NANO-VAC Research Group, Department of Chemistry and Pharmaceutical Technology, School of Pharmacy and Nutrition, University of Navarra, 31008 Pamplona, Spain.
Center for Nutrition Research, School of Pharmacy and Nutrition, University of Navarra, 31008 Pamplona, Spain.
Int J Pharm. 2023 Aug 25;643:123216. doi: 10.1016/j.ijpharm.2023.123216. Epub 2023 Jul 8.
In this study, the ability of zein nanospheres (NS) and zein nanocapsules containing wheat germ oil (NC) to enhance the bioavailability and efficacy of quercetin was evaluated. Both types of nanocarriers had similar physico-chemical properties, including size (between 230 and 250 nm), spherical shape, negative zeta potential, and surface hydrophobicity. However, NS displayed a higher ability than NC to interact with the intestinal epithelium, as evidenced by an oral biodistribution study in rats. Moreover, both types of nanocarriers offered similar loading efficiencies and release profiles in simulated fluids. In C. elegans, the encapsulation of quercetin in nanospheres (Q-NS) was found to be two twice more effective than the free form of quercetin in reducing lipid accumulation. For nanocapsules, the presence of wheat germ oil significantly increased the storage of lipids in C. elegans; although the incorporation of quercetin (Q-NC) significantly counteracted the presence of the oil. Finally, nanoparticles improved the oral absorption of quercetin in Wistar rats, offering a relative oral bioavailability of 26% and 57% for Q-NS and Q-NC, respectively, compared to a 5% for the control formulation. Overall, the study suggests that zein nanocarriers, particularly nanospheres, could be useful in improving the bioavailability and efficacy of quercetin.
在这项研究中,评估了玉米醇溶蛋白纳米球(NS)和含小麦胚芽油的玉米醇溶蛋白纳米胶囊(NC)增强槲皮素生物利用度和疗效的能力。这两种纳米载体具有相似的物理化学性质,包括大小(230 至 250nm 之间)、球形、负 zeta 电位和表面疏水性。然而,与 NC 相比,NS 与肠道上皮的相互作用能力更高,这可以通过大鼠口服生物分布研究得到证明。此外,在模拟流体中,这两种纳米载体都具有相似的载药量和释放曲线。在秀丽隐杆线虫中,发现将槲皮素包封在纳米球中(Q-NS)比游离形式的槲皮素更有效地减少脂质积累,效果高出两倍。对于纳米胶囊,小麦胚芽油的存在显著增加了秀丽隐杆线虫中脂质的储存;尽管添加了槲皮素(Q-NC),但显著抵消了油的存在。最后,纳米颗粒提高了 Wistar 大鼠中槲皮素的口服吸收,与对照制剂相比,Q-NS 和 Q-NC 的相对口服生物利用度分别为 26%和 57%,而对照制剂为 5%。总的来说,该研究表明,玉米醇溶蛋白纳米载体,特别是纳米球,可用于提高槲皮素的生物利用度和疗效。