Comparative studies on the photoreactivity, efficacy, and safety of depigmenting agents

Mota, S., Rosa, G.P., Barreto, M.C., Garrido, J., Sousa, E., Cruz, M.T., Almeida, I.F. & Quintas, C. (2024) Comparative studies on the photoreactivity, efficacy, and safety of depigmenting agents.

Pharmaceuticals, 17(1), 55. DOI:10.3390/ph17010055 (IF2022 4,6; Q2 Chemistry, Medicinal)
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  • Jan, 2024


Depigmenting products are increasingly used to counteract skin hyperpigmentation and related psychosocial issues. This study aimed to compare different depigmenting agents—4-butylresorcinol; bakuchiol; tranexamic acid; ascorbyl glucoside; α-arbutin; and ascorbic acid—for photoreactivity; tyrosinase inhibition; and safety. Photoreactivity was assessed using the Reactive Oxygen Species assay. In vitro tyrosinase inhibition was compared, and cell viability was assessed in B-16V melanocytes to evaluate safety. Results showed 4-butylresorcinol, ascorbyl glucoside, and α-arbutin are non-photoreactive, while for ascorbic acid and bakuchiol it was not possible to reach conclusive results due to the lack of specificity of the ROS assay. 4-Butylresorcinol, acting as a competitive inhibitor, displayed potent tyrosinase inhibition, followed by ascorbic acid and bakuchiol. Both 4-butylresorcinol and bakuchiol reduced cell viability in a concentration-dependent manner. The insights obtained in this work support the development of depigmenting products by providing useful scientific guidance on the photostability, tyrosinase inhibitory efficacy, and skin safety of depigmenting agents.