Tranexamic acid: with which active ingredients should it be combined?

The peptides make up a broad family of short chains of amino acids, whose effects vary according to their structure and biological function. In cosmetics, notably signal peptides stimulate the synthesis of collagen and elastin, inhibitory neurotransmitter peptides used to smooth the appearance of expression lines, or transporter peptides capable of delivering essential trace elements to skin metabolism. Their growing popularity is due to their good tolerability, versatility and ability to act on various markers of skin ageing, from loss of firmness to lack of radiance.

Combining peptides with tranexamic acid holds promise for enhancing skin tone uniformity and overall skin quality.

Depending on the peptide used, the combination can thus contribute to strengthening the barrier function, smoothing out wrinkles or improving skin radiance, whereas the tranexamic acid acts more specifically on the mechanisms involved in hyperpigmentation. For example, at Typology, we decided to combine tranexamic acid with tetrapeptide-2 in our wrinkle and loss-of-firmness serum. This combination not only fades brown spots but also mitigates the signs of skin ageing.

The arbutin acid, and more specifically alpha-arbutin, is an active ingredient recognised for its targeted action against hyperpigmentation. A natural derivative of hydroquinone, it primarily acts by inhibiting the activity of tyrosinase, a key enzyme in melanogenesis, which helps to limit excessive melanin production. Valued for its progressive efficacy and good tolerability, the arbutin acid is frequently used to reduce pigment spots, melasma and other skin tone irregularities, including in sensitive skin.

In this context, it may be appropriate to combine alpha-arbutin with tranexamic acid to target different mechanisms involved in hyperpigmentation.

A clinical trial conducted in Indonesia on 66 women with melasma evaluated a formulation combining 3% tranexamic acid, 2% arbutin, 4% niacinamide and 2% ferment of Galactomyces, recognised for its soothing properties. Participants applied a serum and then a cream containing these actives for four weeks. Melasma progression was monitored using a clinical severity score (MSS) as well as image analysis tools to assess epidermal and dermal pigmentation. The results showed a overall improvement in hyperpigmentation, objectively measurable from the second week of use, suggesting a clinical interest in this combination of actives.

It should nevertheless be noted that the study examined a multi-active formulation, which did not consist solely of tranexamic acid and alpha-arbutin.

The hydroquinone has long been the reference molecule in the management of hyperpigmentation. Its mechanism relies on potent inhibition of tyrosinase and, at higher doses or with prolonged use, on a direct cytotoxic action against melanocytes. This pronounced efficacy is, however, accompanied by numerous controversies: risks of irritation, contact dermatitis, post-inflammatory hyperpigmentation... These adverse effects have led to strict regulation of hydroquinone, and even its ban in cosmetic products in several countries, restricting its use to medical settings under dermatological supervision.

Some data suggest that combining hydroquinone with tranexamic acid can act at different levels on pigmented spots.

Nevertheless, in practice, this combination is most often administered as tranexamic acid orally, in conjunction with topical hydroquinone, although some reports also describe the topical use of tranexamic acid. These regimens are generally reserved for severe or resistant forms of melasma and constitute part of a strictly medical management.

The vitamin C, or ascorbic acid, is a flagship cosmetic active for its antioxidant properties and its role in regulating pigmentation. It neutralises the free radicals notably induced by UV rays and pollution, limits the oxidation of already formed melanin and indirectly contributes to tyrosinase inhibition. In parallel, it supports collagen synthesis, making it a highly versatile active.

In this context, combining vitamin C with tranexamic acid may be appropriate.

This complementarity was explored in a clinical study conducted in female patients presenting with treatment-resistant melasma. The study enrolled ten women who were followed for eight weeks. Each evening, participants applied a topical formulation containing 2% tranexamic acid and 2% vitamin C. Efficacy was assessed using the MASI score and the MelasQoL questionnaire, designed to evaluate the condition’s impact on quality of life. The results demonstrated a progressive and significant decrease in the MASI score over the weeks, accompanied by an improvement in quality of life reported by the patients. Notably, no adverse reactions were observed during the study, suggesting good tolerability of this combination.

The kojic acid is an active ingredient that has long been extensively used to target hyperpigmentation. Of fungal origin, it primarily acts by chelating the copper ions required for tyrosinase activity, thereby slowing melanin production. Despite this well-documented efficacy, its cosmetic use remains controversial. Kojic acid is indeed suspected of being irritating and sensitising, with a non-negligible allergenic potential. Questions have also arisen regarding a possible endocrine-disrupting effect as well as signals of carcinogenicity or mutagenicity observed in certain experimental models, leading to strict regulation of its permitted concentrations.

Nevertheless, kojic acid continues to be combined with other depigmenting agents, such as tranexamic acid, in order to enhance its overall efficacy against pigmented spots.

This combination was specifically evaluated in a 12-week clinical study involving 55 women with melasma. The tested serum contained 3% tranexamic acid, 1% kojic acid and 5% niacinamide, and was applied daily. Efficacy was monitored using a mexameter, a device that quantifies the melanin index. The results demonstrated a significant improvement in the appearance of brown spots.

In accordance with the precautionary principle, at Typology we have excluded kojic acid from our formulations.

The azelaic acid is a naturally derived active ingredient that possesses anti-inflammatory, antibacterial and depigmenting properties. Versatile, it is found in various types of skincare products, for example those designed for people prone to blemishes or rosacea.

The benefit of combining azelaic acid with tranexamic acid was explored in a study conducted on 33 women exhibiting moderate to severe skin hyperpigmentation. Participants applied a cream formulated with these two actives daily for six weeks, although their exact concentrations were not disclosed. Efficacy assessment was based on standardised photographs, clinical dermatological evaluation and software-assisted analysis. At the end of the study, a overall and visible improvement in skin pigmentation was observed, suggesting that the tranexamic acid–azelaic acid combination might be of interest in cases of pigmentary disorders, even though the lack of data on concentrations and the quantified magnitude of the results warrants caution in interpretation.

The glycolic acid is a widely used alpha-hydroxy acid (AHA) in cosmetics and dermatology for its exfoliating action. Thanks to its small molecular size (76.05 g/mol), it easily penetrates the stratum corneum and promotes cellular renewal, which contributes to gradually fading pigmentation spots and attenuating wrinkles.

Some studies have investigated the combination of tranexamic acid and glycolic acid, on the hypothesis of a complementary effect between the inhibition of melanogenesis and the removal of superficial skin cells. However, the results did not show a significant benefit compared with the use of glycolic acid alone. Moreover, in practice, this combination can prove too aggressive for the skin barrier. Thus, despite its theoretical appeal, we therefore do not recommend combining glycolic acid with tranexamic acid within the same skincare routine.

The benzoyl peroxide is a benchmark active ingredient in the management of acne, notably for its antibacterial properties against Cutibacterium acnes. It also works through a mild keratolytic and anti‐inflammatory effect, helping to limit pore obstruction. On the downside, it is a potent ingredient, often associated with marked skin dryness, irritation and a transient alteration of the skin barrier, particularly during the first weeks of use.

Although the idea of combining benzoyl peroxide with tranexamic acid may seem appropriate for simultaneously targeting acne and post-inflammatory hyperpigmentation, as yet there are no studies evaluating this combination.

In practice, it is generally preferable to avoid using benzoyl peroxide and tranexamic acid together. Indeed, benzoyl peroxide is already highly drying and potentially irritating, and it is most often recommended to use it on its own, accompanied only by hydrating, nourishing and soothing actives to preserve skin tolerance. Adding another pigment-targeting agent, such as tranexamic acid, could increase the risk of discomfort without a clearly demonstrated benefit.

Lactic acid belongs to the family of alpha-hydroxy acids (AHAs) and is naturally present in the skin’s natural moisturising factor (NMF). In cosmetics, it is valued for its dual action: gentle exfoliation and moisturisation. By promoting the shedding of corneocytes, it helps improve skin radiance and evenness while supporting skin hydration through its humectant properties. Compared with other AHAs, such as glycolic acid, lactic acid is generally well tolerated, making it an interesting active ingredient for sensitive skin.

To date, no study has demonstrated the existence of synergy between lactic acid and tranexamic acid.

Nevertheless, there is no known contraindication to their combined use. Lactic acid is generally well tolerated and can be incorporated into a regimen containing tranexamic acid, particularly to improve skin texture and radiance while addressing hyperpigmentation.

The salicylic acid is a beta-hydroxy acid (BHA) primarily used for its keratolytic, comedolytic and anti-inflammatory properties. Being lipophilic, it readily penetrates pores, where it facilitates the removal of excess sebum and dead skin cells, making it a benchmark ingredient for treating acne-prone skin. By reducing inflammation and lesion persistence, salicylic acid may indirectly help lower the risk of post-inflammatory hyperpigmentation. It may be assumed that salicylic acid and tranexamic acid could act synergistically to prevent or lessen post-inflammatory hyperpigmentation or brown spots in general.

In the absence of clinical studies on the subject, the potential synergy between salicylic acid and tranexamic acid remains hypothetical.

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