Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA.
Int J Pharm. 2013 Jan 30;441(1-2):56-66. doi: 10.1016/j.ijpharm.2012.12.013. Epub 2012 Dec 20.
The presence of large amounts of reactive oxygen species (ROS) leads to oxidative stress that can damage cell membranes, lead to DNA breakage and cause inactivation of free radical scavenger enzymes, eventually resulting in skin damage. Quercetin is a natural flavonoid that has been shown to have the highest anti-radical activity, along with the ability to act as a scavenger of free radicals and an inhibitor of lipid peroxidation. In this research work, a solvent-free solid lipid based nanosystem has been developed and evaluated for topical delivery of quercetin. Systematic screening of the formulation and process parameters led to the development of a solid lipid (glyceryl dibehenate) based nanosystem using a probe ultrasonication method. The selected variant demonstrated good physical stability for up to 8 weeks at 2-8 °C. Transmission electron microscopy (TEM) images showed spherical particles in the nanometer range. In vitro release studies showed biphasic release of quercetin from the SLN formulation, with an initial burst release followed by prolonged release for up to 24h. In vitro permeation studies using full thickness human skin showed higher amounts of quercetin to be localized within the skin compared to a control formulation with particles in the micrometer range. Such accumulation of quercetin in the skin is highly desirable since the efficacy of quercetin in delaying ultra-violet radiation mediated cell damage and eventual necrosis mainly occurs in the epidermis.
大量活性氧(ROS)的存在会导致氧化应激,从而破坏细胞膜,导致 DNA 断裂,并使自由基清除酶失活,最终导致皮肤损伤。槲皮素是一种天然类黄酮,具有最高的自由基清除活性,能够作为自由基清除剂和脂质过氧化抑制剂发挥作用。在这项研究工作中,开发并评估了一种无溶剂的基于固体脂质的纳米系统,用于透皮递送槲皮素。通过系统筛选配方和工艺参数,采用探针超声法开发了一种基于固体脂质(二硬脂酰基甘油)的纳米系统。选择的变体在 2-8°C 下长达 8 周表现出良好的物理稳定性。透射电子显微镜(TEM)图像显示纳米级的球形颗粒。体外释放研究表明,SLN 制剂中槲皮素呈两相释放,初始突释后持续释放长达 24 小时。使用全厚人体皮肤进行的体外渗透研究表明,与微米级颗粒的对照制剂相比,更多的槲皮素定位于皮肤内。由于槲皮素在延迟紫外线辐射介导的细胞损伤和最终坏死方面的功效主要发生在表皮中,因此将槲皮素在皮肤中的这种积累是非常理想的。