Zhang Na, Ping Qineng, Huang Guihua, Han Xiuzhen, Cheng Yanna, Xu Wenfang
The Pharmaceutical College, Shandong University, 44 Wen hua Xi Lu, Ji'nan, Shandong Province, China.
J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):2959-66. doi: 10.1166/jnn.2006.425.
Wheat germ agglutinin (WGA) modified liposomes and solid lipid nanoparticles (SLNs) were evaluated for improving intestinal absorption of insulin. In an in situ local intestinal perfusion experiment, formulations containing 100 IU/kg insulin were administered to the duodenum, jejunum, and ileum of fasted rats. As hypothesized, ileum was the best intestinal location for the absorption of insulin-containing liposomes. Serum insulin concentrations decreased for the various formulations in different absorption sites according to the following trends: Duodenum > ileum > jejunum for WGA-modified insulin-containing liposomes; duodenum > jejunum > ileum for WGA-modified insulin-containing SLNs; ileum > jejunum > duodenum for insulin-containing liposomes; ileum > duodenum > jejunum for insulin-containing SLNs; and duodenum > or = ileum > jejunum for aqueous solution of insulin. These results imply that the nanoparticle type and delivery site were important factors with respect to increasing the bioavailability of insulin following oral administration. The proteolytic degradation as well as the epithelial permeability were primary determinants influcing insulin mucosal absorption.
评估了小麦胚凝集素（WGA）修饰的脂质体和固体脂质纳米粒（SLN）对改善胰岛素肠道吸收的作用。在原位局部肠道灌注实验中，将含100 IU/kg胰岛素的制剂给予禁食大鼠的十二指肠、空肠和回肠。如所假设的，回肠是含胰岛素脂质体吸收的最佳肠道部位。不同吸收部位的各种制剂的血清胰岛素浓度按以下趋势降低：WGA修饰的含胰岛素脂质体为十二指肠＞回肠＞空肠；WGA修饰的含胰岛素SLN为十二指肠＞空肠＞回肠；含胰岛素脂质体为回肠＞空肠＞十二指肠；含胰岛素SLN为回肠＞十二指肠＞空肠；胰岛素水溶液为十二指肠≥回肠＞空肠。这些结果表明，纳米粒类型和给药部位是口服给药后提高胰岛素生物利用度的重要因素。蛋白水解降解以及上皮通透性是影响胰岛素黏膜吸收的主要决定因素。
