Innovation Lab., Cosmax R&I Center, 255 Pangyo-ro, Bundang-gu, Seongnam-si, Gyeonggi-do 13486, South Korea.
Department of Chemical Engineering, Soft Matter and Functional Interfaces Laboratory, Pohang University of Science and Technology (POSTECH), Pohang, Gyeongsangbuk-do 37673, South Korea.
ACS Appl Mater Interfaces. 2022 Aug 17;14(32):36331-36340. doi: 10.1021/acsami.2c07135. Epub 2022 Aug 2.
In this work, we utilize skin penetration enhancers (SPEs) such as ceramide and fatty acids in lipid nanovesicles to promote the transdermal delivery of active ingredients. These SPE-incorporated lipid nanovesicles (SPE-LNV) interact with the constituents of skin's outermost stratum corneum (SC) layer, enabling even niacinamide and adenosine with high water solubility to effectively permeate through, leading to enhanced skin efficacy. We demonstrate by both and skin permeation studies that the SPE-LNV formulation containing both ceramide and fatty acids (LNV-CF) exhibits deeper penetration depth and faster permeation rate compared to conventional lipid nanovesicles (LNV) without SPE as well as LNV-C with only ceramide. Moreover, clinical trials were also performed to confirm that LNV-CF most effectively mediates the delivery of niacinamide and adenosine, resulting in a substantial decrease in melanin index as well as skin wrinkle compared to the control groups. We envision that the strategy of incorporating both ceramide and fatty acids in lipid nanovesicles offers a simple and convenient route for the rapid and effective delivery of water-soluble active ingredients across the skin barrier layer.
在这项工作中，我们利用皮肤渗透增强剂（SPE），如神经酰胺和脂肪酸，在脂质纳米囊泡中，以促进活性成分的经皮递送。这些含有 SPE 的脂质纳米囊泡（SPE-LNV）与皮肤最外层角质层（SC）的成分相互作用，使即使具有高水溶性的烟酰胺和腺苷也能有效地渗透，从而提高皮肤功效。我们通过 和 皮肤渗透研究表明，含有神经酰胺和脂肪酸的 SPE-LNV 制剂（LNV-CF）与不含 SPE 的常规脂质纳米囊泡（LNV）以及仅含神经酰胺的 LNV-C 相比，表现出更深的渗透深度和更快的渗透速率。此外，还进行了 临床试验以确认 LNV-CF 最有效地介导烟酰胺和腺苷的递送，与对照组相比，黑色素指数和皮肤皱纹显著减少。我们设想，在脂质纳米囊泡中同时包含神经酰胺和脂肪酸的策略为水溶性活性成分快速有效地穿过皮肤屏障层提供了一种简单方便的途径。
