Enhanced Skin Permeation and Pigmentation Reduction Effects of a Novel Tranexamic Acid-Mandelic Acid Ion-Pairing Complex.

IF 3.2 4区医学 Q3 DERMATOLOGY

Skin Research and Technology Pub Date : 2025-09-01 DOI:10.1111/srt.70222

Hyungjoon Jeon, Nojin Park, Jong Gu Won, Yong Won Shin, Jiwon Choi, Kyoungin Min, Eunjung Choi, Chang Kyu Kim, Sang-Wook Park, Nam Seo Son

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Abstract

Purpose: This study investigated the enhanced skin permeation and pigmentation reduction effects of an ion-pair complex formed between tranexamic acid (TXA) and mandelic acid (MA). The TXA-MA complex demonstrated superior skin permeability and greater inhibition of cytokine expression compared to TXA alone, ultimately proving more effective in reducing skin pigmentation.

Methods: After spectroscopic analysis of the TXA-MA ion-pairing complex (TXA-MA complex) structure, an in vitro skin permeation study was conducted using a Franz cell system with porcine skin. Additionally, the effect of the TXA-MA complex on UVB (ultraviolet B)-induced expression changes of inflammation-related genes (IL-1α, IL-6, IL-8, COX2) was evaluated using a human epidermal keratinocyte cell lines (HaCaT) cell model. Finally, an in vivo human study was performed to analyze the efficacy of TXA-MA in reducing actual skin pigmentation.

Results: The formation of the TXA-MA complex was confirmed through zeta-potential measurements, ¹H NMR study, and Fourier-transform infrared spectroscopy (FT-IR) spectroscopy. Skin permeation studies using porcine skin showed enhanced permeability of the TXA-MA complex compared to TXA at equivalent concentrations. In the HaCaT cell model, the TXA-MA complex exhibited greater inhibition of inflammatory markers IL-1α, IL-6, IL-8, and COX-2 expression than TXA alone. Finally, a 4-week human clinical study using ANTERA 3D imaging demonstrated that the TXA-MA complex was significantly more effective than TXA alone in reducing skin pigmentation.

Conclusion: This study successfully formed a TXA-MA complex. Compared to TXA, the TXA-MA complex showed superior effects in skin permeability, inhibition of inflammatory marker expression, and actual skin pigmentation reduction. These results suggest that the TXA-MA complex holds greater potential as an effective cosmetic ingredient for pigmentation improvement than TXA alone.

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一种新型氨甲环酸-扁桃酸离子配对复合物增强皮肤渗透和减少色素沉着的作用。

目的：研究氨甲环酸（TXA）和扁桃酸（MA）之间形成的离子对复合物增强皮肤渗透和减少色素沉着的作用。与单独的TXA相比，TXA- ma复合物具有更好的皮肤渗透性和更大的细胞因子表达抑制作用，最终证明在减少皮肤色素沉着方面更有效。方法：对TXA-MA离子配对复合物（TXA-MA complex）结构进行波谱分析后，采用猪皮Franz细胞体系进行体外皮肤渗透研究。此外，采用人表皮角化细胞（HaCaT）模型，评估TXA-MA复合物对UVB（紫外线B）诱导的炎症相关基因（IL-1α、IL-6、IL-8、COX2）表达变化的影响。最后，进行了一项人体体内研究，以分析TXA-MA在减少实际皮肤色素沉着方面的功效。结果：通过ζ电位测量、1H NMR研究和傅里叶变换红外光谱（FT-IR）证实了TXA-MA配合物的形成。使用猪皮肤进行的皮肤渗透研究表明，与同等浓度的TXA相比，TXA- ma复合物的渗透性增强。在HaCaT细胞模型中，TXA- ma复合物比单独TXA对炎症标志物IL-1α、IL-6、IL-8和COX-2的表达有更大的抑制作用。最后，一项使用ANTERA 3D成像的为期4周的人体临床研究表明，在减少皮肤色素沉着方面，TXA- ma复合物明显比TXA单独更有效。结论：本研究成功形成了TXA-MA复合物。与TXA相比，TXA- ma复合物在皮肤通透性、抑制炎症标志物表达和实际皮肤色素沉着减少方面表现出优越的效果。这些结果表明，与单独的TXA相比，TXA- ma复合物作为改善色素沉着的有效化妆品成分具有更大的潜力。

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来源期刊

Skin Research and Technology 医学-皮肤病学

CiteScore

3.30

自引率

9.10%

发文量

审稿时长

6-12 weeks

期刊介绍： Skin Research and Technology is a clinically-oriented journal on biophysical methods and imaging techniques and how they are used in dermatology, cosmetology and plastic surgery for noninvasive quantification of skin structure and functions. Papers are invited on the development and validation of methods and their application in the characterization of diseased, abnormal and normal skin. Topics include blood flow, colorimetry, thermography, evaporimetry, epidermal humidity, desquamation, profilometry, skin mechanics, epiluminiscence microscopy, high-frequency ultrasonography, confocal microscopy, digital imaging, image analysis and computerized evaluation and magnetic resonance. Noninvasive biochemical methods (such as lipids, keratin and tissue water) and the instrumental evaluation of cytological and histological samples are also covered. The journal has a wide scope and aims to link scientists, clinical researchers and technicians through original articles, communications, editorials and commentaries, letters, reviews, announcements and news. Contributions should be clear, experimentally sound and novel.