Abstract

Quercetin, a substance from nature has various biological effects; while, some challenges like low solubility in water and absorption, and high first-pass metabolism hindered its clinical efficiencies. So, various strategies using novel nanocarriers have been designed to overcome these obstacles. This study aimed to fabricate the polymeric niosomes by incorporating hyaluronic acid to deliver quercetin. After preparation, quercetin entrapped niosomes were investigated in terms of size, zeta potential, quercetin entrapment, CTAB turbidimetric assay, AFM, TEM, differential scanning Calorimetry, X-Ray diffraction, DPPH antioxidant determination, and in vivo anti-inflammatory analysis. The analysis of the results exhibited that size of niosomes containing quercetin and hyaluronic acid was 231.07 ± 8.39 nm with a zeta potential of −34.00 ± 0.95 mV. Moreover, quercetin entrapment efficiency and loading were 94.67 ± 1.62% and 1.65 ± 0.37%, respectively. TEM and AFM showed that polymeric niosomes were spheres. The release data presented that the Higuchi model was the best-fitted model. DPPH antioxidant determination displayed that 80 µl of polymeric niosomes with 7.46 × 10⁻⁸mol of quercetin had a remarkable antioxidant potency. According to the in vivo oedema evaluation, the potency of polymeric formulations was superior to the simple suspension of quercetin to control inflammation in rats by oral administration.

摘要

槲皮素，一种来自自然界的物质，具有多种生物效应；同时，在水中溶解度和吸收率低以及首过代谢高等挑战阻碍了其临床效率。因此，已经设计了使用新型纳米载体的各种策略来克服这些障碍。本研究旨在通过掺入透明质酸来递送槲皮素来制造聚合 niosomes。制备后，在大小、zeta 电位、槲皮素包埋、CTAB 比浊法、AFM、TEM、差示扫描量热法、X 射线衍射、DPPH 抗氧化剂测定和体内研究方面对槲皮素包埋的 niosomes 进行了研究抗炎分析。结果分析表明，含有槲皮素和透明质酸的niosomes大小为231.07±8.39nm，zeta电位为-34.00±0.95mV。此外，槲皮素的包封率和载量分别为 94.67 ± 1.62% 和 1.65 ± 0.37%。TEM 和 AFM 表明聚合 niosomes 是球体。发布数据表明 Higuchi 模型是最适合的模型。DPPH 抗氧化测定表明，80 µl 含有 7.46 × 10 ^-8 mol 槲皮素的聚合 niosomes 具有显着的抗氧化效力。根据体内水肿评估，通过口服给药，聚合物制剂在控制大鼠炎症方面的效力优于槲皮素的简单混悬液。