Hsieh Yun-Shan, Chen Yih-Fung, Cheng Yung-Yi, Liu Wan-Yi, Wu Yu-Tse
School of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Pharmaceutics. 2022 Sep 7;14(9):1896. doi: 10.3390/pharmaceutics14091896.
Exposure to ultraviolet B (UVB) leads to the overproduction of reactive oxygen species (ROS), causing higher risks of skin disorders. Luteolin (Lut) is a naturally occurring antioxidant that can absorb a broad range of ultraviolet light, but its water solubility and skin permeability are limited and insufficient. The aim of the current study was to develop a Lut-loaded self-emulsifying phospholipid preconcentrate (LSEPP) for enhancing the solubility, permeability, and photoprotective activity of Lut. The designed formulations were firstly examined for their droplet size, zeta potential, dispersity, and in vitro corneum permeability after dispensing the preconcentrate to form an emulsion; the optimized formulation was further characterized for its emulsified morphology, compatibility with excipients, stability in the preconcentrate form, and photoprotective activity by the HaCaT cell model under the emulsified status. The optimized LSEPP formulation attained a smaller droplet size (140.6 ± 24.2 nm) with the addition of 1,8-cineole and increased the permeability of Lut by 7-fold. As evidenced in the cell model studies, the optimized LSEPP formulation can efficiently deliver Lut into HaCaT cells after emulsification and result in a 115% better cell viability as well as a 203% stronger ROS scavenging capability, compared with those of unformulated Lut after UVB irradiation. To sum up, we have successfully developed an LSEPP formulation, which is a safe and promising topical delivery system for enhancing the photoprotective effects of Lut.
暴露于紫外线B（UVB）会导致活性氧（ROS）的过量产生，从而增加皮肤疾病的风险。木犀草素（Lut）是一种天然存在的抗氧化剂，能够吸收广泛的紫外光，但其水溶性和皮肤渗透性有限且不足。本研究的目的是开发一种负载木犀草素的自乳化磷脂预浓缩物（LSEPP），以提高木犀草素的溶解度、渗透性和光保护活性。首先，在将预浓缩物分散形成乳液后，检测所设计制剂的粒径、ζ电位、分散性和体外角质层渗透性；通过HaCaT细胞模型，进一步对优化后的制剂在乳化状态下的乳化形态、与辅料的相容性、预浓缩物形式的稳定性以及光保护活性进行表征。优化后的LSEPP制剂在添加1,8-桉叶素后粒径更小（140.6±24.2 nm），木犀草素的渗透性提高了7倍。细胞模型研究表明，与UVB照射后未配制的木犀草素相比，优化后的LSEPP制剂在乳化后能够有效地将木犀草素递送至HaCaT细胞中，使细胞活力提高115%，ROS清除能力增强203%。综上所述，我们成功开发了一种LSEPP制剂，它是一种安全且有前景的局部给药系统，可增强木犀草素的光保护作用。
