Topical Formulations and Intradermal Injections of Tranexamic Acid in the Treatment of Hyperpigmentation - A Review

Abstract

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.

The influence of topical5%tranexamic acid at pH2.38with and without corundum microdermabrasion on pigmentation and skin surface lipids

“…Tranexamic acid (TA, trans-4-aminomethylcyclohexanecarboxylic acid) is a synthetic amino acid which demonstrates anti-hemorrhagic activity and is used to treat bleeding in various origins (Acidum tranexamicum, medicine EXACYL). [1][2][3][4][5] However, during the course of treatment using oral TA, it was observed that administration also yielded whitening effects. 1,3,[6][7][8][9][10][11][12][13][14] Studies have shown that both oral administration and topical application of TA is effective at decreasing pigmentation.…”

“…[1][2][3][4][5] However, during the course of treatment using oral TA, it was observed that administration also yielded whitening effects. 1,3,[6][7][8][9][10][11][12][13][14] Studies have shown that both oral administration and topical application of TA is effective at decreasing pigmentation. 3,[15][16][17][18][19][20][21] In addition, the European Cosmetics Directive safety report does not indicate any health risks related to the superficial use of tranexamic acid for cosmetic purposes 1,3 ; however, topical application should be safer, due to the lack of systemic absorption.…”

“…1,3,[6][7][8][9][10][11][12][13][14] Studies have shown that both oral administration and topical application of TA is effective at decreasing pigmentation. 3,[15][16][17][18][19][20][21] In addition, the European Cosmetics Directive safety report does not indicate any health risks related to the superficial use of tranexamic acid for cosmetic purposes 1,3 ; however, topical application should be safer, due to the lack of systemic absorption. 22,23 The most preferred concentration is in the range of 2% to 5% as preparations containing only tranexamic acid at low concentrations ≤5% offer effective decreases of hyperpigmentation; higher concentrations of 5% to -10% may cause irritation and do not demonstrate an increased effect.…”

“…Alternatively, it is possible to increase effectiveness by increasing the time of application and duration of the course of treatment. 1,9,20,24 Studies indicate that beneficial therapeutic effects can be obtained from TA preparations by administration once or twice daily, with the mean time of application being 8 to 12 weeks. 3,7,9,14,22, [25][26][27] In addition to its whitening effect, TA also reduces redness by influencing the superficial blood vessels in the area.…”

“…3,7,9,14,22, [25][26][27] In addition to its whitening effect, TA also reduces redness by influencing the superficial blood vessels in the area. 1,3 Studies also indicate that topical application of TA further improves the permeability of the epidermal barrier in acne rosacea, reduces the appearance of wrinkles caused by dryness of the skin and accelerates skin regeneration after physicochemical damage. [28][29][30][31] Liposomal formulations of TA can be combined with fruit acid peelings, microdermabrasion, IPL and laser (Nd-YAG) treatments.…”