Neftis Laboratorios opts for tranexamic acid as an innovative treatment to combat melasma

Melasma is a skin pigmentation disorder. It is characterized by excessive production of melanin in a localized and chronic way. It has a significant impact on appearance, causes psychosocial and emotional distress and, in general, reduces the quality of life of affected patients.

Young women are mainly those who suffer from melasma, although it can also appear in men. Melasma appears on the face, especially on the cheeks, the bridge of the nose, the forehead and the upper lip. On certain occasions, the spots can also be found on forearms and neckline.

What are the causes of melasma?

There is no clear evidence about the causes of melasma. One of the possible factors of this dysfunction is sun exposure, because ultraviolet rays affect the cells that control the pigment (melanocytes). Therefore, one way to prevent melasma is, without doubt, sun protection that prevents the formation of pigmented spots caused by the sun.

Other possible factors that favour the development of melasma are hormonal alterations, genetic susceptibility, cosmetics that cause an irritative or allergic process and phototoxic medicines.

Traditional treatments

Up to now, treatments to combat melasma are mainly based on prevention, i.e. avoiding the direct incidence of the sun or light systems on the skin and using sun filters (higher than a FP 50) throughout the year. The R&D team at Neftis Laboratorios has developed the perfect DNA Sun line to protect the skin effectively against UVA and UVB rays (SPF 30 and SPF 50+) with a pleasant texture that allows its application in both dispenser and airless.

Within the group of traditional treatments, we also find the specific treatments, which aim to whiten or eliminate the lesions. Specifically, there are two types of specific treatments: pharmacological and physical therapy. Drug treatments inhibit the formation of melanin by various mechanisms.

For best results, treatment based on oral drugs should be combined with topical treatments. These treatments include mesotherapy and/or treatment with chemical peels. The most common active ingredients are hydroquinone, kojic acid or arbutin, which inhibit the formation of melanin or alpha-hydroxy acids, niacinamide or salicylic acid which exfoliate the skin and remove melanin from the more superficial layers of the epidermis.

Physical therapy based on all kinds of lasers is the last possible treatment to combat melasma in the traditional way. This therapy should always be combined with the above mentioned treatments in order to obtain good results.

Innovative tranexamic acid treatment

Despite traditional treatments, any dermatologist knows that there is no perfect treatment for melasma. Stains can be improved, but they are difficult to remove completely, and they have a high tendency to reappear. This is why we are looking for new solutions and discovering a new use for tranexamic acid.

Tranexamic acid is an active ingredient so far used orally for the treatment or prevention of bleeding. At present, it has been considered as a novel treatment for melasma.

Its effectiveness could be explained by having a molecular structure very similar to tyrosine, so that tranexamic acid could inhibit or block the activity of the tyrosinase enzyme thus blocking melanin production. It has also been corroborated that tranexamic acid has the ability to inhibit the synthesis of plasminogen and prevent the subsequent formation of plasmin present in the epidermis of the skin, protease with the ability to increase melanin synthesis from alpha-melano-stimulant hormone and the release of arachidonic acid. Ultraviolet radiation is known to induce plasminogen synthesis.

Recent studies support the effectiveness of topical use of 2-5% tranexamic acid. A significant improvement in the appearance of hyperpigmentation, melasma, skin texture and homogeneity of skin tone was observed from week 2 onwards. At 12 months of treatment a significant decrease in melanin index, as measured by Mexameter®, was demonstrated compared to pre-treatment control. Other studies show a slight improvement in results by adding 1% kojic acid and/or 5% niacinamide to the treatment.

Although generally considered an effective and safe treatment, as a precaution, tranexamic acid treatment is not recommended for people with a history of arterial or venous thrombosis, pregnancy or breastfeeding.

The bet of Neftis Laboratorios

Our innovative proposal to combat melasma is a cocktail and a cream with 5% of tranexamic acid. Specifically, both the cream and the cocktail have been formulated for the treatment of hyperpigmentation caused by melasma. 5% tranexamic acid is able to inhibit hyperpigmentation by interfering with the enzymatic pathway.

Esperança Figuerola Head of R&D Neftis Laboratorios