School of Life Science, South China Normal University, Guangzhou 510631, China.
MOE Key Laboratory of Laser Life Science & Institute of Laser Life Science, College of Biophotonics, South China Normal University, Guangzhou, China.
Nanomedicine. 2018 Feb;14(2):353-364. doi: 10.1016/j.nano.2017.11.012. Epub 2017 Nov 21.
Although nanoparticles carriers for oral delivery of insulin have been researched for many years, this method still fails to solve issues with toxicity, biocompatibility, and degradability in the organism. We therefore developed an innovative conjugation system to solve this problem. Nano hydroxyapatite (HAP) particles were used as the core, then polyethylene glycol (PEG) was wrapped onto the surface of hydroxyapatite, and, finally, insulin (INS) and gallic acid (GA) were conjugated with PEG. PEG functionalized HAP was increased the hydrophilicity of the nanoparticles, also protected them from degradation in the gastrointestinal (GI) tract. Most importantly, the in vivo absorption of nanoparticles in rat small intestines revealed that HAP-PEG-GA-INS was absorbed by the small intestine epithelium. The blood glucose of the type 1 diabetes (T1D) rats that were given intragastrically HAP-PEG-GA-INS showed an obvious downward trend. Overall, we synthesized a safe, non-toxic, and effective oral insulin delivery system.
尽管纳米载体用于胰岛素的口服递送已经研究了很多年，但这种方法仍然无法解决在生物体中的毒性、生物相容性和可降解性问题。因此，我们开发了一种创新的结合系统来解决这个问题。纳米羟基磷灰石（HAP）颗粒被用作核心，然后将聚乙二醇（PEG）包裹在羟基磷灰石的表面，最后将胰岛素（INS）和没食子酸（GA）与 PEG 结合。PEG 功能化的 HAP 增加了纳米粒子的亲水性，还保护它们免受胃肠道（GI）道的降解。最重要的是，在大鼠小肠中体内吸收纳米粒子的研究表明，HAP-PEG-GA-INS 被小肠上皮吸收。给予 HAP-PEG-GA-INS 灌胃的 1 型糖尿病（T1D）大鼠的血糖明显下降。总的来说，我们合成了一种安全、无毒、有效的口服胰岛素递送系统。
