甘草次酸纳米粒的制备、表征及其抗肿瘤活性研究

目的:制备和表征甘草次酸(GA)纳米粒,并评价其体外抗肿瘤活性。方法:以聚乙烯吡咯烷酮K30为载体,使用反溶剂沉淀-冷冻干燥法制备GA纳米粒。采用X射线衍射分析、红外光谱分析、差示扫描量热分析、粒度分析等方法对所制纳米粒进行表征;采用高效液相色谱法测定纳米粒中GA的溶解度和载药量;采用MTT法考察GA原料药及纳米粒(GA剂量均为12.5、25、50、100、200μmol/L)对人肝癌细胞HepG2的体外抑制活性并计算半数抑制浓度(IC50)。结果:所制纳米粒中GA的X射线衍射特征峰和红外特征吸收峰均消失,吸热峰发生改变。纳米粒的粒径为(194.88±23.52)nm,低于原料药的(2 592.33±207.51)nm;分散指数为0.24±0.04,高于原料药的0.15±0.03;纳米粒的平均载药量为15.99%;溶解度由原料药的(1.05±0.01)μg/mL升至(250.00±0.15)μg/mL。体外抗肿瘤试验结果显示,GA原料药200μmol/L组和纳米粒各剂量组的细胞存活率均较空白对照组显著降低,且GA纳米粒各剂量组(除12.5μmol/L组外)的细胞存活率均显著低于同剂量原...

Preparation,Characterization and Anti-tumor Activity Study of Glycyrrhetinic Acid Nanoparticles

OBJECTIVE:To prepare and characterize glycyrrhetinic acid(GA)nanoparticles,and to evaluate its in vitro anti-tumor activity.METHODS:Using PVP K30 as carrier,GA nanoparticles were prepared by anti-solvent precipitation and freeze-drying method.X-ray diffraction,infrared spectrum,differential scanning calorimetry and granularity analysis were used to characterize the nanoparticles;HPLC method was used to measure the solubility and drug-loading amount of GA in the nanoparticles.MTT method was used to assay the in vitro inhibition activity of GA raw material and nanoparticles(GA doses were 12.5,25,50,100,200μmol/L)on human liver cancer cell HepG2 and calculate its IC50.RESULTS:The characteristic peaks of X-ray diffraction and infrared absorption of GA disappeared in the nanoparticles and the endothermic peak changed.The particle size of the nanoparticles was(194.88±23.52)nm,which was lower than(2592.33±207.51)nm of raw material.The dispersion index was 0.24±0.04,which was higher than 0.15±0.03 of raw material.The average drug-loading amount of GA was 15.99%.Moreover,the solubility of nanoparticles increased from(1.05±0.01)μg/mL to(250.00±0.15)μg/mL.The results of antitumor test in vitro showed that the cell survival rates in the group of GA raw material 200μmol/L and GA nanoparticles groups were significantly lower than that in blank control group,and the cell survival rates of GA nanoparticles groups(except for 12.5μmol/L group)were significantly lower than that of same dose group of raw material(P<0.01).IC50 of GA nanoparticles was 86.3μmol/L,which was lower than 364.4μmol/L of raw material.CONCLUSIONS:GA nanoparticles are prepared successfully;the prepared nanoparticles have small size and uniform distribution,and the solubility are increased and antitumor activity in vitro are enhanced.