Subongkot Thirapit, Ngawhirunpat Tanasait, Opanasopit Praneet
Pharmaceutical Innovations of Natural Products Unit (PhInNat), Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi 20131, Thailand.
Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Pharmaceutics. 2021 Mar 18;13(3):404. doi: 10.3390/pharmaceutics13030404.
This study aimed to develop ultradeformable liposomes (ULs) with fatty acids, namely, oleic, linoleic, and linolenic acid, to improve the skin penetration of rosmarinic acid. This study also investigated the vesicle-skin interaction and skin penetration pathway of ULs with fatty acids using the co-localization technique of multifluorescently labeled particles. The prepared ULs were characterized in terms of size, surface charge, size distribution, shape, % entrapment efficiency (% EE), and % loading efficiency (% LE). The prepared ULs with fatty acids had an average particle size between 50.37 ± 0.3 and 59.82 ± 17.3 nm with a size distribution within an acceptable range and exhibited a negative surface charge. The average % EE and % LE were 9 and 24.02, respectively. The in vitro skin penetration study found that ULs with oleic acid could significantly increase the skin penetration of rosmarinic acid compared to ULs. According to confocal laser scanning microscopy observations, this study suggested that UL vesicles attach to the skin before releasing the entrapped drug to penetrate the skin. These findings suggested that ULs with oleic acid penetrated the skin via the transfollicular pathway as a major penetration pathway.
本研究旨在开发含有脂肪酸（即油酸、亚油酸和亚麻酸）的超变形脂质体（ULs），以提高迷迭香酸的皮肤渗透性。本研究还使用多荧光标记颗粒的共定位技术研究了含脂肪酸的ULs与皮肤的相互作用以及皮肤渗透途径。对制备的ULs进行了粒径、表面电荷、粒径分布、形状、包封率（%EE）和载药率（%LE）等方面的表征。制备的含脂肪酸的ULs平均粒径在50.37±0.3至59.82±17.3nm之间，粒径分布在可接受范围内，且表面带负电荷。平均%EE和%LE分别为9和24.02。体外皮肤渗透研究发现，与不含脂肪酸的ULs相比，含油酸的ULs可显著提高迷迭香酸的皮肤渗透性。根据共聚焦激光扫描显微镜观察结果，本研究表明UL囊泡在释放包封药物以渗透皮肤之前先附着于皮肤。这些发现表明，含油酸的ULs通过毛囊途径作为主要渗透途径穿透皮肤。
