Background: The anti-plasmin activity of Tranexamic Acid (TA) is considered to be the
main mechanism of hypopigmentation. Several studies have found TA to be effective for both oral
and topical application. When used to lighten stains, TA is effective even at low concentrations,
ideally in the range of 2 to 5%. Increasing the duration of treatment is more effective than increasing
the concentration of TA: Higher concentrations of TA (> 5%) do not improve the effect but
rather cause irritation. The TA formulations were applied once or twice a day, and the average duration
was eight to twelve weeks: advantageous therapeutic effects were observed after this period.
Other studies gave intradermal injections once weekly for 12 weeks, also with an acceptable efficiency.
The compound may be administered topically to the skin in the form of emulsions, creams
and solutions, and formulations containing liposomes. Encapsulation of TA in liposomes may reduce
potential skin irritation, and it ensure high formulation stability, decrease the risk of leakage
and allow long-term sustained release. Intradermal injections of TA produce relatively quick
bleaching results without significant side effects.
Conclusion: In conclusion it should be stated that the lightening effect of tranexamic acid in topical
and intradermal applications has been most extensively studied in the case of melasma, and most
studies have been performed in Asia. Therefore, the final evaluation of TA, in the cases other than
melasma and hyperpigmentation, requires further studies. However, further studies are needed in
order to optimize the frequency of application of TA and to determine the long-term benefits from
its use, especially concerning stains other than chloasma.