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Preparation of pectin-tannic acid coated core-shell nanoparticle for enhanced bioavailability and antihyperlipidemic activity of curcumin

Journal 2021 · IF 9.147 · 发表于 2021 年 4 月 27 日
作者: Qihong Zhang,Hui Wang,Zongmiao Feng,Zhaohui Lu,Chen Su,Yunchun Zhao,Jingbo Yu,Alexandr V. Dushkin,Weike Su
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摘要

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 (Na 2 GA) 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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