Skin Pharmacology and Physiology最新文献

{"title":"Novel glyceryl ascorbate derivatives inhibit type 2 alarmin cytokine induction and promote expression of epidermal barrier function-related factors in human keratinocytes in vitro.","authors":"Shunya Sahara, Natsuki Wakita, Miki Iwai, Ayumi Ueno, Miki Kuribayashi, Koich Nakaoji, Kazuhiko Hamada, Manabu Fujimoto","doi":"10.1159/000551909","DOIUrl":"https://doi.org/10.1159/000551909","url":null,"abstract":"<p><p>Atopic dermatitis is characterized by the interplay among type 2 immune responses, skin barrier dysfunction, and pruritus. Despite the pivotal role of interleukin-33 in the pathogenesis of the disease, novel therapeutic strategies remain limited. In this study, we investigated the effects of 2-O-glyceryl-6-O-hexadecanoyl ascorbic acid (2GA16), assessing its impact on inflammatory cytokine production in an epidermal cell-based atopic dermatitis model. Specifically, 2GA16 was introduced to cultured keratinocytes in an inflammatory state induced by phorbol-12-myristate-13-acetate. The inhibitory effects on inflammatory cytokines were confirmed through gene expression analysis. The analysis revealed that 2GA16 suppressed the increased expression levels of alarmins, particularly interleukin-33, in a dose-dependent manner (p < 0.01). Epidermal cells treated with 2GA16 exhibited increased expression levels of filaggrin and involucrin, both crucial to epidermal barrier formation (p < 0.05). Such changes were further supported by Western blot analysis and ex vivo tissue staining, which qualitatively showed corresponding changes at the protein level. These findings suggest that 2GA16 may mitigate the symptoms of atopic dermatitis by inhibiting the induction of type 2 alarmin cytokines in keratinocytes and restoring their capacity to form effective epidermal barriers.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-21"},"PeriodicalIF":3.2,"publicationDate":"2026-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147717972","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Network Pharmacology, Molecular Docking, Hematological Evaluation, and In Vivo Evidence Support Sakuranetin as a Redox and Inflammation-Modulating Agent Against Skin Tumorigenesis.","authors":"Humood Al Shmrany, Abdulkarim S Binshaya","doi":"10.1159/000551641","DOIUrl":"https://doi.org/10.1159/000551641","url":null,"abstract":"<p><strong>Introduction: </strong>Skin cancer is a growing global health concern, often linked to environmental carcinogens like ultraviolet radiation and chemicals. This study investigated the protective effects of sakuranetin against DMBA-induced skin cancer in mice.</p><p><strong>Methods: </strong>A total of 24 mice were randomly divided into four groups: a control group, a disease control group, and two treatment groups that received sakuranetin orally at 10 mg/kg and 20 mg/kg post-DMBA exposure for eight weeks. Tumorigenesis was evaluated through histopathology, followed by hematological (Hb, RBCs, MCV, WBCs, PCV, and MCH), antioxidant enzyme levels (SOD, CAT, GSH), lipid peroxidation, pro-inflammatory markers (IL-1β, IL-6, TNF-α, COX-2), NF-κB, and caspase-3. Additionally, network pharmacology and molecular docking were performed.</p><p><strong>Results: </strong>Treatment with Sakuranetin restored the abnormal hematological parameters, restored antioxidant enzyme levels (SOD, CAT, GSH), reduced lipid peroxidation, and significantly reduced pro-inflammatory markers, NF-κB, while increased caspase-3. Histological examination confirmed reduced neoplastic changes. Sakuranetin at the dose of 20 mg/kg completely prevents tumor development. Network pharmacology identified 53 potential sakuranetin targets, and molecular docking revealed strong binding affinities with key proteins, including COX-2 (-9.2), TGF-β (-8.5), NF-κB (-8.1), caspase-3 (-6.8), and VEGF (-5.9), which are involved in cancer pathways.</p><p><strong>Conclusion: </strong>Sakuranetin effectively mitigated DMBA-induced skin cancer through antioxidant, anti-inflammatory, and pro-apoptotic mechanisms. These findings suggest its potential as a multi-targeted therapeutic candidate for skin cancer prevention.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-17"},"PeriodicalIF":3.2,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147654850","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Human skin responses to UV (predominantly UVC at 254 nm) irradiation - in vivo kinetics of morphological changes and recovery using non-invasive two-photon tomography.","authors":"Tatiana B Lepekhina, Viktor V Nikolaev, David A Lopez Guardado, Yury V Kistenev, Maxim E Darvin","doi":"10.1159/000551755","DOIUrl":"https://doi.org/10.1159/000551755","url":null,"abstract":"<p><strong>Introduction: </strong>The effects of ultraviolet (UV) radiation on the skin are manifold. On the one hand, it aids in the production of vitamin D and is used in phototherapy. On the other hand, it can cause cell damage leading to premature skin aging and the development of various skin pathologies, including skin cancer. Despite the importance of this issue, the development and recovery of morphological changes induced by UV irradiation are still almost unexplored.</p><p><strong>Methods: </strong>In this in vivo study, two-photon tomography combined with fluorescence lifetime imaging was used to investigate structural changes in the skin of healthy volunteers over 30 days after a single UV irradiation (the lamp spectrum includes UVC ≈39.8%, UVB ≈7.5%, UVA ≈8.3%, and visible ≈44.4%) applied for 120 s at a total dose of 43.1 mJ/cm².</p><p><strong>Results: </strong>The results show that UV (predominantly UVC at 254 nm) irradiation leads to an increase in the nucleus/cell ratio, appearance of a bright perinuclear rim, disruption of the membrane, expanded intercellular space, and the appearance of sunburn cells in the epidermis, and a decrease in collagen type I in the dermis, which are recovered 30 days post-UV irradiation. The phasor plot approach enabled the separation of dermal cells into four clusters, allowing fluorescence lifetime analysis of resting and activated mast cells as well as M1 and M2 macrophages. We observed that UV (predominantly UVC at 254 nm) radiation can activate mast cells, leading to a decrease their fluorescence lifetime, whereas no effect was observed in macrophages.</p><p><strong>Conclusion: </strong>The results obtained in this in vivo study confirm that UV (predominantly UVC at 254 nm) has damaging effect on all skin layers. Two-photon tomography is an effective non-invasive method for in vivo imaging morphological changes in the skin following UV irradiation and for studying severe photodamage.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-36"},"PeriodicalIF":3.2,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147521944","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cysteinamide Enhances Fibroblast Survival and Wound Healing by Preventing Serum Deterioration in High-Glucose Conditions.","authors":"Joon Yong Choi, Nam Gyoung Ha, Weon-Ju Lee, Yong Chool Boo","doi":"10.1159/000551460","DOIUrl":"10.1159/000551460","url":null,"abstract":"<p><strong>Introduction: </strong>In patients with diabetes, persistent hyperglycemia causes chemical changes in serum components, increasing the incidence of various complications such as skin wounds. To better understand glucose-associated chemical stress on serum components, this study explores small-molecule nutrients to protect human dermal fibroblasts (HDFs) from glucose-rich, chemically deteriorated culture conditions.</p><p><strong>Methods: </strong>Various cell culture media with different concentrations of glucose and various test compounds were subjected to heat treatment as a chemically accelerated model of serum deterioration. The heat-treated and non-heat-treated media were compared to each other in terms of the content of glycation products and their effects on cell viability and wound healing in vitro.</p><p><strong>Results: </strong>There was no difference in the content of glycation products or their effects on cell viability between the non-heat-treated low-glucose (LG, 5.5 m<sc>m</sc>) and high-glucose (HG, 50 m<sc>m</sc>) media that were not heat treated. However, the heat-treated HG media had a higher content of glycation products and decreased cell viability compared to the heat-treated LG media. Of the 20 free amino acids, 20 amidated amino acids and various antioxidants derived from cysteine (Cys) or ascorbic acid (AA) added to the media, followed by heat treatment, only cysteinamide (C-NH₂) enhanced the viability and wound healing of HDFs cultured in the heat-treated HG media. C-NH₂ reduced glycation of serum proteins while forming its own glycation products, suggesting a competitive interaction with glucose-derived reactions.</p><p><strong>Conclusion: </strong>These findings provide proof-of-concept evidence that C-NH₂ can protect serum components and improve fibroblast-associated wound closure under chemically stressed, glucose-rich conditions. Further studies using physiologically relevant models are required to evaluate its biological and translational significance.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-16"},"PeriodicalIF":3.2,"publicationDate":"2026-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147444904","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Oral Administration of Specific Bioactive Collagen Peptides in the Treatment of Moderate Forms of Atopic Dermatitis: A New Approach.","authors":"Ehrhardt Proksch, Michael Schunck, Denise Zdzieblik, Steffen Oesser","doi":"10.1159/000551215","DOIUrl":"10.1159/000551215","url":null,"abstract":"<p><strong>Introduction: </strong>Effective management of atopic dermatitis (AD) remains challenging, as current therapies often rely on topical corticosteroids associated with adverse effects and limited long-term tolerability.</p><p><strong>Methods: </strong>This double-blind, randomized, placebo-controlled trial investigated the effects of a 12-week oral supplementation with specific bioactive collagen peptides (BCPs, CURADERM®) on clinical symptoms and skin physiology in adults with moderate AD. Participants were randomized to receive either 5 g of BCP or placebo daily.</p><p><strong>Results: </strong>BCP supplementation led to significantly lower corticosteroid rescue medication use (0.94 ± 1.42 g vs. 5.60 ± 7.82 g; p = 0.045; d = 0.847) and an earlier reduction in pruritus, as shown by improvements in the 5-D Pruritus Scale at week 4 (p = 0.024, d = 1.49). Favourable effects were also observed for key physiological parameters of the skin, including maintenance of physiological pH (4.5-5.5) and improved hydration of lesional areas (p = 0.040, d = 1.44). No treatment-related adverse events occurred.</p><p><strong>Conclusion: </strong>Taken together, these findings provide first placebo-controlled evidence that oral BCP supplementation supports skin barrier recovery, stabilizes physiological skin function, and accelerates symptom relief in mild-to-moderate AD. Confirmation of these promising results in larger trials is warranted to validate treatment effects.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-13"},"PeriodicalIF":3.2,"publicationDate":"2026-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13155738/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147318140","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Monocentric, Vehicle-Controlled, Double-Blind Study to Assess the Short- and Long-Term Effects of a Ceramide NP C15-Containing Emollient on the Skin Microbiome and the Skin Barrier Function in Sensitive Skin.","authors":"Florian Dimmers, Doreen Reichert, Thach Nguyen, Niklas Lück, Haribaskar Ramachandran, Andreas Bremges, Jennifer Schild, Michaela Humbek, Susanne Grether-Beck, Andrea Rossi, Christian Staerk, Charlotte Esser, Jean Krutmann","doi":"10.1159/000551043","DOIUrl":"10.1159/000551043","url":null,"abstract":"<p><strong>Introduction: </strong>Sensitive skin is a common skin condition that impairs quality of life and is characterized by unpleasant sensations to normally nonirritating stimuli. Restoration of skin barrier integrity can relieve symptoms, and accumulating evidence indicates a contributory role of the skin microbiome not only in barrier function but also as a potential modulator in sensitive skin. Ceramide-containing emollients improve barrier function and may modulate microbial communities via restoration of stratum corneum lipids, hydration, and immune regulation.</p><p><strong>Methods: </strong>In this randomized, double-blind, vehicle-controlled trial, an emollient containing Ceramide NP C15 was evaluated for its effects on sensitive skin symptoms and skin barrier function. Fifty participants applied the study products in a split-body design for 6 weeks. Primary assessments included skin physiology and symptom burden. Furthermore, skin microbiota changes were explored using flow-cytometry (FC)-based bacterial profiling and 16s rRNA gene sequencing.</p><p><strong>Results: </strong>Both the Ceramide NP C15 formulation and the vehicle were associated with improvements in subjective symptoms. In participants with impaired skin barrier, treatment with the ceramide formulation was associated with a significant reduction in transepidermal water loss. FC- and 16S-based analyses indicated modest, treatment-associated changes in skin microbiota composition including an early and sustained increase in microbial evenness and a significant enrichment of Bifidobacterium.</p><p><strong>Conclusion: </strong>In this exploratory, randomized controlled study, a Ceramide NP C15-containing emollient was associated with improvements in skin barrier function. Exploratory microbiome analyses suggested treatment-associated changes in microbial community characteristics, which should prompt further investigations in their clinical relevance for sensitive skin.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-18"},"PeriodicalIF":3.2,"publicationDate":"2026-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147318230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In vitro and ex vivo cutaneous bioavailability and biotransformation of silymarin and its constituents.","authors":"Jitka Vostálová, Pavel Kosina, Bohumil Zálešák, Kateřina Valentová, Barbora Papoušková, Alena Ryšavá, Jiří Hanyk, Alena Rajnochová Svobodová","doi":"10.1159/000550859","DOIUrl":"https://doi.org/10.1159/000550859","url":null,"abstract":"<p><strong>Introduction: </strong>Silymarin (SM), an extract from the fruits of the milk thistle (Silybum marianum L., Asteraceae) has pleiotropic effects on human health. SM's biological activity assigns to its constitutive polyphenols, mainly flavonolignans. SM has become increasingly interesting for dermal applications. There are currently several commercial dermatological preparations available on the market containing SM or its dominant flavonolignan silybin (SB) as the active ingredients. The metabolic transformation of compounds in skin including SM's polyphenols has only been marginally investigated. Therefore, this study focused on the metabolization of SM and its pure polyphenols (SB, isosilybin (ISB), 2,3-dehydrosilybin (DHSB), silychristin (SC), silydianin (SD) and taxifolin (TA)) in the skin.</p><p><strong>Methods: </strong>Human skin ex vivo (HSE) and normal human dermal fibroblasts (NHDF) were used as experimental models. For cell treatment, a concentration of 10 M (pure compounds) or 4.825 mg L-1 (SM) was used. For HSE treatment, 50 M (pure compounds) or 24.124 mg L-1 (SM) was used.</p><p><strong>Results: </strong>The penetration of studied polyphenols into the skin correlated with their lipophilicity (DHSBISBSBSCSDTA). The bioavailability of SM's polyphenols was relatively high, and thus the substances can be expected to modulate biological processes in the region close to their application site. SM's polyphenol metabolites of the first and second phase of biotransformation were identified in NHDF and HSE.</p><p><strong>Conclusion: </strong>In HSE, the metabolic transformation of SM's components and its pure polyphenols was more extensive, as skin fragments are a more complex cellular and metabolically active system. Human skin ex vivo seems to be a useful tool for studying compounds biotransformation at topical application.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-24"},"PeriodicalIF":3.2,"publicationDate":"2026-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147277144","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optical Coherence Tomography Mapping of the Scattering Coefficient to Study the Skin Hydration Process under Optical Clearing.","authors":"Yury I Surkov, Isabella A Serebryakova, Sergey M Zaytsev, Elina A Genina, Valery V Tuchin, Yulia I Svenskaya","doi":"10.1159/000551016","DOIUrl":"10.1159/000551016","url":null,"abstract":"<p><strong>Introduction: </strong>Skin hydration, which is defined by the hydration index and the spatial distribution of water, represents one of the key parameters reflecting the functional state of the skin. Although various optical methods have been proposed to study the hydration process, these techniques are often limited by a shallow probing depth, insufficient depth resolution, or low spatial and temporal resolution, which precludes a comprehensive assessment of the skin response to topical pharmaceutical agents.</p><p><strong>Methods: </strong>We present an approach for the quantitative assessment and visualization of skin dehydration and rehydration processes with high depth and temporal resolutions. The proposed method is based on reconstructing the scattering coefficient from the optical coherence tomography data. We used this approach to quantify the effective skin dehydration depth and rehydration time in rats ex vivo following the topical application of 70% ethanol and an ethanolic solution of the betamethasone dipropionate, glucocorticosteroid, in both the presence and absence of ultrasound exposure (1 MHz, 0.5 W/cm2, 2 min).</p><p><strong>Results: </strong>Ethanol was shown to induce reversible dehydration of the upper skin layers (168 ± 88 µm) with the recovery occurring within 21 ± 3 min. Ultrasound treatment of the ethanol application area resulted in the enhancement of its penetration depth up to 262 ± 63 µm and reduced the rehydration time to 14 ± 3 min. The addition of betamethasone dipropionate to the ethanol solution further increased the dehydration depth and delayed rehydration process. Visualization of the obtained data as heatmaps enabled a quantitative evaluation of the spatiotemporal changes in the skin.</p><p><strong>Conclusion: </strong>The proposed approach proved to be effective for investigating water diffusion processes in the skin and would facilitate the analysis of dynamic changes in both healthy and pathological tissues, as well as the assessment of the effects of various topical chemical and physical treatments. This work holds significant implications for both basic and practical researches at the interface between optics and biomedicine.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-13"},"PeriodicalIF":3.2,"publicationDate":"2026-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146214063","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Effect of Sequential Topical Application of Dermatologic Medications on Absorption: Clinical Considerations.","authors":"Sarah E Burstein, Howard I Maibach","doi":"10.1159/000550716","DOIUrl":"10.1159/000550716","url":null,"abstract":"<p><strong>Background: </strong>Sequential application of topical dermatologic medications - defined as applying two or more agents to the same anatomical site within a short interval - is common in dermatologic therapy. Despite widespread clinical use, the pharmacologic consequences of application order, timing, and vehicle interactions on percutaneous absorption remain incompletely characterized.</p><p><strong>Summary: </strong>This review synthesizes clinical, in vivo human volunteer, and mechanistic in vitro and ex vivo evidence evaluating the impact of sequential topical application on cutaneous drug absorption and bioavailability. A qualitative literature search identified twelve eligible studies, including randomized controlled trials, in vivo human studies, and experimental diffusion and visualization models. Across heterogeneous study designs, sequential application was not pharmacologically neutral. Alterations in percutaneous absorption were driven by changes in stratum corneum barrier properties and vehicle or excipient interactions rather than formulation class alone. Sequencing effects were most pronounced when the first-applied product induced keratolysis, hydration or occlusion, or lipid film formation, or when vehicle redissolution and redistribution altered the effective treated surface area. In barrier-compromised conditions, such as atopic dermatitis, changes in application order were less likely to translate into measurable clinical effects. Fixed-combination formulations generally demonstrated more consistent and predictable cutaneous delivery than free sequential regimens.</p><p><strong>Key messages: </strong>Sequential topical application can significantly influence percutaneous absorption through barrier modification and vehicle interactions. Pharmacokinetic effects are context-dependent and cannot be inferred solely from formulation type. Mechanism-informed sequencing and judicious selection of compatible vehicles may improve predictability of topical drug delivery, highlighting the need for standardized, pharmacologically focused studies to guide application order and timing.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-14"},"PeriodicalIF":3.2,"publicationDate":"2026-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146087000","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Supramolecular Salicylic Acid-Betaine with Superior Epidermal Benefits and Better Tolerance: In vitro Proof of Concept Studies.","authors":"Yanfeng Liu, Wei Wang, Ya Hu, Mei Zhang, Qingsheng Tao, Nan Huang, Zhenyuan Wang, Hao Wang, Jiaheng Zhang, Yu Gao","doi":"10.1159/000550692","DOIUrl":"10.1159/000550692","url":null,"abstract":"<p><strong>Introduction: </strong>Recent progress in supramolecule research has led to a surge in its application in cosmetic products. However, comprehensive investigation of the potential benefits, especially differentiating biological activities and associating that with physical-chemical properties, remains to be established. The current study aimed to investigate the supramolecular salicylic acid-betaine (Supra-SA-B) compared to its physical mixture (SA+B) for effects on epidermal homeostasis and topical insult potential.</p><p><strong>Methods: </strong>The structure of supra-SA-B and SA+B was characterized by a powder X-ray diffractometer. Skin tolerance was evaluated by applying SA, Supra-SA-B, and SA+B to human keratinocytes or SkinEthic™ reconstructed human epidermis (RHE) models. Inflammatory cytokines were assessed by Luminex assay. Histological morphology was evaluated by hematoxylin-eosin staining, with aquaporin-3 (AQP3) and Ki67 measured by immunofluorescence. RNA sequencing characterized overall biological response.</p><p><strong>Results: </strong>Characteristic peaks remained the same for Supra-SA-B after freeze-drying verified that their crystalline structures were retained in the current solution. Supra-SA-B treated groups demonstrated significantly higher viabilities compared to SA or SA+B. With 18-h of treatment, Supra-SA-B treated group released fewer cytokines. In addition, Supra-SA-B demonstrated a better hydration effect with increased AQP3 expression and more organized epidermal structure. Consistent result was observed in the RNA transcriptomic profiles of RHE models. Supra-SA-B did not induce major transcriptome drift as compared to SA or SA+B, with less evident negative impact on loricrin, and late cornified envelope gene expression. Hyaluronic acid synthase boosting was maintained.</p><p><strong>Conclusion: </strong>Supra-SA-B ameliorated skin tolerance risk for SA, enhanced hydration with less insult on barrier functions, suggesting promising potential for cosmetic application.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"1-11"},"PeriodicalIF":3.2,"publicationDate":"2026-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146087012","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}