School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning Province 110016, PR China; School of Chinese Medicine, Faculty of Science, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong 999077, PR China.
J Photochem Photobiol B. 2013 Oct 5;127:8-17. doi: 10.1016/j.jphotobiol.2013.07.014. Epub 2013 Jul 20.
Ultraviolet (UV) radiation has deleterious effects on cells through direct damage to DNA or through increasing generation of reactive oxygen species (ROS). The flavonol quercetin (Qu) provides cellular protection against UV radiation and the current investigation was carried out to develop a deformable liposome formulation of Qu to enhance its delivery into human skin and to improve its anti-UVB effect. The influence of surfactants (including Span 20, Tween 80 and sodium cholate) on the properties of Qu deformable liposomes was investigated. Liposomes composed of Qu, phosphatidylcholine (PC), cholesterol (Chol), and Tween 80 showed high entrapment efficiencies (80.41±4.22%), small particle sizes (132±14nm), high elasticity (10.48±0.71), and prolonged drug release. The cell viability in UVB-irradiated HaCaT cells increased to 89.89±4.5% at 24h and 78.8±3.19% at 48h following treatment with Qu defomable liposomes. The ROS and malondialdehyde (MDA) level were also reduced. The penetration rate was 3.8-fold greater than that of the Qu suspension. Moreover, the edema and inflammation was alleviated by Qu deformable liposomes. These results showed the potential of deformable liposomes to enhance the anti-UVB effects of Qu both in vitro and in vivo.
紫外线(UV)辐射通过直接损伤 DNA 或增加活性氧(ROS)的产生对细胞产生有害影响。类黄酮槲皮素(Qu)为细胞提供了对 UV 辐射的保护,目前的研究旨在开发 Qu 的可变形脂质体制剂,以增强其递送至人体皮肤的能力,并提高其抗 UVB 效果。研究了表面活性剂(包括 Span 20、Tween 80 和胆酸钠)对 Qu 可变形脂质体性质的影响。由 Qu、磷脂酰胆碱(PC)、胆固醇(Chol)和 Tween 80 组成的脂质体表现出高包封效率(80.41±4.22%)、小粒径(132±14nm)、高弹性(10.48±0.71)和延长的药物释放。与 Qu 变形脂质体处理后,UVB 照射的 HaCaT 细胞中的细胞活力在 24 小时时增加到 89.89±4.5%,在 48 小时时增加到 78.8±3.19%。ROS 和丙二醛(MDA)水平也降低了。渗透速率比 Qu 悬浮液高 3.8 倍。此外,Qu 变形脂质体还减轻了水肿和炎症。这些结果表明,可变形脂质体有潜力增强 Qu 在体外和体内的抗 UVB 作用。