Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting
Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting
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DOI：
10.1023/a:1026422915326
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发表时间：
2000-10-01
影响因子：
3.7
通讯作者：
Uchegbu, IF
中科院分区：
文献类型：
--
作者：
Dufes, C;Schätzlein, AG;Uchegbu, IF
目的。制备用于药物靶向的葡萄糖或转铁蛋白配体的聚合物囊泡和微囊体。合成了葡萄糖-棕榈酸乙二醇壳聚糖(PGC)偶联物，并用超声法制备了葡萄糖-PGC/胆固醇聚合物囊泡。合成了N-棕榈酰氨基葡萄糖胺(NPG)，并将NPG/山梨醇单硬脂酸酯/胆固醇/胆固醇聚24-氧乙烯基醚超声聚合，制备了NPG微球。将这两个葡萄糖小泡与结肠癌刀豆蛋白A金(Con-A金)孵育，洗涤后在透射电子显微镜下观察。转铁蛋白也被连接到PGC囊泡的表面，并通过荧光激活细胞分类分析研究了这些囊泡在表达转铁蛋白受体的A431细胞系中的摄取。TEM成像证实了PGC聚合囊泡和NPG微泡表面存在葡萄糖单位。转铁蛋白与PGC囊泡的偶联水平为每克聚合物0.60+/-0.18克转铁蛋白。FITC-葡聚糖染色阳性的A431细胞比例分别为42%(FITC-葡聚糖溶液)、74%(普通囊泡)和90%(转铁蛋白囊泡)。结论制备了葡萄糖和转铁蛋白的壳聚糖囊泡和葡萄糖微球。含葡萄糖的囊泡将Con-A结合到其表面。以壳聚糖为基础的囊泡被A431细胞摄取，转铁蛋白增强这种摄取。
Purpose. To prepare polymeric vesicles and niosomes bearing glucose or transferrin ligands for drug targeting.Methods. A glucose-palmitoyl glycol chitosan (PGC) conjugate was synthesised and glucose-PGC polymeric Vesicles prepared by sonication of glucose-PGC/ cholesterol. N-palmitoylglucosamine (NPG) was synthesised and NPG niosomes also prepared by sonication of NPG/ sorbitan monostearate/ cholesterol/ cholesteryl poly-24-oxyethylene ether. These 2 glucose vesicles were incubated with coloidal concanavalin A gold (Con-A gold), washed and visualised by transmission electron microscopy (TEM). Transferrin was also conjugated to the surface of PGC vesicles and the uptake of these vesicles investigated in the A431 cell line lover expressing the transferrin receptor) by fluorescent activated cell sorter analysis.Results. TEM imaging confirmed the presence of glucose units on the surface of PGC polymeric vesicles and NPG niosomes. Transferrin was coupled to PGC vesicles at a level of 0.60 +/- 0.18 g of transferrin per g polymer. The proportion of FITC-dextran positive A431 cells was 42% (FITC-dextran solution), 74% (plain vesicles) and 90% (transferrin vesicles).Conclusions, Glucose and transferrin bearing chitosan based vesicles and glucose niosomes have been prepared. Glucose bearing vesicles bind Con-A to their surface. Chitosan based vesicles are taken up by A431 cells and transferrin enhances this uptake.