张娜, 平其能, 徐文方. 荆豆凝集素修饰脂质体对小鼠口服吸收胰岛素的促进作用J. 药学学报, 2004, 39(12): 1006-1010.
引用本文: 张娜, 平其能, 徐文方. 荆豆凝集素修饰脂质体对小鼠口服吸收胰岛素的促进作用J. 药学学报, 2004, 39(12): 1006-1010.
ZHANG Na, PING Qi-neng, XU Wen-fang. Enhancing effect of Ulex europaeus agglutinin I modified liposomes on oral insulin absorption in miceJ. Acta Pharmaceutica Sinica, 2004, 39(12): 1006-1010.
Citation: ZHANG Na, PING Qi-neng, XU Wen-fang. Enhancing effect of Ulex europaeus agglutinin I modified liposomes on oral insulin absorption in miceJ. Acta Pharmaceutica Sinica, 2004, 39(12): 1006-1010.

荆豆凝集素修饰脂质体对小鼠口服吸收胰岛素的促进作用

Enhancing effect of Ulex europaeus agglutinin I modified liposomes on oral insulin absorption in mice

  • 摘要: 目的研究荆豆凝集素(UEA1)修饰的胰岛素脂质体在小鼠胃肠道的吸收作用。方法采用碳二亚胺偶联法制备荆豆凝集素修饰的磷脂酰乙醇胺(PE),将PE-UEA1参入胰岛素脂质体中制成凝集素修饰脂质体,并证实UEA1凝集活性不受影响。分别对正常小鼠及糖尿病模型小鼠灌胃给予350 u·kg-1胰岛素的修饰脂质体溶液,用葡萄糖酶试剂盒测定小鼠血糖,并与同剂量普通胰岛素脂质体比较。结果对于正常小鼠,荆豆凝集素修饰脂质体在4 h使血糖降至初始水平的(84±15)%,8 h降至(78±11)%,12 h为(90±12)%。胰岛素普通脂质体几乎没有降糖作用,与生理盐水对照组相当。对于糖尿病模型小鼠,荆豆凝集素修饰脂质体在4 h使血糖降至初始水平的(73±7)%,8 h降至(74±9)%,12 h为(86±9)%。结论荆豆凝集素修饰的脂质体可能通过与M细胞表面特异性受体的结合促进大分子药物的胃肠吸收。

     

    Abstract: AimTo investigate the enhancing effect on insulin absorption through GI. tract in mice by using the Ulex europaeus agglutinin I (UEA1) modified liposomes as the carrier. MethodsUEA1 modified phosphatidylethanolamine (PE) was prepared by conjugating method of 1-ethyl-3-(3′-dimethylaminopropyl) carbodiimide (EDC), then the modified compound (PE-UEA1) was incorporated into the conventional liposomes of insulin to obtain UEA1 modified liposomes. The agglutination test was performed to examine the UEA1 biological activities after synthesis and modification .When liposomes were applied to healthy mice or diabetic mice at insulin dose of 350 u·kg-1 orally, the hypoglycemic effect was investigated according to the blood glucose level determination. ResultsThe blood glucose levels of the healthy mice reduced by UEA1 modified liposomes were (84±15)% at 4 h, (78±11)% at 8 h and (90±12)% at 12 h after oral administration. The conventional liposomes and saline showed no effect. The blood glucose levels of the diabetic mice reduced by UEA1 modified liposomes were (73±7)% at 4 h, (74±9)% at 8 h, (86±9)% at 12 h after oral administration. ConclusionThe UEA1 modified liposomes promote the oral absorption of insulin due to the specific-site combination on M cell membrane.

     

/

返回文章
返回