Deng Wenji, Wang Huan, Wu Baojian, Zhang Xingwang
Department of Pharmaceutics, College of Pharmacy, Jinan University, Guangzhou 510632, China.
Acta Pharm Sin B. 2019 Jan;9(1):74-86. doi: 10.1016/j.apsb.2018.09.009. Epub 2018 Sep 20.
Diabetes mellitus (DM) remains a great challenge in treatment due to pathological complexity. It has been proven that phytomedicines and natural medicines have prominent antidiabetic effects. This work aimed to develop selenium-layered nanoparticles (SeNPs) for oral delivery of mulberry leaf and extracts (MPE), a group of phytomedicines with significant hypoglycemic activities, to achieve a synergic antidiabetic effect. MPE-loaded SeNPs (MPE-SeNPs) were prepared through a solvent diffusion/ reduction technique and characterized by particle size, potential, morphology, entrapment efficiency (EE) and drug loading (DL). The resulting MPE-SeNPs were 120 nm around in particle size with EE of 89.38% for rutin and 90.59% for puerarin, two marker components in MPE. MPE-SeNPs exhibited a slow drug release and good physiological stability in the simulated digestive fluid. After oral administration, MPE-SeNPs produced significant hypoglycemic effects both in the normal and diabetic rats. intestinal imaging and cellular examinations demonstrated that MPE-SeNPs were provided with outstanding intestinal permeability and transepithelial transport aptness. It was also revealed that MPE-SeNPs could alleviate the oxidative stress, improve the pancreatic function, and promote the glucose utilization by adipocytes. Our study provides new insight into the use of integrative nanomedicine containing phytomedicines and selenium for DM treatment.
由于病理复杂性,糖尿病(DM)在治疗方面仍然是一个巨大的挑战。已证明植物药和天然药物具有显著的抗糖尿病作用。这项工作旨在开发用于口服递送桑叶及其提取物(MPE)的硒层纳米颗粒(SeNPs),MPE是一组具有显著降血糖活性的植物药,以实现协同抗糖尿病效果。通过溶剂扩散/还原技术制备了负载MPE的SeNPs(MPE-SeNPs),并通过粒径、电位、形态、包封率(EE)和载药量(DL)对其进行了表征。所得的MPE-SeNPs粒径约为120nm,MPE中的两种标志性成分芦丁和葛根素的包封率分别为89.38%和90.59%。MPE-SeNPs在模拟消化液中表现出缓慢的药物释放和良好的生理稳定性。口服给药后,MPE-SeNPs在正常大鼠和糖尿病大鼠中均产生了显著的降血糖作用。肠道成像和细胞检查表明,MPE-SeNPs具有出色的肠道通透性和跨上皮转运能力。还发现MPE-SeNPs可以减轻氧化应激,改善胰腺功能,并促进脂肪细胞对葡萄糖的利用。我们的研究为使用含有植物药和硒的整合纳米药物治疗糖尿病提供了新的见解。