青蒿琥酯脂质体的处方优化及抗非小细胞肺癌评价  

Formulation optimization and in vitro antitumor efficacy of artesunate liposomes

作　　者：吴小瑜 龙苗苗[2] 毛静 程沁园 邱立朋[1] 陈敬华 WU Xiao-yu;LONG Miao-miao;MAO Jing;CHEN Qin-yuan;QIU Li-peng;CHEN Jinghua(Department of Pharmacy,Jiangnan University,Wuxi Jiangsu 214122;Department of Pharmacy,Wuxi Higher Health Vocational Technology School,Wuxi Jiangsu 214028)

机构地区：[1]江南大学药学院,江苏无锡214122 [2]无锡卫生高等职业技术学校药学系,江苏无锡214028

出　　处：《中南药学》2021年第7期1294-1299,共6页Central South Pharmacy

基　　金：中国博士后科学基金(No.2019M660166);江苏省无锡市卫生计生委科研项目(No.Q201843);江苏省高校“青蓝工程”中青年学术带头人培养项目。

摘　　要：目的通过薄膜分散法制备青蒿琥酯脂质体(ART-liposome),并考察其体外抗非小细胞肺癌的活性。方法对磷脂/胆固醇比例和探头超声时间进行筛选,制备ART-liposome并表征其制剂学性质。选择非小细胞肺癌A549细胞为模型,通过细胞毒性、生长状态、摄取情况和染色观察评价ART-liposome的抗肿瘤作用。结果优化后制备的ART-liposome粒径为(120±5.01)nm的球形粒子,分布均一,包封率为(92.45±3.57)%,能够在肿瘤酸性条件下特异性释放药物,累积释放率达到60%。体外细胞实验表明,空白脂质体对细胞几乎没有毒性,具有良好的生物相容性。而ART-liposome能够被细胞较好地摄取以有效地杀死肿瘤细胞。结论ART-liposome是一种有前景的抗肿瘤药物新制剂,可为后续青蒿琥酯的开发提供参考。Objective To prepare artesunate-loaded liposomes(ART-liposome)by thin film dispersion method and evaluate the in vitro antitumor activity against non-small cell lung cancer.Methods The phospholipid/cholesterol ratio and probe ultrasound time were screened to prepare ART-liposome and determine the pharmaceutical properties.A549 cells,as the model of non-small cell lung cancer cells,were used to verify the antitumor effect of ART-liposome by determining the cytotoxicity,growth status,cellular uptake and staining observation.Results ART-liposome presented uniformly distributed spherical particles of(120±5.01)nm and encapsulation efficacy of(92.45±3.57)%,and specifically released drugs under the acid condition of tumor.In vitro antitumor experiments showed that blank liposomes showed nearly no toxicity to non-small cell lung cancer A549 cells,suggesting good biocompatibility.However,ART-liposome could be uptaken into the tumor cells resulting in effective killing of the tumor cells.Conclusion ART-liposome is a promising new antitumor formula,which provides reference for further research and development of artesunate.

关 键 词：脂质体 青蒿琥酯 处方优化 抗肿瘤作用 

分 类 号：R285.5[医药卫生—中药学]