Nanomedicine (Lond). 2014 Apr;9(4):451-64. doi: 10.2217/NNM.13.102.
To develop a novel nanocarrier with mucoadhesion and enzymatic inhibition for transnasal insulin delivery. METHODS & METHODS: The physicochemical characterization of the nanoparticles included size and morphology, as well as mucoadhesion and enzymatic inhibition. The in vitro release of insulin from the nanoparticles was evaluated in 3 mg/ml glucose medium. The cytocompatibility of the nanoparticles was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The interactions of the nanoparticles with Caco-2 cells and nasal epithelia, and the effect of the nanoparticles on transnasal insulin delivery were estimated.
The nanoparticles were spherical in shape, with an average size of 100 nm, and presented strong enzymatic inhibitory activity and high mucin adsorption ability. The insulinloaded nanoparticles showed the rapid insulin release in 3 mg/ml glucose medium. The nanoparticles were noncytotoxic to Caco-2 cells. Furthermore, the insulin-loaded nanoparticles overcame mucosal barriers and significantly decreased plasma glucose levels.
开发一种具有黏膜黏附性和酶抑制作用的新型纳米载体，用于经鼻胰岛素传递。方法与方法：对纳米颗粒的物理化学性质进行了表征，包括粒径和形态，以及黏膜黏附性和酶抑制作用。在 3 mg/ml 葡萄糖介质中评估了胰岛素从纳米颗粒中的体外释放情况。通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐法评估了纳米颗粒的细胞相容性。评估了纳米颗粒与 Caco-2 细胞和鼻上皮的相互作用，以及纳米颗粒对经鼻胰岛素传递的影响。结果：纳米颗粒呈球形，平均粒径为 100nm，表现出较强的酶抑制活性和高黏蛋白吸附能力。载胰岛素的纳米颗粒在 3mg/ml 葡萄糖介质中表现出快速胰岛素释放。载胰岛素的纳米颗粒对 Caco-2 细胞无细胞毒性。此外，载胰岛素的纳米颗粒克服了黏膜屏障，显著降低了血浆葡萄糖水平。
