Objective To synthesize RGD-PLGA and further explore its targeting ability in vitro. Methods High molecular polymer PLGA-COOH was prepared using double emulsion technique. Targeted high molecular polymer ultrasound contrast agents RGD-PLGA was synthesized by combining PLGA-COOH ultrasound contrast agents with RGD peptides using covalent binding. The conjugation of FITC-RGD and PLGA was detected by laser scanning confocal microscope! The affinity of RGD-PLGA and PLGA for SKOV-3 cells was investigated with light microscope and fluorescence microscope. Then the targeting ability between RGD-PLGA and control PLGA was compared by flow cytometry technique. Results FITC-RGD-PLGA showed clear green light by laser scanning confocal microscope. It was showed that many RGD-PLGA attached to SKOV-3 tightly in vitro experiment by light microscope and fluorescence microscope. It was also showed that RGD-PLGA has stronger targeting ability to SKOV-3 cells by flow cytometry technique. Conclusion RGD-PLGA was successfully synthesized and proved having strong targeting ability to SKOV-3 cells expressing integrin αvβ3.%目的 制备携RGD肽的PLGA造影剂,并观察其在体外的靶向能力.方法 采用双乳化法制备PLGA-COOH造影剂,利用碳二亚胺法将RGD肽与PLGA-COOH造影剂共价结合,制备出RGD-PLGA的靶向造影剂.用激光共聚焦检测FITC-RGD与PLGA造影剂的连接情况,并在光镜及荧光显微镜下对比观察RGD-PLGA与普通PLGA靶向SKOV-3细胞的能力,而后利用流式细胞检测技术对比RGD-PLGA与普通PLGA的靶向能力.结果 连接FITC-RGD的PLGA显示出明显的绿光,体外靶向实验显示RGD-PLGA较普通PLGA更多地聚集在SKOV-3细胞的周围,流式细胞检测显示RGD-PLGA较普通PLGA有更好的靶向性.结论 成功制备出RGD-PLGA,且在体外实验中对高表达整合素αvβ3的SKOV-3细胞有较强的结合能力.
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