荆豆凝集素修饰牛血清白蛋白脂质体的黏附性评价

In vitro and in vivo bioadhesive evaluation of ulex europaeus agglutinin I modified liposomes loading bovine serum albumin

目的对荆豆凝集素修饰牛血清白蛋白脂质体的黏附性进行评价。方法采用逆向蒸发法制备了荧光标记的普通脂质体和荆豆凝集素修饰的脂质体,通过小鼠胃肠道组织和荧光标记脂质体的离体孵化法考察了制剂的体外黏附性;通过制剂灌胃后的在体实验法考察了其体内黏附性。结果荆豆凝集素修饰的脂质体在小鼠胃、不含派伊尔氏结(peyer's patches,PPs)小肠和结肠中的黏附量与普通脂质体组相比没有明显差异(P>0.05),但在有PPs小肠区域,黏附脂质体量显著增加(P<0.05),且黏附时间可达24 h以上。结论荆豆凝集素修饰的脂质体可以长时间特异性黏附于小鼠含有PPs的小肠部位,从而增强口服黏膜免疫的靶向性和长效性。

Objective To establish the bioadhesive evaluation method of ulex europaeus agglutinin I （UEAI） modified liposomes loading bovine serum albumin. Methods The fluorescent-labeled unmodified and lectinmodified liposomes were prepared using the reverse-phase evaporation method. And then the in vitro and in vivo bioadhesion of these two liposomes were compared. Results UEAI-conjugated liposomes could significantly increase the interaction between liposomes and the intestinal mucosa （ with PPs） （ P 〈 0.05 ）, meanwhile,the bioadhesive time could contain 24 h at least. However, no difference in the extent of interaction was found between UEAI-LIP and stomach, small intestine （without PPs ） and colon （P 〉 0. 05 ）. Conclusions UEAI could specifically target mouse PPs, which could significantly enhance the adhesive amount and time of liposomes.