Peng Fei, Jin Yu, Wang Kunhua, Wang Xiaojing, Xiao Yaqing, Xu Huaide
College of Food Science and Engineering, Northwest A&F University, Yangling 712100, China.
Food Processing Research Institute, Anhui Engineering Laboratory for Agro-Products Processing, School of Tea and Food Science & Technology, Anhui Agricultural University, Hefei 230036, China.
Foods. 2022 Aug 26;11(17):2589. doi: 10.3390/foods11172589.
Betulinic acid (BA) has anti-inflammatory, antioxidative stress, and antitumor activities, but BA bioavailability is low due to its poor water solubility and short half-life. This study aimed to construct a BA delivery system to improve its utilization in vitro. Glycosylated zein (G-zein) was prepared using the wet heating method, and BA-loaded zein composite nanoparticles were prepared using the antisolvent method. Compared to zein, G-zein had the advantages of higher solubility and lower surface hydrophobicity. The encapsulation efficiency of G-zein@BA reached over 80% when the BA concentration was 1 mg/mL. Compared to zein@BA nanoparticles, G-zein@BA was characterized by smaller droplets, higher encapsulation efficiency, and a more stable morphology. The sustained release and solubility of G-zein@BA nanoparticles were also superior to those of zein@BA. Compared with free BA, the dispersions of zein@BA and G-zein@BA nanoparticles in water increased 2.27- and 2.91-fold, respectively. In addition, zein@BA and G-zein@BA nanoparticles markedly inhibited the proliferation of HepG2 cells. This study provides new insights into the structural properties and antitumor activity of BA composite nanoparticles to aid in the development of zein particles as functional materials to deliver bioactive compounds.
桦木酸（BA）具有抗炎、抗氧化应激和抗肿瘤活性，但由于其水溶性差和半衰期短，BA的生物利用度较低。本研究旨在构建一种BA递送系统，以提高其体外利用率。采用湿热法制备了糖基化玉米醇溶蛋白（G-玉米醇溶蛋白），并采用反溶剂法制备了负载BA的玉米醇溶蛋白复合纳米粒。与玉米醇溶蛋白相比，G-玉米醇溶蛋白具有更高的溶解度和更低的表面疏水性。当BA浓度为1 mg/mL时，G-玉米醇溶蛋白@BA的包封率达到80%以上。与玉米醇溶蛋白@BA纳米粒相比，G-玉米醇溶蛋白@BA的特点是液滴更小、包封率更高、形态更稳定。G-玉米醇溶蛋白@BA纳米粒的缓释性和溶解性也优于玉米醇溶蛋白@BA。与游离BA相比，玉米醇溶蛋白@BA和G-玉米醇溶蛋白@BA纳米粒在水中的分散度分别提高了2.27倍和2.91倍。此外，玉米醇溶蛋白@BA和G-玉米醇溶蛋白@BA纳米粒显著抑制了HepG2细胞的增殖。本研究为BA复合纳米粒的结构特性和抗肿瘤活性提供了新的见解，有助于将玉米醇溶蛋白颗粒开发为递送生物活性化合物的功能材料。
