Department of Pharmaceutics, Shenyang Pharmaceutical University, Wen Hua Road No. 103, Shenyang 110016, China.
Normal College, Shenyang University, Shenyang 110044, China.
Carbohydr Polym. 2014 Oct 13;111:433-41. doi: 10.1016/j.carbpol.2014.04.048. Epub 2014 Apr 21.
The objective was to explore the potential of decanoic acid grafted oligochitosan nanoparticles (CSO-DA NPs) as a carrier for insulin. The insulin-loaded CSO-DA NPs obtained by varying the pH and concentrations of CSO and DA had a particle size of 200.6 ± 71.2 nm, with an entrapment efficiency and loading efficiency of 61.18% and 5.56%, respectively. An in vitro study of the formulation showed typical burst of insulin and pH-dependent characteristics. The NPs administered by the in situ loop method were effective in lowering the serum glucose level of rats which was based on the synergistic effect of adhesion of CSO and permeation enhancing effect of DA. In particular, the 50 IU/kg-dose of CSO-DA NPs reduced the serum glucose level by 57.18%. Histopathology investigations showed that the CSO-DA NPs had a low toxicity. Therefore, CSO-DA nanoparticles appear to be promising vehicles for insulin transport through the intestinal mucosa.
目的是探索癸酸接枝壳寡糖纳米粒（CSO-DA NPs）作为胰岛素载体的潜力。通过改变 CSO 和 DA 的 pH 值和浓度，获得载有胰岛素的 CSO-DA NPs，其粒径为 200.6±71.2nm，包封效率和载药效率分别为 61.18%和 5.56%。该制剂的体外研究表明，其具有典型的胰岛素突释和 pH 依赖性特征。原位环法给药的 NPs 通过 CSO 的黏附作用和 DA 的渗透增强作用的协同效应，有效降低了大鼠的血清葡萄糖水平。特别是，50IU/kg 剂量的 CSO-DA NPs 可使血清葡萄糖水平降低 57.18%。组织病理学研究表明，CSO-DA NPs 毒性较低。因此，CSO-DA 纳米粒有望成为通过肠黏膜输送胰岛素的载体。
