文章摘要
李武超,张 平,王 元,林茂铨,李范珠,朱志红.D-甘露糖修饰黄芩苷阳离子脂质体的制备及其对肺癌A549细胞增殖的抑制作用[J].,2021,(4):625-628
D-甘露糖修饰黄芩苷阳离子脂质体的制备及其对肺癌A549细胞增殖的抑制作用
Preparation of D-mannose Modified Baicalin Cationic Liposome and Its Inhibitory Effect on the Proliferation of Lung Cancer A549 Cells
投稿时间:2020-08-06  修订日期:2020-08-31
DOI:10.13241/j.cnki.pmb.2021.04.005
中文关键词: 黄芩苷  阳离子脂质体  体外释放  抗肿瘤活性
英文关键词: Baicalin  Cationic liposome  In vitro release  Antitumor activity
基金项目:国家自然科学基金项目(81873014)
作者单位E-mail
李武超 国家药品监督管理局食品药品审核查验中心 北京 100044 liwch@cfdi.org.cn 
张 平 国家药品监督管理局食品药品审核查验中心 北京 100044  
王 元 国家药品监督管理局食品药品审核查验中心 北京 100044  
林茂铨 国家药品监督管理局食品药品审核查验中心 北京 100044  
李范珠 浙江中医药大学药学院 浙江 杭州311400  
朱志红 浙江中医药大学药学院 浙江 杭州311400  
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中文摘要:
      摘要 目的:制备一种D-甘露糖修饰的黄芩苷阳离子脂质体[Baicalin cationic liposome,BC-Lipo(+)],并考察其对肺癌A549细胞增殖的抑制效果。方法:用乙醇注入法制备BC-Lipo(+),并考察其药剂学性质;以肺癌A549细胞为模型,采用MTT法考察其对肿瘤细胞的抑制效果。结果:透射电镜下可见BC-Lipo(+)呈圆形或类圆形,平均粒径(111.3±2.7)nm,Zeta电位(9.6±0.3)mV,包封率(95.4±0.8)%;体外释药行为符合Ritger-Peppas方程(lnQ=0.3497lnt - 1.6611,r=0.9924); A549细胞的增殖抑制率可达(88.3±5.7)%。结论:处方和制备工艺合理, BC-Lipo(+)包封率较高,粒径分布均匀,带一定的正电荷,具有明显的体外缓释特性,抑制肺癌A549细胞增殖效果显著,为深入研究肺靶向BC纳米脂质体制剂奠定了基础。
英文摘要:
      ABSTRACT Objective: A D-mannose-modified baicalin cationic liposome [BC-Lipo (+)] was prepared and its inhibitory effect on the proliferation of lung cancer A549 cells was investigated. Methods: BC-Lipo (+) was prepared by ethanol injection method, and its properties were investigated; MTT assay was used to investigate the inhibitory effect of BC-Lipo (+) on tumor cells of lung cancer A549 cells. Results: The BC-Lipo(+) were round or quasi-round under transmission electron microscopy, the average particle size was (111.3±2.7) nm, Zeta potential was (9.6±0.3) mV, entrapment efficiency was (95.4±0.8)%. The drug release behavior in vitro conformed to the Ritger-Peppas equation (lnQ=0.3497lnt-1.6611, r=0.9924). The proliferation inhibition rate of BC-Lipo (+) against A549 cells was (88.3±5.7)%. Conclusion: The formulation and preparation technology were feasible, and the prepared BC-Lipo (+) had high entrapment efficiency, uniform particle size distribution, positive charge. It had a slow-release characteristic in vitro, and significantly inhibited the proliferation of lung cancer A549 cells in vitro, laying a foundation for further research on lung-targeted BC nanoliposome preparations.
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