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.

中文翻译：

---

醇质体和转质体作为槲皮素的皮肤递送系统：对黑色素瘤细胞的初步研究

本研究旨在设计用于局部给药槲皮素的乙醇体和转乙醇体。为了克服槲皮素生物利用度低、溶解度差、渗透性差等限制其医药用途的问题，根据不同浓度的磷脂酰胆碱，将药物负载于乙醇体和转乙醇体中。通过低温透射电子显微镜研究囊泡形态，同时通过光子相关光谱和高效液相色谱分别评估长达 3 个月的尺寸分布和槲皮素包封能力。通过光化学发光测试研究其抗氧化性能。使用与不同膜相关的 Franz 细胞在体外研究了槲皮素的释放和渗透。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。结果证明磷脂酰胆碱浓度和槲皮素都会影响囊泡大小。使用由最高量的磷脂酰胆碱产生的转酶体来控制槲皮素的包封能力、抗氧化活性和尺寸稳定性。体外渗透研究表明，与乙醇体相比，转乙醇体的槲皮素渗透性增强。值得注意的是，划伤和迁移测定表明负载槲皮素的转酶体作为皮肤状况的辅助策略的潜力。