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环阿屯醇包封于磷脂囊泡中增强了其在皮肤屏障中的透皮传递和递送。

Encapsulation of cycloastragenol in phospholipid vesicles enhances transport and delivery across the skin barrier.

机构信息

Department of Food Science, University of Guelph, 50 Stone Road East, Guelph, ON N1G 2W1, Canada; Avaria Solutions Inc., 5-650 Jamieson Parkway, Cambridge, ON N3C 0A5, Canada.

Avaria Solutions Inc., 5-650 Jamieson Parkway, Cambridge, ON N3C 0A5, Canada.

出版信息

J Colloid Interface Sci. 2022 Feb 15;608(Pt 2):1222-1228. doi: 10.1016/j.jcis.2021.10.143. Epub 2021 Oct 28.

DOI:10.1016/j.jcis.2021.10.143
PMID:34735856
Abstract

Cycloastragenol (CA) is a plant saponin that functions as a telomerase activator, and it has been made as an oral anti-aging supplement and use as active ingredient in topical cosmetic products. The anti-aging performance in cosmetic products have only been evaluated by description of skin appearance, while direct topical penetration of CA across the skin barrier still needs to be confirmed. The objective of this work was to design encapsulation vehicles to deliver CA across the skin barrier using commercially available ingredients through scalable processes, and to prove its topical penetration. Phospholipid vesicles including liposomes, ethosomes, and transethosomes were prepared using soy and sunflower phospholipids and different penetration enhancers, including ethanol and surfactants. The loading capacity of CA was analyzed using high performance liquid chromatography, and the topical penetration of CA was evaluated using Franz diffusion cells with pig skin. Transethosomes using Tween 80, Span 40, or dicetylphosphate as the penetration enhancer showed better CA delivery across the skin barrier than ethosomes or emulsifier α-gels. Results of this work provide evidence that CA encapsulated in phospholipid vesicles can be transported across the skin barrier. These encapsulation systems could be used for the design of CA-containing anti-aging cosmetic products.

摘要

环黄芪醇 (CA) 是一种植物皂素,具有端粒酶激活作用,已被制成口服抗衰老补充剂,并用作局部美容产品的活性成分。美容产品的抗衰老性能仅通过描述皮肤外观进行评估,而 CA 直接通过皮肤屏障的局部渗透仍需得到证实。本工作的目的是设计封装载体,使用市售成分通过可扩展的工艺将 CA 递送至皮肤屏障,并证明其具有局部渗透作用。使用大豆和葵花磷脂以及不同的渗透增强剂,包括乙醇和表面活性剂,制备了包括脂质体、醇质体和转醇质体在内的磷脂囊泡。使用高效液相色谱法分析 CA 的载药量,并使用Franz 扩散细胞评估 CA 在猪皮上的透皮渗透情况。以吐温 80、司盘 40 或二硬脂酰基磷脂酰胆碱作为渗透增强剂的转醇质体比醇质体或乳化剂 α-凝胶显示出更好的 CA 跨皮肤屏障传递能力。这项工作的结果提供了证据表明 CA 被包裹在磷脂囊泡中可以被运送到皮肤屏障中。这些封装系统可用于设计含有 CA 的抗衰老美容产品。

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