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新型合成酪氨酸酶抑制剂通过固体脂质纳米粒在色素沉着局部治疗中的治疗效果增强

Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation.

作者信息

Al-Amin Md, Cao Jiafu, Naeem Muhammad, Banna Hasanul, Kim Min-Soo, Jung Yunjin, Chung Hae Young, Moon Hyung Ryong, Yoo Jin-Wook

机构信息

College of Pharmacy, Pusan National University, Busan, South Korea.

出版信息

Drug Des Devel Ther. 2016 Dec 2;10:3947-3957. doi: 10.2147/DDDT.S123759. eCollection 2016.

DOI:10.2147/DDDT.S123759
PMID:27980392
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5144896/
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.

摘要

由黑色素过度生成引起的色素沉着是人类主要的皮肤疾病。抑制酪氨酸酶（黑色素生成的关键调节因子）已被用作治疗色素沉着的有效策略。在本研究中，我们研究了使用固体脂质纳米粒（SLNs）作为一种高效且无毒的手段，来递送新合成的强效酪氨酸酶抑制剂MHY498，并通过皮肤靶向黑素细胞。通过水包油乳液溶剂蒸发法制备了负载MHY498的SLNs（MHY-SLNs），并对其形态和理化性质进行了表征。MHY-SLNs显示出比MHY溶液更长的药物释放曲线和更高的皮肤渗透性。在抗黑色素生成活性的体内评估中，MHY-SLNs对紫外线B诱导的黑色素生成显示出显著的抑制作用，与MHY溶液处理组和未处理的对照组相比，C57BL/6小鼠的皮肤颜色没有变化。通过Fontana-Masson染色进一步证实了MHY-SLNs的抗黑色素生成作用。重要的是，MHY-SLNs在L929细胞系中未诱导任何毒性作用。总体而言，这些数据表明MHY-SLNs在色素沉着的局部治疗中显示出前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/b9f0eb943a80/dddt-10-3947Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/735a63de9625/dddt-10-3947Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/2e605a3267ad/dddt-10-3947Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/2fe5ca759c6c/dddt-10-3947Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/03c2468da7b9/dddt-10-3947Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/041f0d92a47f/dddt-10-3947Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/bf319693f132/dddt-10-3947Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/b9f0eb943a80/dddt-10-3947Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/735a63de9625/dddt-10-3947Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/2e605a3267ad/dddt-10-3947Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/2fe5ca759c6c/dddt-10-3947Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/03c2468da7b9/dddt-10-3947Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/041f0d92a47f/dddt-10-3947Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/bf319693f132/dddt-10-3947Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2c/5144896/b9f0eb943a80/dddt-10-3947Fig7.jpg

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