Melasma is a condition that results in excessive pigmentation and vascularization, often concerning women of the ages between 20 and 40. Although the cause of melasma is not known, it often appears on the face, forearms and back in sun-exposed areas. Family history, UV exposure, medications and increased estrogen/progesterone are some of the risk factors associated with melasma. While hydroquinone is a common treatment, it is not always effective and tranexamic acid (TXA), a plasmin inhibitor, is used off-label to treat melasma. TXA can be delivered orally, topically or through injections.

The present article examined the various delivery methods of TXA for melasma treatment and compared their efficacy to traditional treatments.

It analyzed 46 articles obtained through a comprehensive PubMed and Embase search conducted in May 2022.

The study found:

• Oral, intralesional and topical TXA as safe and effective treatments for melasma, based on various randomized controlled trials. 
• Regardless of the delivery method, TXA improved the Melasma Area and Severity Index (MASI) scores in patients with melasma.

This study discovered oral TXA to be the most effective, particularly in cases of refractory melasma. However, it provoked gastrointestinal upset and menstrual irregularities in many individuals. Before prescribing oral TXA, it is important to consider the drugs pro-thrombotic nature. Intralesional injections and microneedling with topical TXA are effective alternatives to oral treatment. 

Further, the study found that although topical TXA alone was the least effective approach, combining it with other cosmeceuticals can improve outcomes. Again, topical TXA shows better tolerance than hydroquinone, a traditional topical melasma treatment.

Source: Konisky H, Balazic E, Jaller JA, Khanna U, Kobets K. Tranexamic acid in melasma: a focused review on drug administration routes. J Cosmet Dermatol. 2023;22(4):1197-206.