Xu Bin, Jiang Guohua, Yu Weijiang, Liu Depeng, Liu Yongkun, Kong Xiangdong, Yao Juming
Department of Materials Engineering, Zhejiang Sci Tech University, Hangzhou 310018, China.
Department of Materials Engineering, Zhejiang Sci Tech University, Hangzhou 310018, China; National Engineering Laboratory for Textile Fiber Materials and Processing Technology (Zhejiang), Hangzhou 310018, China; Key Laboratory of Advanced Textile Materials and Manufacturing Technology (ATMT), Ministry of Education, Hangzhou 310018, China.
Mater Sci Eng C Mater Biol Appl. 2017 Sep 1;78:420-428. doi: 10.1016/j.msec.2017.04.113. Epub 2017 Apr 20.
To improve insulin bioavailability and overcome multiple barriers for oral delivery of insulin, the composite nanocarriers (PLGA/FA-CS) prepared from poly(lactide-co-glycoside) (PLGA) and folic acid modified chitosan (FA-CS) were fabricated via electrostatic self-assembly method. The resultant composite nanocarriers exhibited low cytotoxicity against HT-29 cells and excellent stability against protein solution. The chemical stability of loaded insulin against digestive enzyme were established in presence of simulated gastric fluid (SGF) containing pepsin and simulated intestinal fluid (SIF) containing pancreatin, respectively. The uptake behavior of HT-29 cells was evaluated by confocal laser scanning microscope. After oral administration to the diabetic rats, an effective hypoglycemic effect was obtained compared with subcutaneous injection of insulin. This work suggests that the as-prepared composite nanocarriers may be a promising drug delivery system for oral administration of insulin and other biomacromolecules.
为提高胰岛素的生物利用度并克服胰岛素口服递送的多重障碍，通过静电自组装法制备了由聚（丙交酯 - 共 - 糖苷）（PLGA）和叶酸修饰的壳聚糖（FA - CS）组成的复合纳米载体（PLGA/FA - CS）。所得复合纳米载体对HT - 29细胞表现出低细胞毒性，对蛋白质溶液具有优异的稳定性。分别在含有胃蛋白酶的模拟胃液（SGF）和含有胰酶的模拟肠液（SIF）存在下，确定了负载胰岛素对消化酶的化学稳定性。通过共聚焦激光扫描显微镜评估HT - 29细胞的摄取行为。对糖尿病大鼠口服给药后，与皮下注射胰岛素相比，获得了有效的降血糖作用。这项工作表明，所制备的复合纳米载体可能是一种有前途的用于胰岛素和其他生物大分子口服给药的药物递送系统。
