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采用脂质体介导的结肠靶向递药系统增强姜黄素治疗溃疡性结肠炎的稳定性和抗炎性能。

Enhancing stability and anti-inflammatory properties of curcumin in ulcerative colitis therapy using liposomes mediated colon-specific drug delivery system.

机构信息

Key Laboratory of Food Processing Technology and Quality Control in Shandong Province, College of Food Science and Engineering, Shandong Agricultural University, Tai'an, Shandong Province, 271018, PR China.

Department of Molecular Biosciences and Bioengineering, University of Hawaii at 10Manoa, Honolulu, HI, 96822, USA.

出版信息

Food Chem Toxicol. 2021 May;151:112123. doi: 10.1016/j.fct.2021.112123. Epub 2021 Mar 18.

Abstract

Curcumin liposomes (CUR-LPs) was identified by evaluating morphology, appearance, zeta potential, particle diameter, and drug encapsulation efficiency. The results indicated that particle diameter, surface charge and polydispersity index (PDI) of curcumin (CUR)-loaded anionic liposomes were 167 nm, -34 mV and 0.09, respectively. CUR-LPs is high stable pseudo-pH-sensitive nanoparticles system which has a favorable stability in simulated gastric fluid and slower degradation rate allowing CUR sustained release for prolonged times in simulated intestinal fluid. Within 1 h, the CUR consumption was 21.82% in simulated gastric fluid (SGF) and 27.32% in simulated intestinal fluid (SIF), respectively. CUR-LPs could attenuate clinical symptoms including weight loss, diarrhea and fecal bleeding. Especially, it could also prevent dextran sulfate sodium salt (DSS)-inducedcolon tissue damage and colon shortening, and reduce the production of malondialdehyde (MDA), colonic myeloperoxidase (MPO), Interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in animal model. Our study illustrated that liposomes (LPs) was a potential carrier to develop the colon-specific drug delivery system incorporating CUR for treating ulcerative colitis.

摘要

通过评估形态、外观、Zeta 电位、粒径和药物包封效率,确定姜黄素脂质体(CUR-LPs)。结果表明,载姜黄素(CUR)的阴离子脂质体的粒径、表面电荷和多分散指数(PDI)分别为 167nm、-34mV 和 0.09。CUR-LPs 是一种高稳定性的假 pH 敏感纳米粒子系统,在模拟胃液中具有良好的稳定性,在模拟肠液中的降解速度较慢,允许 CUR 长时间持续释放。在 1h 内,模拟胃液(SGF)中 CUR 的消耗率为 21.82%,模拟肠液(SIF)中 CUR 的消耗率为 27.32%。CUR-LPs 可减轻临床症状,包括体重减轻、腹泻和粪便出血。特别是,它还可以预防葡聚糖硫酸钠(DSS)诱导的结肠组织损伤和结肠缩短,并减少动物模型中丙二醛(MDA)、结肠髓过氧化物酶(MPO)、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)的产生。我们的研究表明,脂质体(LPs)是一种有潜力的载体,可以开发用于治疗溃疡性结肠炎的结肠特异性药物传递系统,该系统将 CUR 作为药物载体。

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