To evaluate the influence of tranexamic acid on epidermal permeability barrier function in rosacea and its potential mechanisms. A randomized, vehicle controlled, split-face study was performed on 30 rosacea patients. This study involved 2 weeks of 3% tranexamic acid solution treatment and vehicle control treatment. Skin physiological parameters, including skin surface pH, stratum corneum hydration, and transepidermal water loss, were measured. The expression of protease-activated receptor 2 (PAR-2) in rosacea and normal skin samples was assessed with immunohistochemical staining. The expression of PAR-2 in HaCaT keratinocytes was determined using reverse transcription polymerase chain reaction after stimulation with tranexamic acid. Changes of intracellular calcium induced by PAR-2 activation were measured using Fluo-4 NW calcium assay. Individuals with rosacea expressed a higher baseline level of PAR-2 compared with normal skin. Tranexamic acid improved the permeability barrier function in rosacea patients and inhibited calcium mobilization in keratinocytes induced by PAR-2 activation. The PAR-2 expression was not altered by tranexamic acid stimulation. Topical tranexamic acid could improve the epidermal permeability barrier function and clinical signs of rosacea, likely resulting from inhibition of PAR-2 activation and consequent calcium influx. Thus, tranexamic acid could serve as an adjuvant therapy for rosacea.
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