芦丁载米蛋白-酪蛋白酸钠纳米粒的制备及其在大鼠体内的生物利用度研究。
Fabrication of Luteolin Loaded Zein-Caseinate Nanoparticles and its Bioavailability Enhancement in Rats.
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.
Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang, 330045, China.
出版信息
J Pharm Sci. 2023 Dec;112(12):3056-3066. doi: 10.1016/j.xphs.2023.06.010. Epub 2023 Jun 24.
Luteolin loaded zein nanoparticles (Lut-ZNP) were prepared by using sodium caseinate as an electrostatic stabilizer. The formulation of the nanoparticles was optimized. Lut-ZNP were spray-dried, and the physicochemical properties were characterized by SEM, XRD, FT-IR and DSC. Then, the bioavailability of luteolin in rats was determined. Under the formulation of luteolin, zein and sodium caseinate with mass ratio of 1:5:15, the particle size, ζ-potential, encapsulation efficiency and loading efficiency of Lut-ZNP were 171.8 nm, -49.05 mV, 85.85% and 3.15%, respectively. Luteolin existed in the nanoparticles with amorphous form. Lut-ZNP exhibited good redispersibility in water after drying. Compared with free luteolin, the solubility, stability and release of luteolin in Lut-ZNP were greatly improved. Besides, the fecal excretion of luteolin in rats was significantly reduced after oral administration of Lut-ZNP. In addition to native luteolin, its metabolites including sulfate, glucuronidate and methylated glucuronidate were found in rat plasma. Lut-ZNP significantly increased the plasma concentrations of luteolin and its metabolites, and the bioavailability of luteolin was enhanced by 2.92 times.
叶黄素载玉米醇溶蛋白纳米粒（Lut-ZNP）通过使用酪蛋白酸钠作为静电稳定剂来制备。优化了纳米粒的配方。将 Lut-ZNP 进行喷雾干燥，并通过 SEM、XRD、FT-IR 和 DSC 对其物理化学性质进行了表征。然后，测定了叶黄素在大鼠体内的生物利用度。在叶黄素、玉米醇溶蛋白和酪蛋白酸钠的质量比为 1:5:15 的配方下，Lut-ZNP 的粒径、ζ-电位、包封效率和载药量分别为 171.8nm、-49.05mV、85.85%和 3.15%。叶黄素以无定形形式存在于纳米粒中。Lut-ZNP 在干燥后具有良好的再分散性。与游离叶黄素相比，叶黄素在 Lut-ZNP 中的溶解度、稳定性和释放得到了极大的提高。此外，口服 Lut-ZNP 后，大鼠粪便中叶黄素的排泄量明显减少。除了天然叶黄素外，在大鼠血浆中还发现了其代谢物，包括硫酸盐、葡萄糖醛酸苷和甲基葡萄糖醛酸苷。Lut-ZNP 显著增加了叶黄素及其代谢物在血浆中的浓度，并且使叶黄素的生物利用度提高了 2.92 倍。
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