果胶-单宁酸包被核壳纳米颗粒的制备提高姜黄素的生物利用度和抗高脂血症活性

IF 11 1区 农林科学 Q1 CHEMISTRY, APPLIED Food Hydrocolloids Pub Date : 2021-10-01 DOI:10.1016/j.foodhyd.2021.106858
Qihong Zhang , Hui Wang , Zongmiao Feng , Zhaohui Lu , Chen Su , Yunchun Zhao , Jingbo Yu , Alexandr V. Dushkin , Weike Su
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引用次数: 20

摘要

姜黄素是一种功能性多酚类化合物,其溶解度和生物利用度较低,限制了其应用。本研究以甘草酸二钠(Na2GA)自组装的姜黄素胶束为材料,用果胶和单宁酸包被构筑核-壳固体分散体(SD-CUR)。通过分子动力学模拟阐明了核壳纳米颗粒的组装机理。SD-CUR在模拟胃液和肠液中的溶解度和体外释放特性得到改善。平行人工膜通透性(PAMPA)试验证实,与纯姜黄素相比,SD-CUR中姜黄素的通透性明显提高。药代动力学研究表明,生物利用度提高了10倍。肠道原位吸收研究证实SD-CUR可促进药物在肠上皮细胞间的转运。进一步的降血脂研究表明,SD-CUR给药组可以显著降低高脂血症大鼠的总胆固醇(TC)、甘油三酯(TG)和低密度脂蛋白(LDL)水平。这些发现证实了SD-CUR在防治高脂血症方面具有广阔的应用前景。
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Preparation of pectin-tannic acid coated core-shell nanoparticle for enhanced bioavailability and antihyperlipidemic activity of curcumin

As a functional polyphenolic compound, curcumin (CUR) has limited application due to its low solubility and bioavailability. In this work, curcumin loaded micelles self-assembled from disodium glycyrrhizin (Na2GA) was coated with pectin and tannic acid to construct a core-shell solid dispersion (SD-CUR). The assembly mechanism of the core-shell nanoparticle was clarified by molecular dynamics simulation. Improved solubility and in vitro release characteristics of SD-CUR in simulated gastric and intestinal juice were achieved. The parallel artificial membrane permeability (PAMPA) test confirmed that the permeability of curcumin in SD-CUR was significantly improved compared with the pure curcumin. Pharmacokinetic studies showed that the bioavailability was increased by 10 times. Intestinal in situ absorption study proved SD-CUR could enhance drug to transport across intestinal epithelial cells. Further hypolipidemic study demonstrated that the SD-CUR medication group could considerably reduce the levels of total cholesterol (TC), triglyceride (TG), and low density lipoprotein (LDL) in hyperlipidemia rats. These findings confirmed that SD-CUR had broad application prospects in the prevention and treatment of hyperlipidemia.

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来源期刊
Food Hydrocolloids
Food Hydrocolloids 工程技术-食品科技
CiteScore
19.90
自引率
14.00%
发文量
871
审稿时长
37 days
期刊介绍: Food Hydrocolloids publishes original and innovative research focused on the characterization, functional properties, and applications of hydrocolloid materials used in food products. These hydrocolloids, defined as polysaccharides and proteins of commercial importance, are added to control aspects such as texture, stability, rheology, and sensory properties. The research's primary emphasis should be on the hydrocolloids themselves, with thorough descriptions of their source, nature, and physicochemical characteristics. Manuscripts are expected to clearly outline specific aims and objectives, include a fundamental discussion of research findings at the molecular level, and address the significance of the results. Studies on hydrocolloids in complex formulations should concentrate on their overall properties and mechanisms of action, while simple formulation development studies may not be considered for publication. The main areas of interest are: -Chemical and physicochemical characterisation Thermal properties including glass transitions and conformational changes- Rheological properties including viscosity, viscoelastic properties and gelation behaviour- The influence on organoleptic properties- Interfacial properties including stabilisation of dispersions, emulsions and foams- Film forming properties with application to edible films and active packaging- Encapsulation and controlled release of active compounds- The influence on health including their role as dietary fibre- Manipulation of hydrocolloid structure and functionality through chemical, biochemical and physical processes- New hydrocolloids and hydrocolloid sources of commercial potential. The Journal also publishes Review articles that provide an overview of the latest developments in topics of specific interest to researchers in this field of activity.
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