Innovation Lab., Cosmax R&I Center, 255 Pangyo-ro, Bundang-gu, Seongnam 13486, Republic of Korea.
School of Chemical Engineering, Sungkyunkwan University, 2066 Seobu-ro, Jangan-gu, Suwon 16419, Republic of Korea.
Int J Pharm. 2020 Apr 15;579:119162. doi: 10.1016/j.ijpharm.2020.119162. Epub 2020 Feb 17.
Herein, we report on a ceramide-coassembled lipid nanovehicle (CLNV) system that can enhance the penetration of active ingredients through the skin barrier by taking advantage of molecular associations between ceramide and lipids in the stratum corneum (SC) layer. For this purpose, we fabricated CLNVs consisting of an asymmetric lipid and a cholesterol derivative. They showed excellent long-term dispersion stability without molecular crystallization of ceramide. Upon forming a stable aqueous dispersion, the CLNVs retained their initial vehicle structure even under harsh conditions including high storage temperatures or salinity conditions. From in vitro skin barrier recovery tests, we observed that topical treatment with CLNVs induced the SC to restore its lamellar structure to the same condition as that prior to chemical damage. An in vivo skin penetration study additionally confirmed that skin penetration was enhanced, since the CLNVs were able to effectively interact with the SC layer. From these results, the CLNVs with robust molecular layer endow various applications in wide range applications including transdermal pharmaceutics delivery systems and cosmetics field.
在此,我们报告了一种神经酰胺组装脂质纳米载体(CLNV)系统,该系统可以利用角质层(SC)层中神经酰胺和脂质之间的分子缔合,增强活性成分通过皮肤屏障的渗透。为此,我们制备了由不对称脂质和胆固醇衍生物组成的 CLNV。它们表现出优异的长期分散稳定性,而没有神经酰胺的分子结晶。在形成稳定的水相分散体后,即使在包括高储存温度或盐度条件在内的苛刻条件下,CLNV 仍保持其初始载体结构。从体外皮肤屏障恢复测试中,我们观察到,CLNV 的局部治疗诱导 SC 恢复其层状结构,使其与化学损伤之前的条件相同。体内皮肤渗透研究进一步证实,由于 CLNV 能够与 SC 层有效相互作用,因此皮肤渗透得到增强。从这些结果来看,具有稳健分子层的 CLNV 具有广泛的应用,包括透皮给药系统和化妆品领域。