Effectiveness of Topical Tranexamic Acid in the Treatment of Melasma
Abstract
Melasma is a chronic skin hyperpigmentation condition that often occurs in women of reproductive age, especially in areas exposed to sunlight. One of the therapeutic agents that has attracted attention is tranexamic acid (TXA), which was originally used as an antifibrinolytic agent, but is now known to have an effective mechanism of action in reducing hyperpigmentation. TXA works through plasminogen inhibition, tyrosinase activity, and angiogenesis, as well as providing anti-inflammatory effects. This study uses the PRISMA systematic review method, involving the analysis of 30 relevant articles out of a total of 289 articles identified. The results showed that topical TXA in various formulations, such as creams, gels, or liposomal serums, provided a significant reduction in the Melasma Area and Severity Index (MASI) score. The combination of TXA with other modalities, such as microneedling, laser, and vitamin C, showed more effective results than monotherapy. Topical TXA is an effective and safe therapeutic agent for melasma, especially in the case of refractory or combination therapies. Further research is needed to evaluate the long-term effectiveness and innovation of new formulations in improving the penetration and efficacy of TXA.
References
Abbas, H., Badr, G., Ramadan, G., & Abd-Elhalem, S. S. (2024). Camel Whey Protein and Baicalein Suppressed Mast Cell Degranulation in Mice Models of IgE-and Non-IgE-Mediated Anaphylaxes: Potential Mechanisms on Downstream Cell Signaling of Mast Cells. Immunological Investigations, 53(8), 1330-1347. https://doi.org/10.1080/08820139.2024.2400538
Abdalla, M. A. (2021). Melasma clinical features, diagnosis, epidemiology and etiology: an update review. Siriraj Medical Journal, 73(12), 841-850. https://doi.org/10.33192/Smj.2021.109
Aghdam, S. B., Mohammad, A. P., Hosseini‐Baharanchi, F. S., Atefi, N., Roohaninasab, M., Kahjoogh, H. A., Yazdanian, N., & Goodarzi, A. (2024). Efficacy, safety, tolerability, and treatment durability of microneedling plus topical tranexamic acid in combination with topical modified Kligman lightening formula for melasma: A four‐arm assessor and analyst blinded randomized controlled clinical trial. Journal of Cosmetic Dermatology, 23(11), 3585–3597. https://doi.org/10.1111/jocd.16464
Agrawal, M., Varma, K., Kumar, U., Bhargava, S., Mahadik, A., & Agrawal, V. (2023). Comparison of oral versus topical tranexamic acid for treatment of melasma. International Journal of Clinical and Experimental Dermatology, 30, 28. https://doi.org/10.18231/j.ijced.2023.015
Akhtar, N., Shah, R. R., Waqas, N., Jasti, S., Sharif, S., Shah, A., & Rao, B. (2023). Assessment of the efficacy of tranexamic acid solution 5% in the treatment of melasma in patients of South Asian descent. Cutis, 112(4), 187–191. https://doi.org/10.12788/cutis.0869
Asditya, A., & Sukanto, H. (2017). Studi retrospektif: Profil pasien melasma. Jurnal Dermatologi Indonesia, 29(3). https://doi.org/10.20473/bikk.V29.3.2017.220-228
Bijalwan, S., Randhawa, G. K., & Kaur, T. (2024). A prospective, randomized, and open-label study to compare efficacy, safety, and quality of life impact of topical glutathione (2%) in comparison to topical tranexamic acid (3%) in adult melasma patients. JK Science: Journal of Medical Education & Research, 26(3), 149–154. https://journal.jkscience.org/index.php/JK-Science/article/view/270
da Silva Souza, I. D., Lampe, L., & Winn, D. (2021). New topical tranexamic acid derivative for the improvement of hyperpigmentation and inflammation in the sun‐damaged skin. Journal of Cosmetic Dermatology, 20(2), 561–565. https://doi.org/10.1111/jocd.13545
Dawaud, S. M. K., Hegab, D. S., El Maghraby, G. M., & El-Ashmawy, A. A. (2023). Efficacy and safety of topical tranexamic acid alone or in combination with either fractional carbon dioxide laser or microneedling for the treatment of melasma. Dermatology Practical & Conceptual, 13(3). https://doi.org/10.5826/dpc.1303a195
Debasmita, B., Raj, C., Ishan, A., & Ipsita, D. (2022). A prospective randomized controlled trial of Q‐switched Nd: YAG laser with topical 3% tranexamic acid (TA) versus microneedling with topical 3% tranexamic acid (TA) in treatment of melasma. Journal of Cosmetic Dermatology, 21(7), 2801–2807. https://doi.org/10.1111/jocd.14532
El Attar, Y., Doghaim, N., El Far, N., El Hedody, S., & Hawwam, S. A. (2022). Efficacy and safety of tranexamic acid versus vitamin C after microneedling in treatment of melasma: Clinical and dermoscopic study. Journal of Cosmetic Dermatology, 21(7), 2817–2825. https://doi.org/10.1111/jocd.14538
Gamea, M. M., Kamal, D. A., Donia, A. A., & Hegab, D. S. (2022). Comparative study between topical tranexamic acid alone versus its combination with autologous platelet-rich plasma for treatment of melasma. Journal of Dermatological Treatment, 33(2), 798–804. https://doi.org/10.1080/09546634.2020.1781755
Grimes, P. E., & Alexis, A. F. (2019). Melasma: Epidemiology, pathogenesis, clinical presentation, and diagnosis. UpToDate Waltham, MA: Wolters Kluwer. https://doi.org/10.1007/s13555-017-0194-1
Guo, L., Liu, X., Liu, Q., Xie, X., & Jiang, X. (2024). Treatment of melasma with tranexamic acid essence combined with iontophoresis: A randomized, double-blind, placebo-controlled clinical trial. Drug Design, Development and Therapy, 18, 3659–3666. https://doi.org/10.2147/DDDT.S472922
Guo, Q., Hu, D., Pei, Q., Wang, S., Yan, M., Dong, J., & Yao, M. (2023). Effects of masks containing 0.5% tranexamic acid‐loaded ethosomes on melasma in Asian skin: A randomized controlled clinical trial. Dermatologic Therapy, 2023(1), 1917453. https://doi.org/10.1155/2023/1917453
Irfanti, R. T., Damayanti, W., Dewi, P. F., Oktriana, P., Mulianto, N., & Mawardi, P. (2021). Terapi topikal kombinasi krim asam traneksamat 3%, nikotinamid 3%, dan microneedling pada melasma (Pilot study). Jurnal Kedokteran Indonesia, 48(3).
Janney, M., Subramaniyan, R., Dabas, R., Lal, S., Das, N., & Godara, S. (2019). A randomized controlled study comparing the efficacy of topical 5% tranexamic acid solution versus 3% hydroquinone cream in melasma. Journal of Cutaneous and Aesthetic Surgery, 12(1), 63. https://doi.org/10.4103/JCAS.JCAS_40_18
Kaikati, J., El Bcherawi, N., Abou Khater, J., Dib, S. M., Kechichian, E., & Helou, J. (2023). Combination of topical tranexamic acid and vitamin C for the treatment of refractory melasma. The Journal of Clinical and Aesthetic Dermatology, 16(7), 63. https://pubmed.ncbi.nlm.nih.gov/37560507/
Kaur, A., Bhalla, M., Pal Thami, G., & Sandhu, J. (2020). Clinical efficacy of topical tranexamic acid with microneedling in melasma. Dermatologic Surgery, 46(11), e96–e101. https://doi.org/10.1097/DSS.0000000000002520
Liu, W., Chen, Q., & Xia, Y. (2023). New mechanistic insights of melasma. Clinical, cosmetic and investigational dermatology, 429-442. https://doi.org/10.2147/ccid.s396272
Maeda, K. (2022). Mechanism of action of topical tranexamic acid in the treatment of melasma and sun-induced skin hyperpigmentation. Cosmetics, 9(5), 108. https://doi.org/10.3390/cosmetics9050108
Malik, F., Hanif, M., & Mustafa, G. (2019). Combination of oral tranexamic acid with topical 3% tranexamic acid versus oral tranexamic acid with topical 20% azelaic acid in the treatment of melasma. Journal of the College of Physicians and Surgeons Pakistan, 29(6), 502–504. https://doi.org/10.29271/jcpsp.2019.06.502
Marpaung, H. K., Toruan, T. L., & Kurniawati, Y. (2021). Comparison of the effectiveness of 3% tranexamic acid cream versus 4% hydroquinone cream for treatment of epidermal type melasma. Bioscientia Medicina: Journal of Biomedicine and Translational Research, 5(3), 340-347. https://doi.org/10.32539/bsm.v5i2.221
Mawu, F. O., Kapantow, M. G., Pandaleke, H. E. J., Cahyadi, A. I., Togelang, L., Tampi, J. A., & Christopher, P. M. (2024). Comparative efficacy of topical 10% versus 5% tranexamic acid in treatment of women with melasma: A double-blind randomized controlled trial. Universa Medicina, 43(2), 213–219. https://doi.org/10.18051/UnivMed.2024.v43.213-219
Mushtaq, F., Marwat, R. K., Saleem, M., Khan, A., Khan, S., & Imran, H. (2024). Comparison of efficacy of 5% tranexamic acid vs 20% azelaic acid in patients with melasma. Journal of Health and Rehabilitation Research, 4(1), 591-595. https://doi.org/10.61919/jhrr.v4i1.465
Ostadkarampour, M., & Putnins, E. E. (2021). Monoamine oxidase inhibitors: a review of their anti-inflammatory therapeutic potential and mechanisms of action. Frontiers in pharmacology, 12, 676239. https://doi.org/10.3389/fphar.2021.676239
Patil, S. S., & Deshmukh, A. R. (2019). Comparative study of efficacy of intradermal tranexamic acid versus topical tranexamic acid versus triple combination in melasma. Pigment International, 6(2), 84-95. https://doi.org/10.4103/Pigmentinternational.Pigmentinternational_
Piętowska, Z., Nowicka, D., & Szepietowski, J. C. (2022). Understanding melasma-how can pharmacology and cosmetology procedures and prevention help to achieve optimal treatment results? A narrative review. International Journal of Environmental Research and Public Health, 19(19), 12084. https://doi.org/10.3390/ijerph191912084
Plawinski, L., Cras, A., Hernández Lopez, J. R., de la Peña, A., Van der Heyden, A., Belle, C., ... & Anglés-Cano, E. (2023). Distinguishing plasmin-generating microvesicles: Tiny messengers involved in fibrinolysis and proteolysis. International journal of molecular sciences, 24(2), 1571. https://doi.org/10.3390/ijms24021571
Qu, Y., Wang, F., Liu, J., & Xia, X. (2021). Clinical observation and dermoscopy evaluation of fractional CO₂ laser combined with topical tranexamic acid in melasma treatments. Journal of Cosmetic Dermatology, 20(4), 1110-1116. https://doi.org/10.1111/jocd.13992
Ramzan, F., Malik, K., Bashir, B., Naseer, Z., Shehzad, A., Malik, L., & Rashid, T. (2023). Efficacy of 5% tranexamic acid in melasma. Journal of Pakistan Association of Dermatologists, 33(4), 1257-1262. https://www.jpad.com.pk/index.php/jpad/article/view/2449
Sahu, P., Dayal, S., & Bhardwaj, N. (2021). Topical 5% tranexamic acid with 30% glycolic acid peel: A useful combination for accelerating the improvement in melasma. Dermatologic Therapy, 34(6), e15107. https://doi.org/10.1111/dth.15107
Saka, S., Rao, G. R. R., Komaram, R. B., Kotha, S., Tatavarthi, R., & Chitturi, L. P. (2019). Efficacy of 10% topical tranexamic acid in melasma: A randomized placebo-controlled split-face study. International Journal of Pharmaceutical Sciences and Research, 10(5), 2583-2586. https://doi.org/10.13040/IJPSR.0975-8232.10(5).2583-86
Saleem, D. Z., Shehzad, D. A., Abeer, D., Tahir, D. K., Siddiqui, D. S., & Amin, D. U. A. (2021). Effectiveness of topical 2% tranexamic acid in the management of melasma. Journal of Pakistan Association of Dermatologists, 31(3), 479-483. https://www.jpad.com.pk/index.php/jpad/article/view/1761
Saleh, F., Abdel-Azim, E., Ragaie, M., & Guendy, M. (2019). Topical tranexamic acid with microneedling versus microneedling alone in treatment of melasma: Clinical, histopathologic, and immunohistochemical study. Journal of the Egyptian Women’s Dermatologic Society, 16(2), 89. https://doi.org/10.4103/JEWD.JEWD_25_19
Shamsi Meymandi, S., Mozayyeni, A., Shamsi Meymandi, M., & Aflatoonian, M. (2020). Efficacy of microneedling plus topical 4% tranexamic acid solution vs 4% hydroquinone in the treatment of melasma: A single‐blind randomized clinical trial. Journal of Cosmetic Dermatology, 19(11), 2906-2911. https://doi.org/10.1111/jocd.13392
Sillen, M., & Declerck, P. J. (2021). A narrative review on plasminogen activator inhibitor-1 and its (patho) physiological role: to target or not to target?. International journal of molecular sciences, 22(5), 2721. https://doi.org/10.3390/ijms22052721
Thawabteh, A. M., Jibreen, A., Karaman, D., Thawabteh, A., & Karaman, R. (2023). Skin pigmentation types, causes and treatment—a review. Molecules, 28(12), 4839. https://doi.org/10.3390/molecules28124839
Yasnova, N., Sirait, S. P., & Rahmayunita, G. (2024). The effectiveness and safety of 3% tranexamic acid cream vs. 4% hydroquinone cream for mixed-type melasma in skin of color: A double-blind, split-face, randomized controlled trial. Acta Dermatovenerologica Alpina, Pannonica et Adriatica, 33(2). https://doi.org/10.15570/actaapa.2024.16
Yatsenko, T., Skrypnyk, M., Troyanovska, O., Tobita, M., Osada, T., Takahashi, S., ... & Heissig, B. (2023). The role of the plasminogen/plasmin system in inflammation of the oral cavity. Cells, 12(3), 445. https://doi.org/10.3390/cells12030445
Zhou, N., Tao, J., Yi, Z., Wu, L., Liu, Z., & Yang, B. (2024). Safety and efficacy of a picosecond 755‐nm alexandrite laser combined with topical tranexamic acid in the treatment of melasma. Journal of Cosmetic Dermatology, 23(11), 3579-3584. https://doi.org/10.1111/jocd.16432
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