Allergic contact dermatitis caused by phenylethyl resorcinol [4‐(1‐phenylethyl)‐1,3‐benzenediol], a skin‐lightening agent in cosmetics

Gohara, Michi; Yagami, Akiko; Suzuki, Kayoko; Morita, Yusuke; Sano, Akiyo; Iwata, Y.; Hashimoto, Takashi; Matsunaga, Kayoko

doi:10.1111/cod.12114

Cited by 16 publications

(9 citation statements)

References 5 publications

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“…This confirmed that sink conditions would be maintained over the course of the permeation study. A concentration of 1% of PR in DMI, PG or glycerol was selected as this within the range of the concentration found in the marketed products . The stability of PR in DMI, PG and glycerol was also evaluated at 32 ± 1 °C.…”

Section: Resultsmentioning

confidence: 99%

Characterization and topical delivery of phenylethyl resorcinol

Zhang¹,

Sil

Kung³

et al. 2019

Intern J of Cosmetic Sci

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Objective Phenylethyl resorcinol (PR) has been used widely in the personal care industry as a novel skin lightening ingredient. Surprisingly, there is only limited information describing the physicochemical properties of this active. Therefore, the primary objective of this study was to perform a comprehensive characterization of PR. A secondary objective was to investigate the delivery of this molecule to mammalian skin. Methods Phenylethyl resorcinol was characterized using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and nuclear magnetic resonance (NMR). A new high‐performance liquid chromatographic (HPLC) method for analysis of PR was developed and validated. The log P (octanol water partition coefficient), value, solubility and short‐term stability of PR in a series of vehicles were also determined using HPLC. The evaporation of the selected vehicles was examined using dynamic vapour sorption (DVS). The permeation profiles of PR were investigated under finite dose conditions in porcine and human skin. Results The melting point of PR was determined to be 79.13 °C and the measured log P (octanol water partition coefficient) at 21 °C was 3.35 ± 0.03. The linearity of the HPLC analytical method was confirmed with an r2 value of 0.99. Accuracy of the method was evaluated by average recovery rates at three tested concentrations, and the values ranged from 99 to 106%. The limit of detection (LOD) and limit of quantification (LOQ) were 0.19 and 0.57 μg mL−1, respectively. The solubility of PR in PG, DMI, glycerol was within the range of 367 to 877 mg mL−1. The stability of PR in tested solvents was also confirmed by the 72 h stability studies. From the DVS studies, 70–125% of applied formulations were recovered at 24 h. The permeation through porcine skin at 24 h ranged from 4 to 13 μg cm−2, while the corresponding amounts of PR delivered through human skin were 2 to 10 μg cm−2. Conclusion The physicochemical properties of PR confirm it is suitable for dermal delivery. In this study, propylene glycol was the most promising vehicle for PR delivery to human skin. Future work will expand the range of vehicles studied and explore the percutaneous absorption from more complex formulations.

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Section: Resultsmentioning

confidence: 99%

Characterization and topical delivery of phenylethyl resorcinol

Zhang¹,

Sil

Kung³

et al. 2019

Intern J of Cosmetic Sci

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“…However, the formulation of PR for topical application is difficult because of the poor aqueous solubility of the compound and its low stability when exposed to light [ 4 ], which results in a color change from white to pink tones. In addition, concentrations of PR in the formulation in excess of 1% can cause skin irritation which may lead to consumer rejection of the product [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Ethosomes of Phenylethyl Resorcinol as Vesicular Delivery System for Skin Lightening Applications

Limsuwan

Boonme

Khongkow

et al. 2017

BioMed Research International

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Ethosome formulations containing phenylethyl resorcinol (PR) were developed. The formulation was produced from 0.5% w/v PR, 0.5% w/v cholesterol from lanolin, 3% w/v L-α-phosphatidylcholine from soybean, 30% v/v absolute ethanol, and water up to 100% v/v. It was characterized by a vesicular size of 389 nm, low polydispersity index of 0.266, zeta potential of −34.19 ± 0.44 mV, high PR entrapment efficiency of 71%, and good stability on storage at 4 and 30°C at 75% RH for 4 months. In vitro studies using pig skin revealed that permeation coefficient of PR from ethosomes was significantly higher than that from liposomes. In vitro retention profiles showed that PR accumulation in pig skin following application of ethosome formulations was 7.4-, 3.3-, and 1.8-fold higher than that achieved using liposomes, 20% propylene glycol solution, and 30% hydroethanolic solution, respectively. An inhibition value of around 80% was measured for antityrosinase activity of PR in pig skin. Consistently, ethosomes exhibited higher tyrosinase inhibition activity and melanin content reduction when compared to other formulations in B16 melanoma cells. Ethosomes did not cause acute dermal irritation in albino rabbits. These findings demonstrate that ethosomes are capable of delivering PR into the skin efficiently and hold promise for topical application of skin lightening products.

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“…Sensitization from phenylethyl resorcinol contained in a skin‐lightening essence involving a Japanese woman was first reported in 2013 . To the best of our knowledge, no other cases have been published thus far.…”

Section: Discussionmentioning

confidence: 97%

“…Nineteen cases of contact dermatitis caused by depigmenting agents in cosmetics have been published in 14 reports, all involving middle-aged women (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14). The incriminated bleaching molecules were quite diverse.…”

Section: Discussionmentioning

confidence: 99%