二氢杨梅素包封在玉米醇溶蛋白-酪蛋白纳米粒中的制备及表征及其在大鼠体内的生物利用度。
Fabrication and characterization of dihydromyricetin encapsulated zein-caseinate nanoparticles and its bioavailability in rat.
机构信息
Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China.
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China.
出版信息
Food Chem. 2020 Nov 15;330:127245. doi: 10.1016/j.foodchem.2020.127245. Epub 2020 Jun 3.
Dihydromyricetin (DMY) encapsulated zein-caseinate nanoparticles (DZP) were fabricated by antisolvent method. The encapsulation and loading efficiency of DMY in DZP were 90.2% and 22.6% as determined by HPLC. DZP is spherical with particle size and ζ potential of 206.4 nm and -29.6 mV, respectively. Physicochemical characterization showed that DMY existed in amorphous form in DZP and its interaction with proteins was found. The fabrication of DZP significantly improved the stability of DMY. Besides, the diffusion rate of DMY in DZP was faster than its suspensions in both simulated gastric and intestinal fluid. The adhesion of DMY in mice gastrointestinal tract was also improved. Besides DMY itself, its methylated metabolites with further sulfation and glucuronide were identified in rat plasma by UPLC-QTOF-MS. UPLC-QqQ-MS/MS quantitative analysis showed that the oral bioavailability of DMY was 1.95 times enhanced. Besides, the concentration of DMY metabolites in plasma were all increased.
二氢杨梅素（DMY）包封的玉米醇溶蛋白-酪蛋白酸钠纳米粒（DZP）通过反溶剂法制备。通过 HPLC 测定，DMY 在 DZP 中的包封率和载药量分别为 90.2%和 22.6%。DZP 呈球形，粒径和 ζ 电位分别为 206.4nm 和-29.6mV。物理化学特性表明，DMY 在 DZP 中呈无定形状态存在，并且发现其与蛋白质相互作用。DZP 的制备显著提高了 DMY 的稳定性。此外，DMY 在 DZP 中的扩散速度快于其在模拟胃液和肠液中的混悬液。DMY 在小鼠胃肠道中的黏附也得到改善。除 DMY 本身外，在大鼠血浆中还通过 UPLC-QTOF-MS 鉴定出其甲基化代谢物进一步硫酸化和葡萄糖醛酸化产物。UPLC-QqQ-MS/MS 定量分析表明，DMY 的口服生物利用度提高了 1.95 倍。此外，血浆中 DMY 代谢物的浓度均升高。
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