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文章编号： 1672-6987（2024）05-0049-08； DOI： 10.16351/j.1672-6987.2024.05.006
肖海蓉1,2， 吴祥根1*(1.青岛科技大学 化工学院， 山东 青岛 266042; 2.高密市人民医院， 山东 高密 261500)
摘要： 制备基于两亲性甜茶苷的漆黄素载药纳米胶束（Fis/Rub胶束），以提高漆黄素的药代动力学特性和疾病治疗效果。采用薄膜分散法制备Fis/Rub胶束，并对其理化性质进行测定；采用亚铁还原能力实验检测Fis/Rub胶束的抗氧化活性；透析法和高效液相色谱法检测Fis/Rub胶束的体外释放能力；考察Fis/Rub胶束的药代动力学特性和体内抗结肠炎活性。所得Fis/Rub胶束的粒径为（76±12） nm，电位为（-386±043） mV。甜茶苷纳米胶束可有效包封漆黄素；提高漆黄素在水中的溶解度(（1912±084） mg·mL-1)；改善漆黄素的体外释放；增强漆黄素的抗氧化活性。大鼠体内药物动力学结果显示，与漆黄素混悬液相比，Fis/Rub胶束可提高漆黄素的口服生物利用度达55倍。药效学研究表明，口服Fis/Rub胶束可有效改善硫酸葡聚糖盐（DSS）诱导的小鼠溃疡性结肠炎的治疗效果。Fis/Rub这一新型制剂改善了漆黄素水溶性差等不足，具有潜在的进一步开发研究和临床意义。
关键词： 漆黄素； 甜茶苷； 纳米胶束； 药物载体； 溃疡性结肠炎
中图分类号： R 943文献标志码： A
引用格式： 肖海蓉， 吴祥根. 基于甜茶苷的漆黄素载药纳米胶束的制备及其抗结肠炎活性
［J］. 青岛科技大学学报(自然科学版), 2024, 45（5）： 49-56.
XIAO Hairong, WU Xianggen. Preparation of fisetin nanomicelles based on rubusoside and its anti-colitis activity［J］. Journal of Qingdao University of Science and Technology（Natural Science Edition), 2024， 45（5）： 49-56.
Preparation of Fisetin Nanomicelles Based on Rubusoside and
Its Anti-colitis Activity
XIAO Hairong1,2, WU Xianggen1
(1. College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China;
2. Gaomi People′s Hospital, Gaomi 261500, China)
Abstract: To prepare the fisetin nanomicelles on amphiphilic rubusoside (Fis/Rub), to enhance the pharmacokinetics and therapeutic effect of Fis. Fis/Rub nanomicelles were prepared by film dispersion method and to determine their physicochemical properties; The antioxidant activity of Fis/Rub nanomicelles was determined by ferrous reducing capacity experiment; The in vitro release capacity of Fis/Rub micelles was determined by dialysis method and HPLC; To investigate the pharmacokinetic properties and in vivo anti-colitis activity of Fis/Rub micelles. The particle size of Fis/Rub micelles was （76±12） nm, and the potential was （-386±043） mV. The water solubility of Fis in Fis/Rub was （1912±084） mg·mL-1. in vitro release characterization of Fis in Fis/Rub was greatly improved. The antioxidant activity of Fis was also provoked improved. The pharmacokinetic results in rats showed that Fis/Rub micelles increased the oral bioavailability of laccaxanthin by 55 times compared with laccaxanthin suspension. The pharmacokinetic results in rats showed that Fis/Rub micelles increased the oral bioavailability of Fis up to 55 times compared with Fis suspension agent. Pharmacodynamic studies have shown that oral administration of Fis/Rub micelles can effectively improve the therapeutic effect of ulcerative colitis in mice model induced by dextran sodium sulfate (DSS). Fis/Rub has improved the poor water solubility of Fis, which has potential further development and clinical significance.
Key words: fisetin; rubusoside; nanomicelle; drug microcarrier; ulcerative colitis
收稿日期： 2023-11-09
基金项目： 山东省自然科学基金项目（ZR2023MH343）.
作者简介： 肖海蓉（1991—），女，硕士研究生.*通信联系人.
