For folate receptor (FR) targeted anticancer therapy, novel folic acid (FA) conjugated cholesterol-modified glycol chitosan (FCHGC) micelles were synthesized and characterized by (1)H NMR, dynamic light scattering, transmission electron microscopy, and fluorescence spectroscopy. The degree of substitution was 1.4 FA groups and 7.7 cholesterol groups per 100 sugar residues of glycol chitosan. The critical aggregation concentration of FCHGC micelles in aqueous solution was 0.0169 mg/ml. The doxorubicin (DOX)-loaded FCHGC (DFCHGC) micelles were prepared by an emulsion/solvent evaporation method. The DFCHGC micelles were almost spherical in shape and their size increased from 282 to 320 nm with the DOX-loading content increasing from 4.53 to 11.4%. DOX released from DOX-loaded micelles displayed sustained release behavior. The targeted micelles encapsulated DOX showed significantly greater cytotoxicity against FR-positive HeLa cells than the nontargeted DOX-loaded micelles and free DOX. These results suggested that FCHGC micelles could be a potential carrier for targeted drug delivery.

译文

针对叶酸受体 (FR) 靶向抗癌治疗,合成了新型叶酸 (FA) 共轭胆固醇修饰的乙二醇壳聚糖 (FCHGC) 胶束,并通过 (1)H NMR,动态光散射,透射电子显微镜和荧光光谱对其进行了表征。取代度为1.4 FA组和7.7胆固醇组,每100糖残基乙二醇壳聚糖。FCHGC胶束在水溶液中的临界聚集浓度为0.0169 mg/ml。通过乳液/溶剂蒸发法制备了载有阿霉素 (DOX) 的FCHGC (DFCHGC) 胶束。DFCHGC胶束的形状几乎是球形的,并且它们的尺寸从282增加到320 nm,而DOX负载含量从4.53增加到11.4%。从载有DOX的胶束释放的DOX显示出持续释放的行为。与未靶向DOX负载的胶束和游离DOX相比,封装的DOX靶向胶束对FR阳性HeLa细胞显示出更大的细胞毒性。这些结果表明,FCHGC胶束可能是靶向药物递送的潜在载体。

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