properties were characterized. MHY-SLNs showed a prolonged drug-release profile and higher skin permeation than that of MHY solution. In an in vivo evaluation of antimelanogenic activity, MHY-SLNs showed a prominent inhibitory effect against ultraviolet B-induced melanogenesis, resulting in no change in the skin color of C57BL/6 mouse, compared with that observed in an MHY solution-treated group and an untreated control group. The antimelanogenic effect of MHY-SLNs was further confirmed through Fontana–Masson staining. Importantly, MHY-SLNs did not induce any toxic effects in the L929 cell line. Overall, these data indicate that MHY-SLNs show promise in the topical treatment of hyperpigmentation. Keywords: melanogenesis, hyperpigmentation, MHY498, solid lipid nanoparticles, skin deliveryhttps://www.dovepress.com/increased-therapeutic-efficacy-of-a-newly-synthesized-tyrosinase-inhib-peer-reviewed-article-DDDTmelanogenesishyperpigmentationMHY498solid lipid nanoparticlesskin delivery |
| spellingShingle | Al-Amin M Cao J Naeem M Banna H Kim M Jung Y Chung HY Moon HR Yoo J Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation Drug Design, Development and Therapy melanogenesis hyperpigmentation MHY498 solid lipid nanoparticles skin delivery |
| title | Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation |
| title_full | Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation |
| title_fullStr | Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation |
| title_full_unstemmed | Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation |
| title_short | Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation |
| title_sort | increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation |
| topic | melanogenesis hyperpigmentation MHY498 solid lipid nanoparticles skin delivery |
| url | https://www.dovepress.com/increased-therapeutic-efficacy-of-a-newly-synthesized-tyrosinase-inhib-peer-reviewed-article-DDDT |
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