D-甘露糖修饰聚合物胶束的制备及其在靶向药物输送中的应用

发布时间：2018-04-20 20:38

本文选题：D-甘露糖 + 聚合物胶束　；参考：《生物工程学报》2016年01期

【摘要】：聚合物胶束作为药物载体具有良好的稳定性和生物相容性,提高疏水性药物溶解性等优势,是一类很有应用潜力的药物传输系统。本研究以合成的共价键连D-甘露糖的双亲性聚合物分子(PGMA-Mannose)为药物载体,包载抗癌药物阿霉素(DOX)制备具有甘露糖受体靶向性和pH敏感药物释放特性的新型载药聚合物胶束。利用激光共聚焦显微镜和MTT细胞毒性评价方法对载药胶束的细胞内吞摄取和毒性进行评价。实验结果表明,载药胶束能特异性识别人乳腺癌细胞MDA-MB-231表面过度表达的甘露糖受体,被癌细胞大量摄取并在细胞溶酶体酸性环境内释放药物,而载药胶束在表面甘露糖受体低表达的HEK293细胞中只有少量摄取。与原药DOX相比,该载药胶束对癌细胞的毒性显著提高,而对正常细胞的毒性较低。因此,该PGMA-Mannose聚合物胶束有望成为一种新型的靶向药物输送系统应用于癌症的治疗。
[Abstract]:As a drug carrier, polymer micelles have many advantages such as good stability, biocompatibility, and high solubility of hydrophobic drugs. In this study, a novel drug carrying polymer micelle with mannose receptor targeting and pH sensitive drug release was prepared by encapsulating adriamycin (DOX) as drug carrier with a covalently bonded amphiphilic polymer molecule (PGMA-Mannose). Endocytosis uptake and toxicity of drug loaded micelles were evaluated by laser confocal microscopy and MTT cytotoxicity evaluation. The results showed that the drug-loaded micelles could specifically recognize the over-expressed mannose receptors on the MDA-MB-231 surface of human breast cancer cells, which were absorbed in large quantities by cancer cells and released in the acidic environment of lysosomes. However, there was only a small uptake of drug-loaded micelles in HEK293 cells with low expression of mannose receptor on the surface. Compared with DOX, the micelle was more toxic to cancer cells than to normal cells. Therefore, the PGMA-Mannose polymer micelles are expected to be a novel targeted drug delivery system for cancer treatment.
【作者单位】：江南大学糖化学与生物技术教育部重点实验室;江南大学生物工程学院;江南大学食品安全与营养协同创新中心;
【基金】：国家自然科学基金(No.51403081) 江苏省自然科学基金(No.BK20140137)资助~~
【分类号】：R943

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