PDF(Pubmed)
Abstract：
The present study is aimed to design ethosomes and transethosomes for topical administration of quercetin. To overcome quercetin low bioavailability, scarce solubility and poor permeability that hamper its pharmaceutical use, the drug was loaded in ethosomes and transethosomes based on different concentrations of phosphatidylcholine. Vesicle morphology was studied by cryogenic transmission electron microscopy, while size distribution and quercetin entrapment capacity were evaluated up to 3 months, respectively, by photon correlation spectroscopy and high-performance liquid chromatography. The antioxidant property was studied by photochemiluminescence test. Quercetin release and permeation was investigated in vitro, using Franz cells associated to different membranes. In vitro assays were conducted on human keratinocytes and melanoma cells to study the behavior of quercetin-loaded nano-vesicular forms with respect to cell migration and proliferation. The results evidenced that both phosphatidylcholine concentration and quercetin affected the vesicle size. Quercetin entrapment capacity, antioxidant activity and size stability were controlled using transethosomes produced by the highest amount of phosphatidylcholine. In vitro permeation studies revealed an enhancement of quercetin permeation in the case of transethosomes with respect to ethosomes. Notably, scratch wound and migration assays suggested the potential of quercetin loaded-transethosomes as adjuvant strategy for skin conditions.
摘要：
本研究旨在设计用于槲皮素局部给药的醇质体和转囊体。克服槲皮素生物利用度低，溶解度低，渗透性差，阻碍其药物使用，基于不同浓度的磷脂酰胆碱，该药物被装载在醇体和转体中。通过低温透射电子显微镜研究了囊泡形态，而大小分布和槲皮素包封能力的评价长达3个月，分别,光子相关光谱和高效液相色谱。通过光化学发光测试研究了其抗氧化性能。槲皮素的体外释放和渗透研究，使用与不同膜相关的Franz细胞。对人角质形成细胞和黑色素瘤细胞进行体外测定，以研究负载槲皮素的纳米囊泡形式在细胞迁移和增殖方面的行为。结果表明，磷脂酰胆碱浓度和槲皮素都会影响囊泡的大小。槲皮素截留能力,使用最高量的磷脂酰胆碱产生的跨酶体控制抗氧化活性和大小稳定性。体外渗透研究表明，相对于醇质体，在转体的情况下，槲皮素的渗透增强。值得注意的是,划痕伤和迁移试验表明，槲皮素负载的跨酶体作为皮肤疾病的辅助策略的潜力。
