90 DEPIGMENTATION


Tranexamic acid: next-gen skin depigmenting active


Mihaela Gorcea, Mary R. Davis, Jon Anderson - Actives International ABSTRACT


Tranexamic acid (TXA) is a traditional hemostatic, anti-inflammatory and anti- allergenic ingredient used as an oral supplement for treatment of melasma.1-7 Recently, it is used in topical cosmetic and dermatological applications for skin pigmentation disorders and vascular related pigmentation issues.1-7


ViaDerm® TXA (INCI:


Tranexamic acid) is a next generation skin depigmenting active that delivers a multi- targeted mode of action to address multiple concerns of skin pigmentation. Its biological mode of action impacts plasminogen/plasmin activity associated with melanogenesis and angiogenesis pathways. In vivo clinical efficacy study results demonstrate that it lightens dark spots/hyperpigmentation, imparts an even skin tone and enhances skin radiance and brightness. It also reduces red spots and redness associated with vascular pigmentation problems.


In the beauty and personal care industry, there is an increasing consumer demand for effective multifunctional skin products that can address various skin concerns. Skin pigmentation is one area where multifunctionality is especially important.Traditional dark spot correctors and skin brighteners work via several known biological pathways such as tyrosinase inhibition, antioxidant activity or enzymatic degradation. ViaDerm® TXA (INCI: Tranexamic acid)


is a next generation of skin depigmenting active and dark spot corrector that employs


UV Light Keratinocytes


Plasminogen Activator


TXA Plasmin α-MSH Melanocytes


Figure 1: Proposed mechanism of action of tranexamic acid (TXA) in treatment of skin pigmentation and vascular related pigmentation concerns6


PERSONAL CARE March 2024


Arachidonic Acid Angiogenesis


TXA VEGF


a different biological mode of action to affect skin pigmentation. It inhibits the activity of plasminogen/plasmin system and the subsequent inflammation cascade, and prevents the UV induced activation of melanocytes, thus inhibiting melanogenesis.1-7


Biological activity of tranexamic acid The proposed biological mechanism of action of tranexamic acid (TXA), with emphasis on treatment of skin pigmentation concerns and vascular related pigmentation issues, is


shown in Figure 1.1-7 It is well recognized that


excessive UV light exposure is one of the key factors in the development of skin dark spots, hyperpigmentation and melasma. Plasmin (a serine protease enzyme) is an


activated form of plasminogen, known for its anti-fibrinolytic activity.1-7


It is known that


UV radiation induces plasminogen activator synthesis and increases plasmin activity in keratinocytes.1-7 ■ Activated plasmin (AP) has an impact on three different pathways that are involved in melanogenesis: 1-7 ■ AP increases the release of arachidonic acid (AA), which stimulates melanogenesis via prostaglandins (PGE2). ■ AP elevates alpha melanocyte stimulating hormone (α-MSH), which further activates melanin synthesis in melanocytes. ■ AP releases fibroblast growth factor (FGF), which stimulates melanin production in skin. In addition, activated plasmin stimulates


vascular endothelial growth factor (VEGF), thus stimulating angiogenesis.1-7 It is reported that tranexamic acid (trans- 4-aminomethylcyclohexanecarboxylic acid) inhibits keratinocyte - melanocyte signaling (induced by UV light) and inhibits plasminogen activator synthesis by preventing binding of plasminogen to the keratinocytes.


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