靶向血栓高分子超声造影剂的制备及其体外寻靶实验  

Preparation of High Molecular Ultrasound Contrast Agent Targeting Thrombus and Experiments in Vitro

作　　者：张瑜[1] 郭大静[1] 敖梦[2] 冉海涛[2] 郑元义[2] 赵建农[1] 

机构地区：[1]重庆医科大学附属第二医院放射科,重庆市400010 [2]重庆医科大学附属第二医院超声影像研究所,重庆市400010

出　　处：《中国超声医学杂志》2012年第4期289-292,共4页Chinese Journal of Ultrasound in Medicine

基　　金：重庆市自然科学基金计划项目(CSTC;No.2008BB5233);国家自然科学基金面上项目(No.81171332)

摘　　要：目的制备靶向血栓高分子超声造影剂,并对其理化性质及体外寻靶能力进行研究。方法以高分子材料端羧基聚乳酸/羟基乙酸(PLGA-COOH)为载体,采用双乳化法制备PLGA微球;并用碳二亚胺法将该微球与血栓靶向短肽片段精氨酸-甘氨酸-天冬氨酸-丝氨酸(RGDS)共价结合制备靶向血栓高分子超声造影剂(RGDS-PL-GA);检测该造影剂的理化特性并通过体外寻靶实验,评价其对血栓的亲和性。结果采用本法成功制备了RGDS-PLGA,其形态规则,呈大小均匀的球形,平均粒径为(1.21±0.27)μm,RGDS携带率25.69%。体外实验显示RGDS-PLGA可以牢固结合到血栓表面。结论采用双乳化法及碳二亚胺法可以成功制备靶向血栓高分子超声造影剂,该造影剂粒径小,对血栓具有很强的靶向性及稳定性,有望在分子水平为血栓的诊断提供新方法。Objective To prepare high molecular ultrasound contrast agent targeting thrombus and identify its physical and chemical properties and the ability to target thrombus in vitro. Methods Double emulsion solvent-evaporation technique was used to prepare PLGA particles using PLGA-COOH as a carrier. Arg-Gly-Asp-Ser（RGDS）peptides were further immobilized by carbodiimide method to prepare the polymer ultrasound contrast agent targeting thrombus （RGDS-PLGA）. The characteristics of the particles were tested and the ability to target thrombus was assessed by experimental study in vitro. Results RGDS-PLGA was successfully prepared by this way. The particles had a mean diameter of （1.21±0.27） tin1. The rate of carrying RGDS peptides was 25.69%. In the experiments in vitro, it showed that RGDS-PLGA particles had successfully been eonjuneted with the thrombus. Conclusions High molecular ultrasound contrast agent targeting thrombus was successfully prepared by the way of double emulsion solventevaporation technique and carbodiimide method. The sizes of the particles were small and the ability to target thrombus was stable. It was helpful to provide a new method to diagnose thrombosis at the molecular level.

关 键 词：PLGA RGDS 靶向 血栓 超声 造影剂 

分 类 号：TQ421.7[化学工程]