载卡莫司汀脂质超声造影剂制备及特性的研究

Preparation and characteristics of BCUN- loaded lipid ultrasound contrast agent

目的:制备载卡莫司汀脂质超声造影剂,检测其物理性状与造影增强效果。方法:采用机械振荡法制备载卡莫司汀脂质超声造影剂,显微镜下观察并计算其浓度、马尔文测量粒径大小、分布、电位,高效液相色谱法测量药物的包封率。微泡经冷冻干燥与60Co辐照消毒后,经兔耳缘静脉注射,观察其在兔肝内显像效果。结果:载药脂质造影剂的浓度为(2.6～3.1)×109/ml,平均粒径为(1.05±0.20)μm;卡莫司汀包封率为42.6%±0.11%;电位为-(12.93±1.84)mV;经兔耳缘静脉注射后,兔肝内可见持续的增强显像效果。结论:成功制备的卡莫司汀脂质超声造影剂,有望为肿瘤的靶向治疗提供新方向。

Objective： To preparate BCUN-loaded lipid ultrasound contrast agent and detect its physical properties and contrast-enhancing effects. Methods： Mechanical oscillation was used to prepare BCUN-loaded lipid contrast agent. Density was detected and analyzed with microscope. Malvem determined intensity,disposition and Zeta potential. RP-HPLC detected envelopment rate. Cryodesiccated-microb ubbles were sterilized by ^60Co irradiation. Following injected it through rabbit ear vein, effects of uhrasounic enhanced imaging in rabbit liver was observed. Results ：The density of mierobubble was （2.6-3.1） × 10^9/ml.The mean intensity was（ 1.05 ± 0.20）μm. The mean Zeta potential was （ 12.93 ± 1.84） mY. The mean nvelopment rate was （42.6 ± 0.11 ）%. After injecting this mierobubble, good and sustained ultrasounic enhanced images in rabbit liver were seen.Conclusions： BCUN- loaded lipid contrast agents were sueeessfully prepared,which hopefully provide a new option of targeting treatment for the tumor.