What is the current clinical data on the use of topical tranexamic acid (TXA) and niacinamide for treating hyperpigmentation?

From the Guidelines

Topical tranexamic acid (TXA) and niacinamide are effective treatments for hyperpigmentation, with growing clinical evidence supporting their use, particularly when used in conjunction with other therapies like platelet-rich plasma (PRP) for enhanced results. The current clinical data on the use of topical TXA and niacinamide for treating hyperpigmentation suggests that these agents can significantly reduce the appearance of melasma and post-inflammatory hyperpigmentation 1. Topical TXA at concentrations of 2-5% has shown efficacy in treating melasma and post-inflammatory hyperpigmentation when applied twice daily for 8-12 weeks, by inhibiting plasmin activity, which reduces melanocyte tyrosinase activity and melanin production. Niacinamide (vitamin B3) is typically used at 2-5% concentration and shows benefits after 4-8 weeks of twice-daily application, functioning by inhibiting melanosome transfer to keratinocytes and having anti-inflammatory properties. Some studies suggest that PRP may be more effective than TXA in treating melasma, with a significant reduction in mMASI score from pre-treatment to post-treatment observed in all studies 1. The combination of TXA and PRP may yield better results than using either treatment alone, as PRP can boost the therapeutic effect of TXA cream 1. Patients should be advised that visible improvements typically take at least 4 weeks, and consistent sun protection is crucial for preventing hyperpigmentation recurrence. The safety profiles of both TXA and niacinamide are favorable, with minimal side effects, mainly mild irritation or dryness. For optimal results, these agents can be combined with other treatments like sunscreen (essential), retinoids, or alpha hydroxy acids. Overall, the current clinical data supports the use of topical TXA and niacinamide, potentially in combination with PRP, as effective treatments for hyperpigmentation, with significant improvements in patient satisfaction and quality of life.

From the Research

Summary of Clinical Data

The current clinical data on the use of topical tranexamic acid (TXA) and niacinamide for treating hyperpigmentation is promising, with several studies demonstrating their effectiveness in reducing the appearance of hyperpigmentation.

• A 2019 study published in the Journal of Drugs in Dermatology found that a topical serum containing 3% TXA, 1% kojic acid, and 5% niacinamide significantly improved the appearance of post-inflammatory hyperpigmentation (PIH), hyperpigmentation, and melasma in Brazilian female subjects with Fitzpatrick skin types I-IV 2.
• A 2014 study published in Skin Research and Technology found that a combination of topical niacinamide and TXA reduced the appearance of irregular facial pigmentation in Korean women 3.
• While there are studies on the use of oral TXA for hyperpigmentation, the focus here is on topical application, and thus, studies like the 2023 review on oral TXA are less directly relevant but indicate the broader potential of TXA in treating hyperpigmentation disorders 4.
• The efficacy of TXA, both orally and topically, suggests it could be a valuable treatment option for various hyperpigmentation conditions, including melasma, as supported by a 2018 review in Dermatologic Surgery 5.
• Niacinamide has been shown to be effective in reducing hyperpigmentation when combined with other agents, such as N-acetyl glucosamine, as demonstrated in a 2010 study published in the British Journal of Dermatology, though this study did not involve TXA 6.

Key Findings

• Topical TXA and niacinamide combinations have been shown to be effective and well-tolerated for treating hyperpigmentation, including melasma and PIH 2, 3.
• The mechanism of action of TXA involves inhibiting the release of inflammatory mediators that trigger melanogenesis, making it a potent agent against hyperpigmentation 2.
• Clinical evaluations and bio-instrumental measurements have supported the efficacy of these treatments, with significant improvements observed in the appearance of hyperpigmentation and skin tone homogeneity 2, 3.
• Further research is needed to fully understand the potential of topical TXA and niacinamide for hyperpigmentation, especially in diverse skin types and conditions.
• The existing evidence suggests that topical formulations containing TXA and niacinamide could offer a valuable treatment option for individuals seeking to reduce hyperpigmentation, potentially providing an effect beyond that achieved with traditional treatments like sunscreen.