Saeki Yuko, Kato Eiko, Tokudome Yoshihiro
Active Chemical Group, Functional Co-Creation Chemistry Department, Institute for Polymer Technology, Resonac Co., Tokyo, Japan.
Laboratory of Cosmetic Sciences, Graduate School of Science and Engineering/Advanced Health Sciences, Saga University, Saga, Japan.
Skin Pharmacol Physiol. 2024;37(4-6):109-115. doi: 10.1159/000541325. Epub 2024 Oct 4.
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.
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.
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.
Using an infinite model of this system, we assessed the cumulative permeation of vitamin derivatives within 8 h using a reconstructed skin model.
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.
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.
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.
Using an infinite model of this system, we assessed the cumulative permeation of vitamin derivatives within 8 h using a reconstructed skin model.
当维生素衍生物穿透表皮时，它们通过对化学修饰剂的酶促消化释放出活性化合物，如抗坏血酸（AsA）和生育酚。为了确定衍生物的透皮渗透率，应考虑衍生物及其从衍生物中释放的活性化合物的总渗透率。在本研究中，我们建立了一种使用具有活性表皮酶的培养重建皮肤模型的皮肤渗透测试方法。我们分析了两种具有不同化学性质的维生素衍生物：抗坏血酸磷酸镁（APM）和生育酚磷酸钠（TPNa），它们在重建模型中的皮肤渗透性以及表皮酶对AsA和α-生育酚的消化作用均已得到证实。
我们制备了含有APM或TPNa的1%水溶液。然后，我们在培养的重建皮肤上以25 μL/cm²（有限剂量）和85 μL/cm²（无限剂量）这两种施加体积测试了衍生物的累积渗透率，并在长达24小时的时间内每2小时观察一次渗透物的渗透情况。
当使用施加的配方评估蒸发速率以确定测试系统的终点时，有限模型中的所有水分在6小时内蒸发，无限模型中的所有水分在8小时内蒸发。两个模型均显示，活性化合物的累积渗透率在施用后8小时内增加且通量恒定；然而，此后通量下降，这表明通量下降取决于测试系统的终点。这表明我们的测试系统可以在达到终点前8小时内分析维生素衍生物的渗透率。
使用该系统的无限模型，我们使用重建皮肤模型评估了8小时内维生素衍生物的累积渗透率。
当维生素衍生物穿透表皮时，它们通过对化学修饰剂的酶促消化释放出活性化合物，如抗坏血酸（AsA）和生育酚。为了确定衍生物的透皮渗透率，应考虑衍生物及其从衍生物中释放的活性化合物的总渗透率。在本研究中，我们建立了一种使用具有活性表皮酶的培养重建皮肤模型的皮肤渗透测试方法。我们分析了两种具有不同化学性质的维生素衍生物：抗坏血酸磷酸镁（APM）和生育酚磷酸钠（TPNa），它们在重建模型中的皮肤渗透性以及表皮酶对AsA和α-生育酚的消化作用均已得到证实。
我们制备了含有APM或TPNa的1%水溶液。然后，我们在培养的重建皮肤上以25 μL/cm²（有限剂量）和85 μL/cm²（无限剂量）这两种施加体积测试了衍生物的累积渗透率，并在长达24小时的时间内每2小时观察一次渗透物的渗透情况。
当使用施加的配方评估蒸发速率以确定测试系统的终点时，有限模型中的所有水分在6小时内蒸发，无限模型中的所有水分在8小时内蒸发。两个模型均显示，活性化合物的累积渗透率在施用后8小时内增加且通量恒定；然而，此后通量下降，这表明通量下降取决于测试系统的终点。这表明我们的测试系统可以在达到终点前8小时内分析维生素衍生物的渗透率。
使用该系统的无限模型，我们使用重建皮肤模型评估了8小时内维生素衍生物的累积渗透率。
