具有肿瘤靶向及穿膜效应的壳聚糖胶束的制备

发布时间：2018-09-10 19:14

【摘要】：在壳聚糖(CS)表面修饰疏水基团辛基形成辛基壳聚糖(OC),然后再修饰亲水基团聚乙二醇(PEG)、肿瘤靶向配体氨基葡萄糖(DG)和穿膜肽九聚精氨酸(9R),形成DG和9R共同修饰的、同时具有肿瘤靶向性及穿膜效应的壳聚糖纳米胶束(DG/9R-PEG-OC)。核磁共振光谱分析及聚丙烯酰胺凝胶电泳检测结果证实了DG/9R-PEG-OC的成功制备;测得壳聚糖纳米胶束的粒径为151.8 nm左右、Zeta电位约为16.5 m V;透射电子显微镜照片显示该壳聚糖纳米胶束为均匀的球形结构;紫外分光光度法测定该载体的荧光素载药量约为28.2%,包封率约为75.0%,释药实验表明壳聚糖胶束具有良好的缓释作用;荧光显微镜观察显示,该DG/9R-PEG-OC胶束对肿瘤细胞尤其是葡萄糖受体高表达的肿瘤细胞Hep G2具有较好的靶向性及细胞穿膜效应。故DG/9R-PEG-OC胶束可作为脂溶性抗肿瘤药物的载体用于肿瘤的靶向化学治疗。
[Abstract]:Octyl chitosan (OC), was formed on the surface of chitosan (CS) by modifying hydrophobic group octyl group to form octyl chitosan (OC), then modified hydrophilic agglomeration ethylene glycol (PEG), tumor target ligand glucosamine (DG) and transmembrane peptide 9 polyarginine (9R) to form DG and 9R modified. Chitosan nanoparticles (DG/9R-PEG-OC) with tumor targeting and transmembrane effect. The results of NMR and polyacrylamide gel electrophoresis confirmed the successful preparation of DG/9R-PEG-OC. The particle size of chitosan nano-micelle was about 151.8 nm and the Zeta potential was about 16.5mV.The transmission electron microscopy (TEM) showed that the chitosan nano-micelle was a uniform spherical structure. The amount of fluorescein loaded on the carrier was about 28.2and the encapsulation efficiency was about 75.0 by ultraviolet spectrophotometry. The drug release experiment showed that chitosan micelle had good slow-release effect, and the fluorescence microscope showed that, The DG/9R-PEG-OC micelle has a good targeting and transmembrane effect on tumor cells, especially Hep G2 cells with high glucose receptor expression. Therefore, DG/9R-PEG-OC micelle can be used as a carrier of liposoluble anti-tumor drugs for tumor targeting chemotherapy.
【作者单位】：南通大学药学院;
【基金】：国家自然科学基金资助项目(No.81202467) 江苏省自然科学基金资助项目(No.BK2012232) 江苏省高校优势学科建设工程资助项目南通大学研究生科技创新计划资助项目(No.14060)~~
【分类号】：R943

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