载盐酸阿霉素全氟己烷脂质体的制备及相变超声显影研究  

Preparation and Phase Change Ultrasound Development of Doxorubicin Hydrochloride-Loaded Perfluorohexane Liposomes

作　　者：苏琳[1] 胡聪[2] 许晓华[1] 王志刚[2] 李攀[2] 鲁树坤[1] 

机构地区：[1]香港大学深圳医院超声中心,广东深圳518000 [2]重庆医科大学超声影像学研究所,重庆400010

出　　处：《南昌大学学报（医学版）》2017年第3期36-39,共4页Journal of Nanchang University：Medical Sciences

基　　金：深圳市科创委基金(JCYJ20160429185900035);深圳市卫生计生系统科研项目(201607032)

摘　　要：目的制作载盐酸阿霉素全氟己烷(PFH)脂质体,检测其基本性质并查看其体外超声增强显像特点。方法用旋转蒸发和声震法制备载盐酸阿霉素的PFH脂质体,用光学显微镜和马尔文仪测量脂质体大小、形态和电荷。用低强度聚焦超声(LIFU)辐照后,观察脂质体的变化及其增强效果。应用不同功率的LIFU辐照载盐酸阿霉素PFH脂质体,得出最佳功率后在该功率下,寻求最佳脂质体的显影浓度计数。采用紫外分光光度计测包封率,并寻找最佳药脂比。结果载盐酸阿霉素PFH脂质体为砖红色混悬液,显微镜下脂质体形态球状,大小均匀;琼脂糖容器中经LIFU后,脂质体中PFH相变变为微泡,超声显影在基波和谐波模式均可显著增强。LIFU辐照载盐酸阿霉素PFH脂质体最佳功率是8 W、10min辐照;LIFU辐照载盐酸阿霉素PFH脂质体的最佳显影浓度计数为8.53×109 mL-1;载盐酸阿霉素PFH脂质体最佳药脂比1:10。结论载盐酸阿霉素PFH脂质体可同时进行造影和治疗,在一定的条件下可发生声致相变,使超声显像明显增强,有望成为超声分子影像学中新型造影剂。Objective To prepare doxorubicin hydrochloride-loaded perfluorohexane(PFH)liposomes,and to examine their basic properties and contrast-enhanced ultrasound characteristics.Methods Doxorubicin hydrochloride-loaded PFH liposomes were prepared by rotating evaporation and acoustic resonance method,and their size,shape and charge were measured by optical microscopy and Malvin apparatus.After low intensity focused ultrasound(LIFU)irradiation with different power,the changes in liposomes and enhanced effect were observed,and the optimal power was obtained to explore the optimal liposome development concentration.The encapsulation efficiency was measured by ultraviolet spectrophotometry and the optimal drug-to-lipid ratio was found.Results Doxorubicin hydrochloride-loaded PFH liposomes were prepared as a brickred suspension,and microscopically showed spherical shape with uniform size.After LIFU irradiation in agarose container,PFH phase changed into microbubbles.Ultrasonic development was significantly enhanced in both fundamental and harmonic modes.The optimal power of LIFU irradiation was 8 W/10 minute and the optimal concentration of doxorubicin hydrochloride-loaded PFH liposomes was 8.53× 109 mL^(-1).The optimal drug-to-lipid ratio was 1:10.Conclusion Doxorubicin hydrochloride-loaded PFH liposomes can be simultaneously used for contrast and treatment.Under certain conditions,they can produce acoustic phase change and obviously enhance ultrasound imaging.Therefore,doxorubicin hydrochloride-loaded PFH liposomes can be used as a new contrast media in ultrasonic molecular imaging.

关 键 词：全氟己烷 盐酸阿霉素 脂质体 造影剂 

分 类 号：R445.1[医药卫生—影像医学与核医学]