比较两种制备载紫杉醇超声微泡的方法  

Comparison of two preparation methods of ultrasound microbubbles loaded with paclitaxel

作　　者：朱梅[1] 刘政[2] 张萍[3] 梁红敏[1] 谭开彬[2] 付赤学[2] 李佩倞[2] 高云华[2] 李睿[1] 

机构地区：[1]昆明医学院第一附属医院超声科,云南昆明650032 [2]第三军医大学附属新桥医院超声科,重庆400037 [3]第三军医大学附属西南医院超声科,重庆400037

出　　处：《中国医学影像技术》2009年第7期1148-1151,共4页Chinese Journal of Medical Imaging Technology

基　　金：国家自然科学基金地区项目(30860269);云南省应用基础研究计划面上项目(C0620056Q)

摘　　要：目的比较能被超声击破的两种载紫杉醇超声微泡的制备方法,并评价其理化性质以及超声散射强度。方法用单纯紫杉醇法Ⅰ号和三醋酸甘油酯溶解法Ⅱ号分别制备载紫杉醇脂质超声微气泡,测定其包封率、载药量、粒径大小、分布和Zeta电位、pH值,并行超声击破试验及兔VX2皮下肿瘤显像试验。结果两种微泡显像无明显差异,可被低能量超声击破,但Ⅱ号(加入三醋酸甘油酯)脂质微泡较Ⅰ号(常规冷冻干燥法制备)载药微泡粒径显著减小[(1.07±0.38)μmvs(2.79±0.41)μm,P<0.01],表面电位增高[(19.10±0.32)mVvs(-5.90±0.21)mV,P<0.01],包封率和载药量显著增高[(95.00±1.22)%vs(36.10±4.74)%,P<0.01;(5.60±0.11)%vs(0.50±0.04)%,P<0.01]。结论三醋酸甘油酯溶解法制备的Ⅱ号微泡在局部药物释放中具有更大的应用价值。Objective To compare two effective preparation methods for paclitaxel-loaded lipid microbubbles, and to evaluate the physiochemical properties as for acoustic activated drug delivery. Methods Paclitaxel-loaded lipid microbubbles were prepared with two methods： one was mixed with phospholipids directly （ Ⅰ ）; the other was added in triacetin, then mixed with phospholipids （ Ⅱ ）. Concent ration, size, pH, drug entrapment efficiency, drug-loading amounts of these two kinds of paclitaxel-loaded lipid microbubbles were studied, while drug release with ultrasound and tumor imaging enhanced on rabbit breast tumor were observed. Results There was no significant difference in tumor imaging between two kinds of microbubbles which could be ruptured by low energy ultrasound. Compared with Ⅰ , the mean diameter of Ⅱ decreased significantly （[ 1.07±0.38] μm vs [2.79± 0.41] μm, P〈0.01）, the surface potencial was higher （[19.10±0.32] mV vs [-5.90± 0.21] mV, P〈0.01）, whereas entrapment efficiency and drug-loading amounts increased markedly （[ 95.00±1.22]% vs [36.10±4.74]%, P〈0.0]; [5.60±0.11]% vs [0.50±0.04]%, P〈0.01）. Conclusion The Ⅱ paclitaxel-loaded lipid microbubbles added triacetin have an important clinical value.

关 键 词：紫杉醇 微泡 超声检查 药物释放 造影剂 

分 类 号：R445.7[医药卫生—影像医学与核医学] R-332[医药卫生—诊断学]