Liu Chun, Cheng Fenfen, Yang Xiaoquan
Research and Development Center of Food Proteins, School of Food Science and Engineering, South China University of Technology , Guangzhou 510640, People's Republic of China.
Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, South China University of Technology , Guangzhou 510640, People's Republic of China.
J Agric Food Chem. 2017 Mar 22;65(11):2426-2434. doi: 10.1021/acs.jafc.7b00097. Epub 2017 Mar 8.
Curcumin is a poorly water-soluble drug, and its oral bioavailability is very low. Here, a novel self-assembly nanoparticle delivery carrier has been successfully developed by using soybean Bowman-Birk inhibitor (BBI) to improve the solubility, bioaccessibility, and oral absorption of curcumin. BBI is a unique protein, which can be resistant to the pH range and proteolytic enzymes in the gastrointestinal tract (GIT), bioavailable, and not allergenic. The encapsulation efficiencies (EE) and the loading capacities (LC) of curcumin in the curcumin-loaded BBI nanoparticles (Cur-BBI-NPs, size = 90.09 nm, PDI = 0.103) were 86.17 and 10.31%, respectively. The in vitro bioaccessibility of Cur-BBI-NPs was superior to that of curcumin-loaded sodium caseinate (SC) nanoparticles (Cur-SC-NPs) (as control). Moreover, Cur-BBI-NPs significantly enhanced the bioavailability of curcumin in rats compared with Cur-SC-NPs, and the clathrin-mediated endocytosis pathway probably contributed to the favorable bioavailability of Cur-BBI-NPs, as revealed by the cellular uptake inhibition study.
姜黄素是一种水溶性差的药物，其口服生物利用度非常低。在此，通过使用大豆鲍曼-伯克抑制剂（BBI）成功开发了一种新型自组装纳米颗粒递送载体，以提高姜黄素的溶解度、生物可及性和口服吸收。BBI是一种独特的蛋白质，它能抵抗胃肠道（GIT）中的pH范围和蛋白水解酶，具有生物可利用性且无致敏性。姜黄素负载的BBI纳米颗粒（Cur-BBI-NPs，尺寸 = 90.09 nm，PDI = 0.103）中姜黄素的包封率（EE）和载药量（LC）分别为86.17%和10.31%。Cur-BBI-NPs的体外生物可及性优于姜黄素负载的酪蛋白酸钠（SC）纳米颗粒（Cur-SC-NPs）（作为对照）。此外，与Cur-SC-NPs相比，Cur-BBI-NPs显著提高了姜黄素在大鼠体内的生物利用度，细胞摄取抑制研究表明，网格蛋白介导的内吞途径可能有助于Cur-BBI-NPs具有良好的生物利用度。
