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In vitro and in vivo evaluation of MHY908-loaded nanostructured lipid carriers for the topical treatment of hyperpigmentation

Authors
Banna, HasanulHasan, NurhasniLee, JuhoKim, JihyunCao, JiafuLee, Eun HeeMoon, Hyung RyongChung, Hae YoungYoo, Jin-Wook
Issue Date
12월-2018
Publisher
ELSEVIER
Keywords
Anti-melanogenesis; Tyrosinase inhibitor; MHY908; Nanostructured lipid carrier; Topical drug delivery
Citation
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, v.48, pp.457 - 465
Indexed
SCIE
SCOPUS
Journal Title
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
Volume
48
Start Page
457
End Page
465
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/71410
DOI
10.1016/j.jddst.2018.10.032
ISSN
1773-2247
Abstract
Hyperpigmentation disorder, caused by the immoderate performance of tyrosinase, is a major abnormality of human skin. Downregulation of tyrosinase enzyme through tyrosinase inhibitors has emerged as an effective strategy for hyperpigmentation therapy. In this study, a newly synthesized tyrosinase inhibitor (MHY908) was loaded into a nanostructured lipid carrier (MHY908/NLC) for the topical treatment of hyperpigmentation. MHY908/NLCs were prepared by a reverse instilling technique of melt and ultrasonication. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and transmission electron microscopy (TEM) analyses showed that MHY908 was highly dispersed and encapsulated in NLC in an amorphous state. MHY908/NLCs exhibited a dual drug release kinetic (initial burst release followed by prolonged drug release), higher skin permeation, and significant occlusion effect (in vitro and ex vivo) than MHY908 solution. The anti-melanogenesis activity of MHY908/NLCs in a mouse model of UVB-induced hyperpigmentation was significantly higher than that of MHY908 solution. Furthermore, the in vitro cytotoxicity test revealed the non-toxicity of MHY908/NLCs to healthy fibroblast cells. Therefore, MHY908/NLC could serve as a promising topical delivery system for the treatment of hyperpigmentation.
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