载诺帝脂质微泡的制备及特性的实验研究

目的 制备载诺帝(去甲二氢愈创木酸)脂质微泡并测定其包封率、载药量及观察其体内超声显像效果.方法 采用机械振荡法制备载诺帝脂质微泡,测定其粒径大小、分布和Zeta电位、包封率、载药量;超声造影观察其在兔肝内的显像效果.结果 载药脂质微泡的浓度为(2.53±0.52)×109个/ml,粒径为(2.61±0.32)μm,Zeta电位为+(17.52±2.04)mV;脂质微泡诺帝的包封率(27.1±2.01)%,载药量为(10.9±0.90)%;微泡经外周静脉注射后,兔肝可见良好、持续的增强显像效果.结论 采用机械振荡法可以成功制备携带诺帝的脂质微泡,微泡可以通过肺血管床,符合静脉注射要求,在家兔体内获得了良好的显像效果.

Preparation and Characteristics of Acoustically Active Nordy-carrying Microbubbles

Objective To prepare and evaluate Nordy-carrying microbubbles as a new ultrasound contrast agent for chemotherapeutic drug delivery.Methods Nordy-carrying microbubbles were prepared by using a shaking-device.Characteristics and properties(appearence，size,concentration,surface potential) of the microbubbles were observed and blood cell counting chamber,and Zetasizer 3000,etc were detected with optical microscope,The entrapment efficiency of Nordy was detected with high-performance liquid chromatography(HPLC).Results Acoustically active microbubbles containing Nordy had a mean particle count which approximates to(2.53±0.52)×10~9 particles per ml,a mean size of(2.61±0.32) μm,surface potencial＋(17.52±2.04) mV,the drug entrapment efficiency（27.1±2.01）% and the carried Nordy(10.9±0.90%).After intravenous injection of Nordy-carrying microbubbles,the rabbit liver imaging was remarkbly enhanced.Conclusions The Nordy-carrying microbubbles can be prepared successfully by machanical vibration.and can be carried through lung vessel.The properties of microbubbles can meet the demand of intravenous injection and produce a contrast-enhanced ultrasonography in vivo.