Effect of a Tranexamic Acid, Kojic Acid, and Niacinamide Containing Serum on Facial Dyschromia: A Clinical Evaluation

May 2019 | Volume 18 | Issue 5 | Original Article | 454 | Copyright © 2019

Seemal Desai MD,a,b Eloisa Ayres MD,c Hana Bak MD,d,e Megan Manco MS,f Stephen Lynch PhD,g Susana Raab MS,g Ana Du BS,g DesTenee Green BS,g Cezary Skobowiat PhD,g Janet Wangari-Talbot PhD,g Qian Zheng MD PhDg

aUniversity of Texas Southwestern Medical Center, Dallas, TX bInnovative Dermatology, Plano, TX cEZSkin Dermatologia, Niterói, Rio de Janeiro, Brazil dCheongdam-Hana Dermatology, Seoul, Korea eYonsei University Wonju College of Medicine, Wonju, Korea fSkinceuticals, New York, NY gL’Oréal Research and Innovation, Clark, NJ


Background: Stubborn dyschromia such as melasma and post-inflammatory hyperpigmentation (PIH) are leading causes for cosmetic consultation. Topical treatment is challenging, using a range of modalities, to stop, hinder, and/or prevent steps in the pigment production process. Tranexamic acid (TXA), a potent plasmin inhibitor, is proposed to control pigmentation by inhibiting the release of inflammatory mediators involved in triggering melanogenesis. TXA has been recently introduced as a topical therapy aimed at reducing pigmentation in melasma. Methods: In a 12-week clinical study, a novel, topical facial serum containing 3% TXA, 1% kojic acid, and 5% niacinamide was evaluated for its effectiveness in treating melasma, PIH, and hyperpigmentation in Brazilian female subjects with Fitzpatrick skin types I-IV. Efficacy evaluations were performed at pre-treatment baseline, weeks 2, 4, 8, and 12, and included expert clinical grading, bio-instrumental measurements, and self-assessment questionnaires. Cutaneous tolerability was also evaluated by assessing subjective and objective irritation of the treatment area. Results: A significant improvement in the appearance of PIH, hyperpigmentation, melasma, skin texture, and skin tone homogeneity was observed beginning at week 2 and continued through week 12. Melanin index, as measured by Mexameter®, demonstrated a significant decrease by week 12 as compared to both pre-treatment baseline and control. Conclusions: The findings suggest that the test product is an effective and well-tolerated treatment option for addressing hyperpigmentary conditions, including melasma. Additional in vitro data suggests that TXA may act by mediating the inhibition of PGE2-stimulated human epidermal melanocytes.

J Drugs Dermatol. 2019;18(5):454-459.

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The etiology of skin dyschromia remains complex and its treatment remains challenging, particularly for melasma. Melasma is a common, persistent disorder of hyperpigmentation affecting a significant portion of the population, particularly women living in areas with intense ultraviolet radiation.1,2 It is characterized by symmetric hyperpigmented macules or patches with irregular borders, most often distributed on the forehead, cheeks, and along the jawline.3,4 The causes of melasma remain unknown, although some triggering factors are described, such as sun exposure, pregnancy, use of oral contraceptives and steroids, hepatopathies, use of photosensitizing drugs, inflammatory processes of the skin, and stressful events.5 Melasma, hyperpigmentation, and post-inflammatory hyperpigmentation (PIH), are prevalent in all Fitzpatrick skin types, especially in those with darker skin tones.6 These dermatologic conditions are a leading cause for cosmetic consultation, and account for the high demand for effective skin lightening therapies.7 Studies have shown that hyperpigmentation, particularly melasma, greatly affects quality of life, causing psychosocial distress.8 Treatments for melasma include topical depigmenting agents, such as hydroquinone (HQ (2-4%)), tretinoin, azelaic acid, superficial peeling agents, and lasers. Results with these treatments are often temporary, as the discoloration generally returns with continued exposure to the sun.9Kojic acid and niacinamide, two well-known skin lightening agents, either alone or in combination with other actives, have been demonstrated to be effective in reducing the hyperpigmentation, including melasma.10-14 Tranexamic acid (trans-4-aminomethylcyclohexanecarboxylic acid: TXA) is a

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