光敏ROS响应型雷帕霉素脂质体的制备及表征  

Preparation and characterization of photosensitive ROS-responsive rapamycin liposomes

作　　者：高习清 卢光照 鲁莹 邹豪 GAO Xiqing;LU Guangzhao;LU Ying;ZOU Hao(Department of Pharmaceutics,School of Pharmacy,Naval Medical University,Shanghai 200433,China)

机构地区：[1]海军军医大学药学系药剂学教研室,上海200433

出　　处：《药学实践与服务》2022年第5期437-441,共5页Journal of Pharmaceutical Practice and Service

基　　金：国家自然基金面上项目(81773278)。

摘　　要：目的研究光敏活性氧自由基(reactive oxygen species,ROS)响应型雷帕霉素脂质体的制备工艺及其性质,旨在开发一种稳定高效的刺激响应型脂质体载体。方法采用薄膜分散法制备雷帕霉素脂质体;马尔文激光粒度仪测定其粒径及Zeta电位;利用HPLC法建立雷帕霉素含量测定方法;经近红外光照射后,采用反向透析法考察雷帕霉素脂质体的体外释放特性。结果雷帕霉素脂质体粒径<200 nm,PDI值<0.200;雷帕霉素在0.2~40μg/ml范围与峰面积呈良好的线性关系,相关系数r=0.9995;雷帕霉素脂质体包封率>94.20%;经730 nm近红外光照射5 min后,雷帕霉素脂质体12 h内体外释放率可达60%。结论成功制备了光敏ROS响应型雷帕霉素脂质体,具有较高的包封率和体外刺激响应效率。Objective To study the preparation process and properties of photosensitive ROS(Reactive oxygen species)responsive rapamycin liposome,and to develop a stable and efficient stimulus-responsive liposome carrier.Methods Rapamycin liposomes were prepared by thin film dispersion method.The particle size and Zeta potential were determined by Malvern laser particle size analyzer.An assay method for rapamycin was established by HPLC.In vitro release characteristics of rapamycin liposomes were investigated by reverse dialysis after irradiation with near-infrared light.Results The particle size of rapamycin liposome was less than 200 nm and the PDI value was less than 0.200.Rapamycin showed a good linear relationship with peak area in the range of 0.2-40μg/ml,with the correlation coefficient of 0.9995.Encapsulation rate of rapamycin liposomes was>94.20%.The release efficiency of rapamycin liposomes reached 60%within 12 h after irradiation with 730 nm near infrared light for 5 min.Conclusion Photosensitive ROS-responsive rapamycin liposomes were successfully prepared,which had high encapsulation rate and stimulation response efficiency in vitro.

关 键 词：脂质体 雷帕霉素 近红外光 活性氧自由基 体外释放 

分 类 号：R943[医药卫生—药剂学] R96[医药卫生—药学]