Department of Chemical and Geological Sciences, University of Cagliari, s.s 554 bivio Sestu, Monserrato, I-09042, Italy; CSGI, Consorzio Interuniversitario per lo Sviluppo dei Sistemi a Grande Interfase, via della Lastruccia 3 Sesto Fiorentino, Florence, I-50019, Italy; Division of Physical Chemistry, Department of Chemistry, Lund University, P.O. Box 124, Lund, SE-221 00, Sweden.
Department of Life and Environmental Sciences, University of Cagliari, via Ospedale 72, Cagliari, I-09124, Italy.
Colloids Surf B Biointerfaces. 2021 Mar;199:111564. doi: 10.1016/j.colsurfb.2021.111564. Epub 2021 Jan 6.
The delivery of bio-active molecules through the skin is challenging given the complex structure of its outer layer, the stratum corneum. Here we explore the possibility to encapsulate natural compounds into nanocarriers containing permeation enhancers that can affect the fluidity of the stratum corneum lipids. This approach is expected to facilitate dermal or transdermal release. For this purpose, the application of bile salts, which are natural surfactants involved in vivo in lipid digestion, was exploited. Bile salts were added to lipid liquid crystalline nanoparticles (NPs) made of monoolein for antioxidant topical delivery. Monoolein self-assembly behaviour in water was affected by the presence of bile salts molecules, giving a transition from a bicontinuous cubic to unilamellar vesicles dispersion. By adding oleic acid (OA), the change of curvature in the system led to a reverse hexagonal phase. The morphology, structure and size of the nanocarriers was investigated before the nanoparticles were loaded with catechin, a natural antioxidant occurring in plants and food. The encapsulation did not affect significantly the formulation phase behaviour. The formulation loaded with bile salts and catechin was thereafter tested in vitro on the skin from new-born pig. The results for two different lipid formulations without bile salts were compared under the same experimental conditions and with the same antioxidant. The formulation with bile salts showed the best performance, allowing a superior permeation of catechin in the different skin layers in comparison with formulations without bile salt.
鉴于其外层（角质层）的复杂结构，生物活性分子通过皮肤的传递具有挑战性。在这里，我们探索了将天然化合物封装到纳米载体中的可能性，这些纳米载体包含能够影响角质层脂质流动性的渗透增强剂。这种方法有望促进皮肤或经皮释放。为此，我们利用了胆汁盐，它是体内参与脂质消化的天然表面活性剂。将胆汁盐添加到由单油酸甘油酯制成的用于抗氧化剂局部递送的类脂液晶纳米颗粒（NPs）中。胆汁盐的存在影响了单油酸甘油酯在水中的自组装行为，导致从双连续立方相到单层囊泡分散相的转变。通过添加油酸（OA），体系曲率的变化导致形成反向六方相。在将儿茶素（一种存在于植物和食物中的天然抗氧化剂）负载到纳米颗粒之前，研究了纳米载体的形态、结构和大小。包封对制剂相行为没有显著影响。此后，在新生猪的皮肤上对载有胆汁盐和儿茶素的制剂进行了体外测试。在相同的实验条件下，用相同的抗氧化剂比较了不含胆汁盐的两种不同脂质制剂的结果。含有胆汁盐的制剂表现出最佳的性能，与不含胆汁盐的制剂相比，允许儿茶素在不同的皮肤层中更好地渗透。
