隐丹参酮纳米混悬剂的制备及其抗肿瘤活性  

Preparation and anti-tumor activity of cryptotanshinone nanosuspensions

作　　者：李晓婷 决利利 郝海军 王世广 LI Xiao-ting;JUE Li-li;HAO Hai-jun;WANG Shi-guang(School of Medicine,Zhengzhou University of Industrial Technology,Zhengzhou 451150,China;China State Institute of Pharmaceutical Industry,Shanghai 201203,China)

机构地区：[1]郑州工业应用技术学院医学院,河南郑州451150 [2]中国医药工业研究院,上海201203

出　　处：《中成药》2021年第1期6-10,共5页Chinese Traditional Patent Medicine

基　　金：河南省科技攻关项目(202102310417)。

摘　　要：目的制备隐丹参酮纳米混悬剂,并评价其抗肿瘤活性。方法高压均质法制备纳米混悬剂后,测定其平均粒径、Zeta电位、形态、稳定性、体外释药,MTT法检测它对人胃癌细胞SGC-7901的抑制作用。结果所得纳米混悬剂呈球形,平均粒径为104.15 nm,PDI为0.014,Zeta电位为-36.3 mV;室温下30 d内粒径无明显变化,在1.8%氯化钠溶液中的粒径变化程度小于空白血浆中;12 h内累积释放度达64.28%,之后呈明显缓释特征,体外释药符合Higuchi模型(R2=0.9817)。纳米混悬剂对SGC-7901细胞的抑制率高于原料药(P<0.05,P<0.01),并呈浓度、时间依赖性。结论纳米混悬剂可增强隐丹参酮稳定性和抗肿瘤活性。AIM To prepare cryptotanshinone nanosuspensions and to evaluate their anti-tumor activity.METHODS High-pressure homogenization method was applied to preparing nanosuspensions,after which the particle size,Zeta potential,morphology and in vitro drug release were determined,and their inhibitory effects on human gastric cancer cells SGC-7901 were detected by MTT.RESULTS The obtained spherical nanosuspensions demonstrated the average particle size of 104.15 nm,PDI of 0.014 and Zeta protential of-36.3 mV.The particle size displayed no obvious change within 30 d at room temperature,whose variation degree in 1.8%sodium chloride solution was smaller than that in the blank plasma.The accumulative release rate reached 64.28%within 12 h and then exhibited sustained-release characteristics,and the in vitro drug release accorded with Higuchi model(R2=0.9817).The inhibitory rate of nanosuspensions on SGC-7901 cells was higher than that of raw medicine(P<0.05,P<0.01)in concentration-dependent and time-dependent manners.CONCLUSION Nanosuspensions can enhance the stability and anti-tumor activity of cryptotanshinone.

关 键 词：隐丹参酮 纳米混悬剂 制备 抗肿瘤活性 高压均质法 SGC-7901细胞 MTT 

分 类 号：R944[医药卫生—药剂学]