和厚朴酚脂质体的制备及其体外抗肿瘤活性的研究

determined by Zetasizer nano ZS and transmission electron microscope （TEM）, respectively; DiL fluorescence probe was
used to mark the liposome-HNK and to explore the cellular uptake in a time dependent fashion; the pharmacological
（0.24 ±0.00） and zeta potential was （53.23 ±1.16）mV; when the lipid-drug ratio was 7% , the encapsulation rate
reached the highest, as high as （99.47±0.20）% and had a long-term stability in 4℃ environment; the apoptosis rate of
老年医学与保健 2019 年第 25 卷第 1 期 Geriatr Health Care，2019，Vol.25.No.1
和厚朴酚脂质体的制备及其体外抗肿瘤活性的研究
魏晓 1，杜子秀 2，陆平 1
1.上海交通大学医学院附属第九人民医院老年科，上海 200011；2.上海交通大学药学院，上海 200240
effects of liposomLeabharlann Baidu-HNK on HCCLM3 cells were detected by WST -1 and BD apoptosis kits.
Liposome-HNK
was （112.30±0.78） nm in average particle size with even size distribution, the polydispersity index （PDI） value was
liposome-HNK was significantly higher than that in free-drug group （ ＜0.05）.
The preparation process of
liposome-HNK is simple and feasible, and it has stable physicochemical property, high encapsulation rate and higher
[关键词] 和厚朴酚；脂质体；肝肿瘤；人肝癌高转移细胞
Preparation of Honokiol Liposomes and Their Antitumor Activity in Vitro Wei Xiao1, Du Zixiu2*, Lu Ping1*
*Corresponding author：Du Zixiu, E-mail: zixiudu@sjtu.edu.cn Lu Ping, E-mail: luping.shanghai@163.com
Liposome-HNK with different lipid-drug ratio was prepared by thin film dispersed method （TFDM） and determination of
encapsulation efficiency （EE） was made; the particle size distribution of liposome-HNK and the time stability were
pharmaceutical effect.
honokiol（HNK）; liposome; liver neoplasms; highly metastatic human hepatocellular carcinoma cell
我国的原发性肝癌死亡率位居恶性肿瘤第 2 位［1］，其治愈率低，转移率高。检出时大多已属中晚
基金项目：国家自然科学基金（81300092） 共同通信作者：杜子秀，电子信箱：zixiudu@sjtu.edu.cn
To prepare the DOTAP/DOPE honokiol liposomes （liposome-HNK） and to explore their
physicochemical property and pharmacodynamics to treat human hepatocellular carcinoma cells lines （HCCLM3）.
［摘要］ 目的 制备（2,3-二油酰基-丙基）-三甲胺（1,2-dioleoyl-3-trimethylammonium-propane，DOTAP）/二油酰磷 脂酰乙醇胺（dioleoyl phosphoethanolamine, DOPE）包裹和厚朴酚脂质体，并对其理化性质和人肝癌高转移细胞（highly metastatic human hepatocellular carcinoma cell, HCCLM3）的药效学进行研究。方法 利用薄膜分散法制得和厚朴酚脂质 体，对不同药脂比的包封率进行考察；通过纳米粒度仪检测和厚朴酚脂质体的粒径电势分布、时间稳定性；通过生物透 射电镜（transmission electron microscopy, TEM）对其大小和形态学进行观测；用细胞膜红色荧光探针标记和厚朴酚脂质 体，探究HCCLM3细胞对脂质体摄取的时间依赖性；用WST-1和BD凋亡试剂盒检测和厚朴酚脂质体对HCCLM3细胞的 药效作用。结果 和厚朴酚脂质体粒径分布均匀，平均粒径为（112.30±0.78）nm，多分散系数为（0.24±0.00），电势为 （53.23±1.16）mV。药脂比为7%时包封率最高，高达（99.47±0.20）%，并且在4℃环境下可以长期稳定存在。和厚朴酚脂 质体的促凋亡水平明显强于原药，差异有统计学意义（ ＜0.05）。结论 和厚朴酚脂质体制备工艺简单易行，具有稳定 的理化性质和较高的包封率，同时优于和厚朴酚原药的药效作用。