Department of Pharmaceutics, Faculty of Pharmacy, Alborz University of Medical Sciences, Karaj, Iran.
Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
J Drug Target. 2021 Feb;29(2):225-234. doi: 10.1080/1061186X.2020.1830408. Epub 2020 Oct 12.
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 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 × 10mol of quercetin had a remarkable antioxidant potency. According to the oedema evaluation, the potency of polymeric formulations was superior to the simple suspension of quercetin to control inflammation in rats by oral administration.
槲皮素是一种天然物质,具有多种生物学效应;然而,一些挑战,如低水溶性和吸收性,以及高首过代谢,阻碍了其临床疗效。因此,已经设计了各种使用新型纳米载体的策略来克服这些障碍。本研究旨在通过加入透明质酸来制备聚合物胶束来递送槲皮素。在制备后,对载有槲皮素的胶束进行了考察,包括粒径、Zeta 电位、槲皮素包封率、CTAB 浊度测定、原子力显微镜、透射电子显微镜、差示扫描量热法、X 射线衍射、DPPH 抗氧化测定和抗炎分析。结果分析表明,含有槲皮素和透明质酸的胶束的粒径为 231.07±8.39nm,Zeta 电位为-34.00±0.95mV。此外,槲皮素包封效率和载药量分别为 94.67±1.62%和 1.65±0.37%。TEM 和 AFM 显示聚合物胶束为球体。释放数据表明,Higuchi 模型是最佳拟合模型。DPPH 抗氧化测定显示,80µl 载有 7.46×10mol 槲皮素的聚合物胶束具有显著的抗氧化能力。根据水肿评估,聚合物制剂的功效优于简单的槲皮素混悬液,通过口服给药控制大鼠炎症。