Chaudhuri R K, Bojanowski K
Sytheon Ltd., 315 Wootton Street, Boonton, NJ, USA.
Sunny BioDiscovery, Inc., 972 East Main St., Zone B Santa Paula, CA, USA.
Int J Cosmet Sci. 2017 Oct;39(5):518-526. doi: 10.1111/ics.12405. Epub 2017 Jul 24.
The study involved the synthesis of a novel derivative of caprylic acid - isosorbide dicaprylate (IDC) - and the evaluation of its potential in improving water homoeostasis and epidermal barrier function in human skin.
The effect of IDC on gene expression was assayed in skin organotypic cultures by DNA microarrays. The results were then confirmed for a few key genes by quantitative PCR, immuno- and cytochemistry. Final validation of skin hydration properties was obtained by four separate clinical studies. Level of hydration was measured by corneometer either by using 2% IDC lotion alone vs placebo or in combination with 2% glycerol lotion vs 2% glycerol only. A direct comparison in skin hydration between 2% IDC and 2% glycerol lotions was also carried out. The epidermal barrier function improvement was assessed by determining changes in transepidermal water loss (TEWL) on the arms before and after treatment with 2% IDC lotion versus placebo.
IDC was found to upregulate the expression of AQP3, CD44 and proteins involved in keratinocyte differentiation as well as the formation and function of stratum corneum. A direct comparison between 2% IDC versus 2% glycerol lotions revealed a three-fold advantage of IDC in providing skin hydration. Severely dry skin treated with 2% IDC in combination with 2% glycerol showed 133% improvement, whereas 35% improvement was observed with moderately dry human skin.
Topical isosorbide dicaprylate favourably modulates genes involved in the maintenance of skin structure and function, resulting in superior clinical outcomes. By improving skin hydration and epidermal permeability barrier, it offers therapeutic applications in skin ageing.
本研究涉及合成一种新型辛酸衍生物——异山梨醇二辛酸酯（IDC），并评估其在改善人体皮肤水稳态和表皮屏障功能方面的潜力。
通过DNA微阵列在皮肤器官型培养物中检测IDC对基因表达的影响。然后通过定量PCR、免疫和细胞化学对一些关键基因的结果进行确认。通过四项独立的临床研究获得皮肤水合特性的最终验证。使用角质层水合测定仪测量水合水平，方法是单独使用2% IDC乳液与安慰剂对比，或与2%甘油乳液联合使用与仅使用2%甘油对比。还对2% IDC和2%甘油乳液的皮肤水合情况进行了直接比较。通过测定2% IDC乳液与安慰剂治疗前后手臂上的经表皮水分流失（TEWL）变化来评估表皮屏障功能的改善情况。
发现IDC可上调水通道蛋白3（AQP3）、CD44的表达以及参与角质形成细胞分化以及角质层形成和功能的蛋白质的表达。2% IDC与2%甘油乳液的直接比较显示，IDC在提供皮肤水合方面具有三倍优势。用2% IDC与2%甘油联合治疗的严重干性皮肤改善了133%，而中度干性人体皮肤改善了35%。
局部应用异山梨醇二辛酸酯可有利地调节参与维持皮肤结构和功能的基因，从而产生更好的临床效果。通过改善皮肤水合和表皮渗透屏障，它在皮肤衰老方面具有治疗应用价值。
