跨膜梯度法制备羟苯磺酸铵-盐酸阿霉素脂质体  

Loading of doxorubicin hydrochloride into liposomes by ammonium dobesilate transmembrane gradient method

作　　者：宋阳[1] 张小飞[1] 周欣羽[1] 邹佳[1] 张玲[1] 邓意辉[1] 

机构地区：[1]沈阳药科大学药学院

出　　处：《中国药剂学杂志（网络版）》2009年第4期260-265,共6页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的:以2,5-二羟基苯磺酸铵形成脂质体内外水相跨膜梯度,主动装载盐酸阿霉素。方法:以2,5-二羟基苯磺酸铵溶液为水化介质制备空白脂质体。通过透析法建立空白脂质体跨膜梯度。超滤法结合离子对-高效液相色谱法(IP-HPLC)测定空白脂质体外水相2,5-二羟基苯磺酸铵浓度。将已建立梯度的空白脂质体与盐酸阿霉素溶液50℃孵育20min制备盐酸阿霉素脂质体。结果:脂质体平均粒径约为106.4nm,包封率为28.54%。结论:可以通过建立2,5-二羟基苯磺酸铵跨膜梯度来制备盐酸阿霉素脂质体。Objective Ammonium dobesilate was used to form transmembrane gradient to load doxorubicin hydrochloride (DOX) into liposomes. Methods:The lipid mixture was hydrated by 80 mmol·L-1 ammonium dobesilate to form liposomes. Ammonium dobesilate transmembrane gradient was obtained by dialysis method. The concentration of extraliposomal ammonium dobesilate was determined by ion-pair-HPLC method. The DOX solution was incubated with blank liposomes having transmembrane gradient at 50 ℃ for 20 minutes. Results:The average particle size of the liposomes was 106.4 nm. The entrapment efficiency of DOX liposomes determined by ultraviolet spectrophotometry was 28.54%. Conclusion:Ammonium dobesilate transmembrane gradient can be used to load DOX into liposomes.

关 键 词：药剂学 脂质体 盐酸阿霉素 2 5-二羟基苯磺酸铵 跨膜梯度载药 

分 类 号：R94[医药卫生—药剂学]