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携RGDS的靶向超声造影剂的制备及鉴定 被引量:8
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作者 杨钰楠 高云华 +1 位作者 谭开彬 刘政 《中国医学影像技术》 CSCD 北大核心 2005年第11期1677-1679,共3页
目的制备血栓靶向脂膜超声造影剂,并对其理化特性及靶向作用进行鉴定。方法将脂膜超声造影剂通过酰胺键共价键键合的方式与血栓靶向短肽片段(RGDS)进行结合。制备产物通过流式细胞仪进行携带率和稳定性的检测;对内源性凝血途径产生的血... 目的制备血栓靶向脂膜超声造影剂,并对其理化特性及靶向作用进行鉴定。方法将脂膜超声造影剂通过酰胺键共价键键合的方式与血栓靶向短肽片段(RGDS)进行结合。制备产物通过流式细胞仪进行携带率和稳定性的检测;对内源性凝血途径产生的血栓进行寻靶特性研究。结果流式细胞仪显示携带RGDS的脂膜超声造影剂其波长发生了明显变化,携带率达到82%;激光共聚焦显微镜显示携带RGDS的脂膜超声造影剂对离体血栓具有很强的靶向性和稳定性。结论采用共价键键合的化学修饰方法成功制备了亲血栓靶向脂膜超声造影剂。 展开更多
关键词 RGDS 血栓靶向 造影剂 微泡
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Preparation of Thrombosis-targeted Lipid Microbubbles and Determination of Rabbit Carotid Artery Thrombosis by Microbubbles Ultrasonogaphy 被引量:1
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作者 徐卫明 冯敏 +3 位作者 赵洪洋 谢明星 黎维勇 符荣 《Journal of Huazhong University of Science and Technology(Medical Sciences)》 SCIE CAS 2013年第1期146-152,共7页
A kind of thrombus-targeted lipid-coated microbubbles were prepared, and the target prop- erty of the microbubbles and the effects of different methods detecting thrombosis in vessels were ob- served. Phospholipid-coa... A kind of thrombus-targeted lipid-coated microbubbles were prepared, and the target prop- erty of the microbubbles and the effects of different methods detecting thrombosis in vessels were ob- served. Phospholipid-coated microbubbles were prepared by membrane-hydration method. Throm- bus-targeted lipid-coated fluorocarbon microbubbles were labeled with specific fluorescence and then integrated to the thrombus in vivo and ex vivo through an avidin biotin system. The thrombus was im- mediately observed for the distribution and property of the thrombus-targeted microbubbles under the optical microscope, fluorescence microscope and transmission electron microscope. The carotid throm- bosis models were set up in rabbits, and the effects of different methods detecting thrombosis in vessels were observed. The diameter of the phospholipid-coated microbubbles was 0.8-2.5μm, and even reached nanoscale in some of them. The zeta electric potential was about -11 mV and the concentration was about 1.08×10μmL. Immunofluorescence of rapid frozen sections in vivo and ex vivo showed that massive targeted lipid-coated microbubbles flocked around fresh blood clots and some aggregated within them under the light and fluorescence microscope. The number of aggregated microbubbles ex vivo was greater than that observed in the experiment in vivo, and the fluorescence observed in the ex- periment ex vivo was stronger than that in the experiment in vivo. The same imaging was observed un- der the electron microscope. Models of carotid thrombosis in rabbits were established successfully. Ef- fects of detecting thrombosis by means of thrombosis-targeted microbubble ultrasonoraphy and Sono Vue ultrasonography in vessels were more satisfactory than those by Color Doplor Flow Imaging (CDFI), ordinary microbubbles and Three Dimensions-time of flight MR angiography (3D-TOF-MRA) (P〈0.01). Compared to ordinary microbubbles ultrasonography, thrombosis-targeted microbubbles ultrasonography had the advantages whenever in imaging qualit 展开更多
关键词 thrombus-targeted phospholipid-coated microbubbles fluorescence detection electron mi- croscope thrombus magnetic resonance angiography
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HV12p-rPA血栓靶向脂质体的制备及体内溶栓实验
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作者 邓璇 梁兰 +4 位作者 高漫潞 康丽梅 余蓉 苏志国 吴梧桐 《药物生物技术》 CAS CSCD 2011年第3期215-219,共5页
将通过蛋白质工程获得的抗凝溶栓双功能蛋白水蛭素12肽-瑞替普酶(HV12p-rPA)制备成靶向脂质体,并考察其体内溶栓效果。用薄膜分散-超声法制备HV12p-rPA脂质体,通过正交设计优化处方,采用碳二亚胺法偶联抗纤维蛋白原单克隆抗体(McAbSZ-65... 将通过蛋白质工程获得的抗凝溶栓双功能蛋白水蛭素12肽-瑞替普酶(HV12p-rPA)制备成靶向脂质体,并考察其体内溶栓效果。用薄膜分散-超声法制备HV12p-rPA脂质体,通过正交设计优化处方,采用碳二亚胺法偶联抗纤维蛋白原单克隆抗体(McAbSZ-65)制备HV12p-rPA靶向脂质体,采用大鼠颈总动脉血栓模型,考察HV12p-rPA靶向脂质体的体内溶栓效果。结果:最佳处方中HV12p-rPA脂质体的粒径为(142.45±1.20)nm,Zeta电位为(-30.63±0.48)mV,平均包封率为(91.59±1.39)%。靶向脂质体组(0.48±0.083)mg在相同剂量下(80k IU/kg)与PBS空白对照组(2.04±0.114)mg、游离HV12p-rPA组(1.2±0.100)mg和普通HV12p-rPA脂质体组(0.74±0.089)mg分别比较,其血栓干重明显减轻(P<0.05);靶向脂质体组与5倍剂量(400k IU/kg)的游离HV12p-rPA组(0.52±0.084)mg比较,其血栓干重较之偏轻(P>0.05)。制备出的靶向HV12p-rPA脂质体具有体内靶向溶栓效果。 展开更多
关键词 水蛭素12肽-瑞替普酶 脂质体 靶向溶栓 颈总动脉血栓模型
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血栓靶向尿激酶脂质体的制备及其体内溶栓效果 被引量:20
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作者 王向涛 李沙 +1 位作者 张小滨 侯新朴 《药学学报》 CAS CSCD 北大核心 2003年第3期231-235,共5页
目的 制备血栓靶向的尿激酶脂质体 ,并在大鼠颈总动脉血栓模型上考察其溶栓情况。方法 通过液相合成法合成出靶向于血栓的特异性配体H Arg Gly Asp Ser OH (RGDS) ,并将其与monocarboxylpoly (ethyleneglycol)35 0 0distearoylphospha... 目的 制备血栓靶向的尿激酶脂质体 ,并在大鼠颈总动脉血栓模型上考察其溶栓情况。方法 通过液相合成法合成出靶向于血栓的特异性配体H Arg Gly Asp Ser OH (RGDS) ,并将其与monocarboxylpoly (ethyleneglycol)35 0 0distearoylphosphatidylethalnolamine (DSPE PEG350 0 COOH)偶联后插入到脂质体双层膜中得到血栓靶向尿激酶脂质体 ;通过制备方法的改进 ,以氢化豆磷脂在室温下制备尿激酶脂质体 ;在大鼠颈总动脉血栓模型上 ,考察了血栓靶向脂质体的体内溶栓效果。结果 所得的尿激酶脂质体包封率高、粒径小 ,稳定性好 ;与空白对照组的栓重相比 ,在相同剂量 (6 0kU·kg- 1 ,小剂量 )下 ,游离尿激酶组几乎无任何改变 ,尿激酶脂质体组血栓重量稍有减轻但无显著性差异 ,血栓靶向尿激酶脂质体组血栓重量明显减轻 (P <0 0 0 1) ;干重时的情况略有不同。与同剂量的普通脂质体相比 ,血栓靶向尿激酶脂质体溶栓效果显著改善 (湿重时P <0 0 1,干重时P <0 0 5 ) ,表现出明显的靶向溶栓能力。 展开更多
关键词 血栓靶向 RGDS 尿激酶 脂质体 颈总动脉血栓模型
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