Efficacy and tolerability of a depigmenting gel serum comprising tranexamic acid, niacinamide, 4‐butylresorcinol, phytic acid, and a mixture of hydroxy acids that targets the biological processes regulating skin melanogenesis

Abstract Background The diverse causes of hyperpigmentation and complex nature of melanogenesis make it a challenge to manage. Current approaches either fail to deliver effective pigmentation control or have undesirable safety profiles that preclude their long‐term use. Aims To evaluate the capacity of a cosmetic gel serum comprising tranexamic acid, niacinamide, 4‐butylresorcinol, phytic acid, and a mixture of hydroxy acids that was designed to target the biological processes regulating skin melanogenesis to attenuate melanin production in vitro and reduce hyperpigmentation clinically. Methods Capacity to reduce melanin production in vitro was determined in melanocyte‐containing reconstructed human epidermis (RHEm). Clinical efficacy and skin tolerability following twice daily application were assessed in 35 subjects with slight to moderate facial hyperpigmentation by instrumental (VISIA®‐CR, Mexameter®) and clinical (mMASI, clinical score, IGA for hyperpigmentation) evaluation on D14, D28, D56, and D84. Maintenance of pigmentation control was followed up 1 month after cessation of treatment on D112. Results In RHEm in vitro, melanin production was reduced by 50.0% from baseline (D0) on D14 ( p < 0.001) and by 67.0% on D21 ( p < 0.001). Clinical reductions from baseline in brown spots count (−9.0%; p < 0.05), brown spots area (−16.7%; p < 0.001), and the melanin index (−11.4%; p < 0.001) were observed within 14 days of use. Statistically significant improvements in all clinical parameters were achieved by D28. By the end of treatment on D84, the number and surface area of brown spots were reduced by 28.4% and 40.3% compared to D0, respectively ( p < 0.001, both), the melanin index was reduced by 31.1% ( p < 0.001), mMASI was reduced by 63.0% ( p < 0.001), and skin luminosity was increased by 79.0% ( p < 0.001). IGA was reduced from 2.3 on D0 to 1.3 on D84 ( p < 0.001). Improvements to all these parameters were maintained until D112, 1 month after termination of treatment. The product also demonstrated very good skin tolerability. Conclusion A gel serum comprising tranexamic acid, niacinamide, 4‐butylresorcinol, and hydroxy acids, designed to target the biological processes regulating skin melanogenesis, demonstrates rapid, robust, and sustained pigmentation control in this cohort.