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| 肺靶向性多室脂质体磁共振对比剂的制备及其特性分析 |
| 张薇,耿芳,姜庆军,刘士远,肖湘生,余宇宏,魏晓慧 |
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| (上海交通大学附属仁济医院放射科,上海,200001;上海交通大学药学院大分子给药实验室,上海,200030;第二军医大学长征医院影像科,上海,200003) |
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| 摘要: |
| 目的:制备具有肺靶向性的多室脂质体DepoFoam(Depo)磁共振对比剂,对其理化性质及生物特性进行初步观察.方法:以Depo为载体包封常规磁共振对比剂钆喷酸葡胺(Gd-DTPA,Gd),制备多室脂质体磁共振对比剂Depo-Gd;观察其形态,分析其粒径,计算其包封率.10只小鼠随机平均分为Depo-Gd尾静脉注射组和Depo-Gd肠系膜静脉注射组2组,每组各5只,分别经鼠尾静脉或肠系膜静脉注射附有红色荧光的Depo-Gd,观察小鼠一般状况,初步分析其生物毒性;20 min后将所有小鼠的肝脏、肺脏和肾脏取出,制成切片,观察各脏器内有无红色荧光染色.结果:成功制备Depo-Gd粒子,电镜下可见其形态圆整,流动性好,性质稳定,粒径均匀(平均18 μm),包封率为50﹪,Gd的浓度为0.041 7 mmol/ml.注药后各组小鼠始终很活跃,未见明显的呼吸和神智异常;荧光显微镜下观察,Depo-Gd尾静脉注射组小鼠肺内见大量的红色物质显像,而肝肾内未见显影;Depo-Gd肠系膜静脉注射组小鼠肝脏显影良好而肺内未见染色.结论:Depo包载Gd制备的Depo-Gd理化性质稳定,具有较高的包封率,无明显生物毒性及过敏反应,经周围静脉注射时,具有很好的肺靶向性,值得进一步研究以应用于临床. |
| 关键词: 多室脂质体、钆喷酸葡胺、肺、磁共振成像 |
| DOI：10.3724/SP.J.1008.2007.00087 |
| 投稿时间：2006-05-28修订日期：2006-12-13 |
| 基金项目:上海市科委科研计划项目(03JC14009). |
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| Preparation and characterization of pulmonary targeting DepoFoam loaded MR contrast media: gadopentetate dimeglumine |
| ZHANG Wei,GENG Fang,JIANG Qing-jun,LIU Shi-yuan,XIAO Xiang-sheng,YU Yu-hong,WEI Xiao-hui |
| (上海交通大学附属仁济医院放射科,上海,200001;上海交通大学药学院大分子给药实验室,上海,200030;第二军医大学长征医院影像科,上海,200003) |
| Abstract: |
| Objective：To prepare a pulmonary targeting DepoFoam loaded MR contrast media： gadopentetate dimeglumine （Gd-DTPA）, and to observe its physi-chemical and biologic characteristics. Methods： The routine magnetic resonance contrast media Gd-DTPA was encapsulated with multivesicular liposome （DepoFoam, Depo） labelled with red fluorescence to obtain a new particle Depo-Gd. The morphology, diameter, and the encapsulation rate of the new particle were examined. The targeting efficiency of the particle was assessed by animal test with mice. Ten mice were evenly divided into 2 groups： one group received caudal vein-injection of Depo-Gd and the other group received vena mesenterica-injection of Depo-Gd. Twenty minutes after the injection the slices of the mouse liver, lung, and kidney were obtained from both group and the fluorescence labeling were observed. Results： Under microscope, the produced Depo-Gd particles were round in shape and stable in status, with good mobility and well-distributed diameter （18μm in average）. The encapsulation rate of the particles was 50% and the concentration of Gd was 0. 0417 mmol/ml. The animal fluorescence test showed that mice in the 2 groups were all active and with normal respiratory and conscious status after the injection. In the Depo-Gd caudal vein-injection group, large amount of red dyeing was found in the lung while little red dyeing was found in the liver and kidney; in vena mesenterica-injection group, satisfactory dyeing was found in the liver but not in the lung. Conclusion： The produced Depo-Gd particles have a stable physicchemical property and with satisfactory encapsulation rate. There is no obvious biological toxicity and allergic reaction. Besides, the particles have a good pulmonary targeting ability when injected into peripheral veins, making them promising in future clinical application |
| Key words: DepoFoam Gd-DTPA lung magnetic resonance imaging |
