Skin Pharmacology and Physiology最新文献

{"title":"Do Transdermal Administration of α₁- and α₂-Adrenergic Receptor Antagonists Modulate Sweating in Exercising Young Females in the Heat?","authors":"Lu Meng, Hui Wang, Junto Otsuka, Yumi Okamoto, Shotaro Yokoyama, Shoma Oshima, Hanano Kato, Tze-Huan Lei, Tatsuro Amano","doi":"10.1159/000546961","DOIUrl":"10.1159/000546961","url":null,"abstract":"<p><strong>Introduction: </strong>Adrenergic modulation of sweating remains equivocal in females. We investigated whether α₁- and α₂-adrenergic receptors can modulate sweating during active heat stress in healthy female participants.</p><p><strong>Methods: </strong>Thirty young adults (15 females) cycled at 50% peak oxygen uptake for 30 min at 32°C and 40% relative humidity. Sweat rates (ventilated capsule technique) on both forearms were assessed following pretreatment with terazosin (α₁-adrenergic receptor antagonist), rauwolscine (α₂ antagonist), or control (NaCl) using transdermal iontophoresis procedure. The efficacy of α₁ blockade was confirmed postexercise with phenylephrine (α₁-adrenergic agonist)-induced sweating, while α₂ antagonist efficacy was verified in a separate follow-up study assessing clonidine (α₂ agonist)-induced cutaneous vasoconstriction.</p><p><strong>Results: </strong>Participants sweated by 0.32 ± 0.13 and 0.54 ± 0.26 mg∙cm-2∙min-1 at the end of exercise for females and males, respectively. Neither terazosin nor rauwolscine affected sweating during exercise in males (p ≥ 0.125, interaction and treatment effect) or females (p ≥ 0.277) as compared to control sites. However, the reduction in sweat rate at the terazosin-treated site was negatively correlated with sweat rate at control sites in both sexes (all p ≤ 0.050, r ≤ -0.514), while no such correlation was observed for rauwolscine. Successful α₁-blockade was confirmed by attenuated phenylephrine-induced sweating during postexercise (p ≤ 0.025). Rauwolscine effectively abolished clonidine-induced cutaneous vasoconstriction in a follow-up study, verifying successful transdermal delivery.</p><p><strong>Conclusion: </strong>The α₁- and α₂-adrenergic receptors do not alter sweating during moderate-intensity exercise in males and females, at least among individuals with relatively low sweat production.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"149-158"},"PeriodicalIF":3.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144326852","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 Provocation on Formation of the Corneocyte Lipid Envelope.","authors":"Philip Wesley Wertz","doi":"10.1159/000546731","DOIUrl":"10.1159/000546731","url":null,"abstract":"<p><strong>Background: </strong>The major carriers of linoleic acid in the epidermis are an acylglucosylceramide in the viable portion of the epidermis and an analogous acylceramide in the stratum corneum. The acylglucosylceramide and acylceramide are the precursors of the corneocyte lipid envelope (CLE).</p><p><strong>Summary: </strong>Oxidation of the ester-linked linoleate by two lipoxygenases working in tandem has been shown to be involved in CLE formation. Acylglucosylceramide appears to be the substrate for initial CLE formation at the bottom of the stratum corneum, while acylceramide is the precursor for the covalently attached ω-hydroxyceramide thereafter. It would be expected that consumption of linoleate in CLE formation would decrease the linoleate content of the remaining acylceramide; however, this is not observed for total acylceramide. When acylceramide from only the outer layers of stratum corneum has been analyzed, the linoleate content is notably reduced compared to the values found for these lipids from full thickness stratum corneum or epidermis. This is consistent with a major role for the linoleate-containing acylceramide in the later stages of CLE maturation. This also suggests that a mechanism that is not selective for ester-linked linoleate may also be involved in early CLE formation, while the oxygen-dependent mechanisms are essential in the later stage of envelope maturation.</p><p><strong>Key message: </strong>This review proposes an oxygen-independent mechanism that may contribute to the early stages of CLE formation. The lipoxygenase-dependent contribution to the formation of the CLE would be more prominent in the later stages of maturation.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"159-164"},"PeriodicalIF":3.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144584732","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 Antibacterial and Antifungal Activity of a Skin Ointment and Its Active Pharmaceutical Ingredients Larch Turpentine, Turpentine Oil, and Eucalyptus Oil.","authors":"Elisa Pianta, Nils Günnewich, Christian Zimmermann, Orlando Petrini, Juan Diaz-Miyar, Cristina Fragoso-Corti","doi":"10.1159/000543158","DOIUrl":"10.1159/000543158","url":null,"abstract":"<p><strong>Introduction: </strong>Turpentine derivatives and eucalyptus oil are herbal substances traditionally used to treat various skin infections. Limited non-clinical data suggest they exert an immunological activity, but only scant information exists on their antibiotic effects. This in vitro study has been carried out to investigate the antibacterial and antifungal activity of a marketed skin ointment; its active pharmaceutical ingredients larch turpentine, eucalyptus oil, and turpentine oil; and their mixture, against bacteria and yeasts commonly present on the skin and causing skin infections.</p><p><strong>Methods: </strong>The antibiotic activity was tested using the drop dilution assay on the Gram-positive bacteria Staphylococcus aureus (wild type), a methicillin-resistant S. aureus strain, S. epidermidis, S. haemolyticus, Streptococcus pyogenes, the Gram-negative Pseudomonas aeruginosa, and the yeasts Candida albicans and C. tropicalis.</p><p><strong>Results: </strong>The ointment exerts a strong inhibitory effect on all Gram-positive bacteria at a concentration of 5 g/100 mL in the Müller-Hinton medium. It also has inhibiting effect on both Candida species but does not inhibit P. aeruginosa growth. As for the single active pharmaceutical ingredients, larch turpentine was the most active substance. The mixture of the three ingredients, in the concentrations used in the ointment, had a higher antibiotic effect than any of the individual ingredients studied, suggesting at least an additive activity.</p><p><strong>Conclusions: </strong>Our study has shown that the herbal ingredients and their combination exert antimicrobial activities, especially against Gram-positive bacteria, that justify their use in the treatment of skin infections.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"68-75"},"PeriodicalIF":2.8,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12136597/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142954671","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":"Bioavailability of Hydroquinone from Topical Formulations: A Product Comparison Study Using the in vitro Permeation Test.","authors":"Paul A Lehman, Thomas J Franz","doi":"10.1159/000545618","DOIUrl":"10.1159/000545618","url":null,"abstract":"<p><strong>Introduction: </strong>The in vitro Permeation Test (IVPT) is considered to be an important tool for assessing the topical pharmacokinetics of dermatologic formulations. An IVPT study evaluating products that contain the skin bleaching agent, hydroquinone (HQ), as the active ingredient, is presented in support of the value of IVPT in comparing the relative bioavailability of HQ products from different commercial products.</p><p><strong>Methods: </strong>Ten former OTC and Rx products were evaluated for in vitro bioavailability using human ex vivo skin in Franz diffusion cells. In addition, to assess the correlation between in vitro and in vivo absorption, the suction blister technique was used to determine HQ concentration in interstitial fluid from two products differing in HQ bioavailability.</p><p><strong>Results: </strong>Significant differences in HQ absorption between products were found. Total absorption varied from 27 to 279 μg/cm2/48 h, and neither total absorption nor the rates of absorption were found to correlate with labeled drug concentration. In vivo suction blister data on the two products were in accordance with the IVPT results.</p><p><strong>Discussion: </strong>Overall, this study demonstrates the sensitivity and value of the IVPT method for detecting differences in the pharmacokinetics of topical formulations containing a single therapeutic agent but which differ in formulation design.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"113-120"},"PeriodicalIF":3.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143781103","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 Brief Review of Vehicles for Topical Therapies.","authors":"Kripa Ahuja,Miranda An,Peter Lio","doi":"10.1159/000541418","DOIUrl":"https://doi.org/10.1159/000541418","url":null,"abstract":"Background Topical therapy has been a fundamental part of dermatology, evolving from early ointments to advanced transdermal treatments. These formulations allow for effective management of skin conditions by maximizing local drug delivery and minimizing systemic effects. Modern topical therapies continue to benefit from innovations that improve both efficacy and patient outcomes. Summary Topical formulations consist of a vehicle and active ingredients, with the vehicle enhancing drug absorption and patient experience. Historically categorized by physical properties, vehicles are vital in drug delivery. Recent innovations, such as nanoemulsions and derma-membrane structures, offer improved skin penetration and therapeutic results, representing significant advancements in topical treatment options. Key Messages Topical therapies provide targeted, effective treatment in dermatology with minimal systemic side effects. Vehicle choice is essential to therapy success, and innovations such as nanoemulsions are improving drug delivery and patient care. Ongoing research into novel delivery systems continues to enhance the future of dermatological treatments.","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":"20 1","pages":"1-9"},"PeriodicalIF":2.7,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142269257","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":"Diesel Particulate Matter Permeation into Normal Human Skin and Intervention Using a Topical Ceramide Formulation.","authors":"Kyong-Oh Shin, Kenya Ishida, Hisashi Mihara, Yerim Choi, Jae-Ho Park, Soo-Hyun Park, Jin-Taek Hwang, Joan S Wakefield, Yasuko Obata, Yoshikazu Uchida, Kyungho Park","doi":"10.1159/000539291","DOIUrl":"10.1159/000539291","url":null,"abstract":"<p><strong>Introduction: </strong>Diesel particulate matter (DPM) emitted from diesel engines is a major source of air pollutants. DPM is composed of elemental carbon, which adsorbs organic compounds including toxic polycyclic aromatic hydrocarbons (PAHs). The skin, as well as airways, is directly exposed to DPM, and association of atopic dermatitis, psoriasis flares, and premature skin aging with air pollutant levels has been documented. In skin, the permeation of DPM and DPM-adsorbed compounds is primarily blocked by the epidermal permeability barrier deployed in the stratum corneum. Depending upon the integrity of this barrier, certain amounts of DPM and DPM-adsorbed compounds can permeate into the skin. However, this permeation into human skin has not been completely elucidated.</p><p><strong>Methods: </strong>We assessed the permeation of PAHs (adsorbed to DPM) into skin using ex vivo normal (barrier-competent) organ-cultured human skin after application of DPM. Two major PAHs, 2-methylnaphthalene and triphenylene, and a carcinogenic PAH, benzo(a)pyrene, all found in DPM, were measured in the epidermis and dermis using liquid chromatography electrospray ionization tandem mass spectrometry. In addition, we investigated whether a topical formulation can attenuate the permeation of DPM into skin.</p><p><strong>Results: </strong>2-Methylnaphthalene, triphenylene, and benzo(a)pyrene were recovered from the epidermis. Although these PAHs were also detected in the dermis after DPM application, these PAH levels were significantly lower than those found in the epidermis. We also demonstrated that a topical formulation that has the ability to form more uniform membrane structures can significantly suppress the permeation of PAHs adsorbed to DPM into the skin.</p><p><strong>Conclusion: </strong>Toxic compounds adsorbed by DPM can permeate even barrier-competent skin. Hence, barrier-compromised skin, such as in atopic dermatitis, psoriasis, and xerosis, is even more vulnerable to air pollutants. A properly formulated topical mixture that forms certain membrane structures on the skin surface can effectively prevent permeation of exogenous substances, including DPM, into skin.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"32-39"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141071624","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":"Cluster Analysis Identifies Clinical Phenotypes of Primary Hyperhidrosis.","authors":"Mattias A S Henning, Gregor B E Jemec, Ole B Pedersen, Elisabeth H Taudorf","doi":"10.1159/000540516","DOIUrl":"10.1159/000540516","url":null,"abstract":"<p><strong>Introduction: </strong>Identifying subgroups of patients with primary hyperhidrosis (PHH) can improve the understanding of the disease pathophysiology. The study objective was to determine the naturally occurring subgroups of patients with PHH based on clinical characteristics.</p><p><strong>Methods: </strong>In this retrospective cohort study, data were collected from participants included in a clinical trial. The data were collected between January 2020 and June 2021 from outpatients with PHH attending a dermatologic department in Denmark. Overall, 84 patients with PHH were screened for inclusion in the clinical trial. Of these, 41 met the eligibility criteria. Four participants were excluded because of missing data. The main outcome was the identification of subgroups of patients with PHH using an unsupervised hierarchical cluster analysis.</p><p><strong>Results: </strong>Overall, 37 patients were included {28 (76.7%) females; median age at inclusion 28.0 (interquartile range [IQR] 24.0-38.3); median body mass index 24.9 (IQR 20.9-27.4); median age of onset 13.0 (IQR 9.5-18.5); and 26 (70.3%) had a familial disposition toward PHH}. Two clusters of 18 and 17 patients were identified. The first cluster had, when compared to the second, a younger age of onset (median age 11.0 [IQR 0-13.0] vs. 17.0 [IQR 15.0-21.0], p = 0.003) and higher sweat rates on gravimetry (median 175.0 [IQR 121.2-252.5] vs. 40.0 [IQR 20.0-60.0] milligrams of sweat/5 min, p < 0.001) and transepidermal water loss (median 93.7 [IQR 91.2-97.8] vs. 59.0 [IQR 44.4-73.2] g/m2/h, p < 0.001). No differences were observed for the other variables.</p><p><strong>Conclusions: </strong>This study identifies 2 subgroups of patients with PHH. The patients with an onset of PHH during childhood had a substantially higher sweat and evaporation rate in adulthood than those with an onset during adolescence. These findings may imply a changed understanding of the pathophysiology of PHH, by indicating that an early disease onset can lead to a worse disease course.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"63-69"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142093713","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":"Effects of a pH-Regulating Emollient Cream in Mild Atopic Dermatitis Patients with Moderate Localized Lesions.","authors":"Sue Phay Ng, Stephan Bielfeldt, Sabrina Laing, Simon Danby, Michael J John Cork","doi":"10.1159/000541022","DOIUrl":"10.1159/000541022","url":null,"abstract":"<p><strong>Introduction: </strong>Increased skin pH values in patients with atopic dermatitis (AD) contribute to poor antimicrobial and permeability barrier functions of the skin. In practice, the majority of topical preparations available for dry skin conditions do not provide sufficient pH and buffering capacity for maintaining optimum skin surface conditions. To address this issue, we tested a novel zinc lactobionate preparation to determine whether the regular application would lower skin surface pH, and in doing so improve the condition of lesional skin.</p><p><strong>Methods: </strong>The assessment for local severity of AD was done with the Scoring Atopic Dermatitis Index (SCORAD) and skin dryness was assessed by capacitance measurement.</p><p><strong>Results: </strong>The results showed that the test product lowered skin pH and improved AD skin lesions from moderate to mild during 2 weeks of application. In the treated area a lowered pH of about 0.85 units was found. Together with the lowering of pH, the local SCORAD significantly improved from 8.3 on average down to 4.0, while in the untreated area, only a slight improvement (from 8.2 to 6.4) was found.</p><p><strong>Conclusion: </strong>Synergistic effects of the test product's pH lowering and emollient properties might explain the observed improvements in clinical signs of AD and further research against a comparator would allow the specific contribution of pH modulation to these improvements to be unambiguously isolated.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"49-58"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11488831/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142093714","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":"Evaluation of Bioequivalence and Pharmacokinetic Profiles for Topical Desonide Cream Using Chinese Skins.","authors":"Yuanyuan Sun, Nan Yang, Jie Huang, An Yao, Ling Ye, Shuang Yang, Min Xiao, Xuqing Zhang, Jinsong Ding, Yun Kuang, Yali Zhou, Guoping Yang","doi":"10.1159/000540782","DOIUrl":"10.1159/000540782","url":null,"abstract":"<p><strong>Introduction: </strong>Skin-blanching assay has been established as a surrogate method for assessing bioequivalence of topical corticosteroids. This study aimed to apply the skin-blanching assay to evaluate the bioequivalence of a test desonide cream (T) compared with the reference Desonide® (R) using Chinese skins. Additionally, the pharmacokinetics and safety profiles were also assessed.</p><p><strong>Methods: </strong>By detecting the degree of skin blanching under different dose durations in a pilot dose-duration-response study, the area under the observed effect-time curve (AUEC) and half of the maximum effect (ED50) was calculated. Based on this, the skin color of different time points after a dose duration of ED50, D1 (0.5 × ED50), and D2 (2 × ED50) were detected as a pharmacodynamic indicator to compare between test and reference creams. Single-center, single-dose, randomized, open-label, two-cycle crossover pharmacokinetic studies were designed to make sure the exposure of tested formulationswas not higher than that of the reference formulations. Subjects experiencing adverse events (AEs) were monitored and utilized for safety analysis.</p><p><strong>Results: </strong>These studies involved 12 subjects for the dose-duration-response study, 100 subjects for the bioequivalence study, and 12 subjects for the pharmacokinetic study. The results showed that the population ED50 was 0.88 ± 0.45 h; the mean ratio of area under effective curve from 0 to 24 h (AUEC0-24h) of test and reference preparations was 0.95, with a 90% confidence interval as 88.09-101.72%, indicating the bioequivalence of the test formulation and Desonide®. The maximum plasma concentration (Cmax) and area under the concentration time curve from time 0 to the last time point (AUC0-t) of T and R were 20.8 ± 11.5 pg/mL versus 19.7 ± 10.1 pg/mL, respectively, and 451.04 ± 363.65 pgh/mL versus 541.47 ± 581.41 pgh/mL, respectively. The systemic exposure of a single dose of the test cream was not higher than that of the reference preparation. All of the volunteers experienced grade 1 AEs, suggesting that single administration of the test desonide cream is well tolerated in the Chinese healthy population.</p><p><strong>Conclusions: </strong>This study demonstrated the applicability of skin-blanching assay in Chinese skins and established the bioequivalence of test and reference desonide creams.</p>","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"70-79"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142005175","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 Consideration on Infinite and Finite Dosing in Skin Permeation Using Reconstructed Models.","authors":"Yuko Saeki, Eiko Kato, Yoshihiro Tokudome","doi":"10.1159/000541325","DOIUrl":"10.1159/000541325","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;When vitamin derivatives penetrate the epidermis, they release active compound such as ascorbic acids (AsA) and tocopherols via enzymatic digestion of chemical modifiers. To determine the transdermal penetration of the derivatives, the total permeation of both the derivatives and their active compounds that released from the derivatives should be considered. In this study, we established a skin penetration test method using a cultured, reconstructed skin model with active epidermal enzymes. And we analyzed two vitamin derivatives with different chemical properties: magnesium ascorbyl phosphate (APM) and sodium tocopheryl phosphate (TPNa), both of which has been confirmed their skin permeation in the reconstructed models and the digestion to AsA and α-tocopherol by the epidermal enzymes, respectively.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;We prepared the 1% of water solution containing either APM or TPNa. Then, we tested the cumulative permeation of the derivatives at 2 application volumes, 25 μL/cm2 (finite dosing) and 85 μL/cm2 (infinite dosing), on cultured reconstructed skin and observed the permeation of the permeants every 2 h up to 24 h.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;When the applied formula was used to assess the evaporation rate to determine an end point of the test system, all the water evaporated in 6 h in finite model and in 8 h in infinite model. Both models showed that the cumulative permeation of the active compounds increased and a constant flux until 8 h after application; however, the flux decreased thereafter, indicating that the decreased flux depended on an end point of the test system. This indicated that our test system can analyze the permeation of the vitamin derivatives within 8 h before reaching the end point.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;Using an infinite model of this system, we assessed the cumulative permeation of vitamin derivatives within 8 h using a reconstructed skin model.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;When vitamin derivatives penetrate the epidermis, they release active compound such as ascorbic acids (AsA) and tocopherols via enzymatic digestion of chemical modifiers. To determine the transdermal penetration of the derivatives, the total permeation of both the derivatives and their active compounds that released from the derivatives should be considered. In this study, we established a skin penetration test method using a cultured, reconstructed skin model with active epidermal enzymes. And we analyzed two vitamin derivatives with different chemical properties: magnesium ascorbyl phosphate (APM) and sodium tocopheryl phosphate (TPNa), both of which has been confirmed their skin permeation in the reconstructed models and the digestion to AsA and α-tocopherol by the epidermal enzymes, respectively.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;We prepared the 1% of water solution containing either APM or TPNa. Then, we tested the cumulative permeation of the derivatives at 2 applicat","PeriodicalId":21748,"journal":{"name":"Skin Pharmacology and Physiology","volume":" ","pages":"109-115"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11797928/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142381622","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}