In daily life, when ultraviolet rays penetrate the stratum corneum of human skin to the inner epidermis layer, tyrosinase in melanocytes will be activated, and tyrosinase will hydroxylate tyrosine to generate dopa, and dopa is then oxidized to dopaquinone. When the key substance dopaquinone is formed, a series of complex chemical reactions can be carried out spontaneously to produce melanin [1], which can form pigmentation or cause uneven skin tone.
Tranexamic acid, also known as tranexamic acid, coagulic acid, hemostatic cyclic acid, chemical formula is C8H15NO2, the earliest used to stop bleeding. In the fifties and sixties of the twentieth century, Japan's medical development was not as good as it is now, and the mortality rate of postpartum hemorrhage in women was very high, and a female doctor in Japan, Okamoto Geko, spent more than ten years of research and searching, and found that tranexamic acid has a very good hemostatic effect and has continued to this day.
In fact, tranexamic acid can stop bleeding at the same time, but also has a whitening effect, studies have shown the effect of tranexamic acid whitening and removing freckles (data source: Tokyo, Japan: Bunkodo Press, 2006: 130-138.).
In 1979, during the use of tranexamic acid for the treatment of chronic urticaria, tranexamic acid was first discovered to lighten melasma in patients, and since then people have begun to study the whitening effect of tranexamic acid.
Whitening mechanism
The whitening mechanism of tranexamic acid is roughly divided into two aspects: the front end interferes with melanin production and the back end blocks the transport and diffusion of the generated melanin.
Front
1. Tranexamic acid and tyrosine have similar chemical structures, both have a hydroxyl group, reduce melanin production [2];
2. Tranexamic acid can interfere with the interaction between keratinocytes and melanocytes, reduce ultraviolet-induced melanocyte tyrosinase activity, and prevent melanin production [3];
3. Tranexamic acid can interfere with melanin production by reducing tyrosinase activity [4].
Rear end
As a protease inhibitor, tranexamic acid can inhibit whitening from the posterior end [5,6].
Kanechorn et al. [7] prepared a 5% tranexamic acid liposomal gel, and the efficacy of tranexamic acid liposomal gel in the treatment of melasma was studied in a clinical double-blind randomized controlled trial, and the subjects applied twice a day for 3 months as a course of treatment. The test results show that
Features and security
Compared to general whitening ingredients, tranexamic acid has:
Therefore, in the field of cosmetics, tranexamic acid, as a commonly used whitening agent, has been allowed to be used in cosmetics in many countries, such as Europe, the United States, etc. Mainland China also included tranexamic acid in the scope of permitted use in the Catalogue of Used Cosmetic Raw Materials (2015 Edition) [8].
bibliography
[1] LUO Xiaojun, JIANG Yongmei, ZHANG Wenxian. Melanin production mechanism, related diseases and inhibition strategies[J]. Biology Teaching Vol. 46, No. 2, pp. 5-7, 2021, PKU, 2021.
[2] SU Xin,ZHU Xiaofang. New progress in the treatment of melasma[J].Chinese Journal of Aesthetic Medicine, 2020,29( 2): 167-170.)
[3] WANG Yanbo, ZHANG Zhengzhong. Progress in the treatment of melasma[J]. Chinese Journal of Leprosy and Dermatology,2019,35( 10): 633-636.
[4] Zhu JW，Ni YJ，Tong XY，et al． Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Ｒeceptors［J］．Int J Med Sci，2020，17( 7) : 903－911．
[5] Li Y，Xie H，Deng Z，et al． Tranexamic acid ameliorates rosacea symptoms through regulating immune response and angiogenesis［J］．Int Immunopharmacol，2019，67: 326－334．
[6] Jakhar D，Kaur I，Misri Ｒ． Topical 10% Tranexamic acid for erythematotelangiectatic steriod induced rosacea［J］．J Am Acad Dermatol J，2020． doi: 10．1016 /j．jaad．2019．12．067．
[7] Kanechorn Na Ayuthaya P，Niumphradit N，Manosroi A，et al． Topical 5% tranexamic acid for the treatment of melasma in Asians: a double-blind randomizedcontrolled clinical trial[J] ．J Cosmet Laser Ther，2012，14 ( 3 ) : 150 － 154．
[8] JI Weijia, YI Luyao, YANG Tingting. Determination of Tranexamic Acid in Whitening Cosmetics by HPLC-MS/MS [J]. Drug Evaluation, 2022(001):019.