王星,冉海涛,王志刚,王红红,张辉.携RGD肽靶向高分子造影剂的制备及体外靶向实验[J].中国医学影像技术,2011,27(12):2403~2406
携RGD肽靶向高分子造影剂的制备及体外靶向实验
Preparation of RGD-PLGA and in vitro targeting study
投稿时间:2011-06-10  修订日期:2011-07-25
DOI:
中文关键词:  药物释放系统  高分子  造影剂
英文关键词:Drug delivery systems  Polymers  Contrast media
基金项目:国家自然科学基金面上项目(81071157)、重庆市科技攻关项目(CSTC,2009AB5216)。
作者单位E-mail
王星 重庆医科大学超声影像学研究所,重庆 400010  
冉海涛 重庆医科大学超声影像学研究所,重庆 400010
重庆医科大学附属第二医院超声科,重庆 400010 
rht@163.com 
王志刚 重庆医科大学超声影像学研究所,重庆 400010
重庆医科大学附属第二医院超声科,重庆 400010 
 
王红红 重庆医科大学超声影像学研究所,重庆 400010  
张辉 重庆医科大学超声影像学研究所,重庆 400010  
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中文摘要:
       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。
英文摘要:
      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.
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