摘要
目的制备去氢骆驼蓬碱脂质体并对其制备工艺进行优化,评价脂质体的相关表征及对肝癌细胞的毒性。方法用薄膜水化法制备去氢骆驼蓬碱脂质体。以包封率作为评价指标,以大豆卵磷脂和药物的质量比、大豆卵磷脂与胆固醇的质量比和超声时间作为评价因素对脂质体包封率的影响。并对脂质体的粒径、Zeta电位、外观和稳定性进行评价。CCK-8法对比去氢骆驼蓬碱和去氢骆驼蓬碱脂质体的抗肝癌细胞增殖活性。结果最优制备工艺:大豆卵磷脂和药物的质量比为11.4︰1,大豆卵磷脂与胆固醇的质量比为4.4︰1,超声时间为33 min。在此条件下制备的脂质体的包封率为81.88%,粒径为143.65 nm,Zeta电位为–12.68 mV,低温环境稳定性良好,具有缓释效应。去氢骆驼蓬碱脂质体的抗肝癌细胞增殖活性大于裸药。结论所制得的去氢骆驼蓬碱脂质体包封率和稳定性均符合标准。将去氢骆驼蓬碱制备成为脂质体能提高其抗肝癌细胞增殖活性。
OBJECTIVE To prepare harmine liposomes and optimize their preparation process,and to evaluate the characteristics of liposomes and their toxicity to liver cancer cells.METHODS The harmine liposomes were prepared by membrane hydration method.Taking the encapsulation rate as the evaluation index,the influence of the mass ratio of soybean lecithin to drug,the mass ratio of soybean lecithin to cholesterol and the ultrasound time as evaluation factors on the encapsulation rate of liposomes was studied.The particle size,Zeta potential,appearance and stability of liposomes were evaluated.The CCK-8 method was used to compare the anti-proliferative activity of harmine and harmine liposomes on liver cancer cells.RESULTS The optimal preparation process was as follows:the mass ratio of soybean lecithin to drug was 11.4∶1,the mass ratio of soybean lecithin to cholesterol was 4.4∶1,and the ultrasound time was 33 min.The encapsulation efficiency of liposomes prepared under these conditions was about 81.88%,the particle size was 143.65 nm,the Zeta potential was–12.68 mV,which stability was good in low temperature environment with slow release effect.The anti proliferative activity of harmine liposomes on liver cancer cells was greater than that of naked drugs.CONCLUSION The encapsulation rate and stability of the prepared harmine liposomes meet the standard.The preparation of harmine as a liposome can improve the its proliferative activity on liver cancer cells.
作者
张光财
史阔豪
武康雄
李菡
ZHANG Guangcai;SHI Kuohao;WU Kangxiong;LI Han(School of Food and Biological Engineering,Shaanxi University of Science&Technology,Xi’an 710021,China)
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2022年第13期1677-1684,共8页
Chinese Journal of Modern Applied Pharmacy
基金
国家自然科学基金项目(81803784)
中国博士后面上项目(211956)
陕西省自然科学基金项目(2019JQ-779)
陕西科技大学科研启动基金项目(2016BJ-57)
关键词
去氢骆驼蓬碱
脂质体
制备工艺
抗肝癌活性
harmine
liposome
preparation process
anti-hepatocarcinoma activity
作者简介
张光财,男,硕士生,E-mail:zhangguangcai321@sina.com;通信作者:李菡,女,博士,副教授,E-mail:lihan@sust.edu.cn
