New Topical Tranexamic Acid Derivative for the Improvement of Hyperpigmentation and Inflammation in the Sun-Damaged Skin

Ivan D. da Silva Souza / PhD

Daniel Winn / PhD

Lorraine Lampe / Bachelor of Chemistry Student


Background: Skin-lightening products are used worldwide to treat persistent pigmentation disorders that impact our quality of life and self-confidence. However, consumers of cosmetic and over-the-counter skin lighteners struggle to find products that perform to their expectations. New, safe, and effective bioactives are needed to fill this gap.

Objective: To investigate the safety and skin-lightening performance of a new topical tranexamic acid derivative, that is, cetyl tranexamate mesylate.

Methods: The test material was a facial serum containing 2.0% (w/w) of the new bioactive. Safety was evaluated by a modified Human Repeat Insult Patch Test with 54 subjects of either sex. Performance was objectively assessed based on the improvement of melanin and erythema indexes through time, and also subjectively by photographs and self-perception questionnaires. Thirty-five female subjects applied the serum twice a day for 8 weeks.

Results: No questionable adverse reactions were observed. Melanin and erythema indexes improved significantly and continuously from the baseline to the end of the study (-16.9% and -34.3%, respectively). Photographs further support instrumental data. On average, after 2 weeks, the subjects already noticed an improvement in skin tone (79.3%), a reduction in dark spots (78.6%), and an improvement in facial redness (77.1%).

Conclusion: A topical serum containing cetyl tranexamate mesylate was well-tolerated and successfully improved the overall facial skin tone, as well as the appearance of dark spots and redness.

Keywords: aging skin; dark spots; facial redness; photodamage; tranexamic acid.


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