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Cosmetics 2017, 4(3), 31; doi:10.3390/cosmetics4030031

In Vitro Methods for Predicting Chemical Leukoderma Caused by Quasi-Drug Cosmetics

Bionics Program, Tokyo University of Technology Graduate School, 1404-1 Katakuramachi, Hachioji City, Tokyo 192-0982, Japan
School of Bioscience and Biotechnology, Tokyo University of Technology, 1404-1 Katakuramachi, Hachioji City, Tokyo 192-0982, Japan
Author to whom correspondence should be addressed.
Received: 27 July 2017 / Revised: 29 August 2017 / Accepted: 30 August 2017 / Published: 2 September 2017
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Skin care cosmetics frequently contain whitening or lightening agents. The present study aimed to establish in vitro methods for predicting chemical leukoderma caused by whitening agents in cosmetics. The risks of chemical leukoderma were predicted based on percutaneous absorption rates, toxic concentrations, and toxicity mechanisms. Thus, in vitro skin permeation rate and cytotoxic concentrations of whitening agents were studied using excised skin and cultured B16 melanoma cells. Pigment cell toxicity was observed using transmission electron microscopy (TEM). The levels of hydroxyl radical (∙OH) were measured and the location of ∙OH generation sites were determined in cultured B16 melanoma cells. Pigment cells cultured under conditions with high tyrosinase activity developed cytotoxicity when exposed to compounds known to cause leukoderma, while those cultured under conditions with low tyrosinase activity did not. Phenolic compounds that cause leukoderma were applied to the pigment cells at the concentration absorbed percutaneously under conditions with high tyrosinase activity. Cells that were observed using TEM demonstrated a large number of vacuolar degenerations in intracellular melanosomes after treatment with phenolic compounds that are known to cause leukoderma. Hydroxyl radical generation during the tyrosinase reaction was examined, as the whitening agents that inhibit tyrosinase activity serve as tyrosinase substrates. Only phenolic compounds that cause leukoderma generated high amounts of hydroxyl radicals. Thus, the hydroxyl radical is a melanocyte-specific toxin that disrupts tyrosinase-containing melanosomes. Whitening agents that generate high amounts of hydroxyl radicals may cause leukoderma. The in vitro method being reported here can predict the potential of a drug to cause leukoderma and whether the use of a specific whitening agent poses a risk. View Full-Text
Keywords: quasi-drug cosmetics; chemical leukoderma; melanocytes; hydroxyl radical quasi-drug cosmetics; chemical leukoderma; melanocytes; hydroxyl radical

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Gu, L.; Zeng, H.; Takahashi, T.; Maeda, K. In Vitro Methods for Predicting Chemical Leukoderma Caused by Quasi-Drug Cosmetics. Cosmetics 2017, 4, 31.

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