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甘草次酸纳米粒的制备、表征及其抗肿瘤活性研究
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| 篇名： | 甘草次酸纳米粒的制备、表征及其抗肿瘤活性研究 |
| TITLE： | Preparation，Characterization and Anti-tumor Activity Study of Glycyrrhetinic Acid Nanoparticles |
| 摘要： | 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（2592.33±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料药组（P＜0.01）；GA纳米粒的IC50值为86.3μmol/L，低于原料药的364.4μmol/L。结论：成功制得GA纳米粒；所制纳米粒粒径小且分布均匀，溶解度增大且体外抗肿瘤活性增强。 |
| ABSTRACT： | OBJECTIVE：To prepare and characterize glycyrrhetinic acid （GA）nanoparticles，and to evaluate its in vitro anti-tumor activity. METHODS ：Using PVP K 30 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 12.5，25，50，100，200 μmol/L）on human liver cancer cell HepG 2 and calculate its IC 50. 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 （2 592.33±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 200 μmol/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 12.5 μmol/L group）were significantly lower than that of same dose group of raw material （P＜0.01）. IC 50 of GA nanoparticles was 86.3 μmol/L，which was lower than 364.4 μmol/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. |
| 期刊： | 2020年第31卷第13期 |
| 作者： | 张丽娟，喻红梅，张勇，龚宁波 |
| AUTHORS： | ZHANG Lijuan，YU Hongmei ，ZHANG Yong，GONG Ningbo |
| 关键字： | 甘草次酸纳米粒；反溶剂沉淀-冷冻干燥法；制备；表征；抗肿瘤活性；HepG2细胞 |
| KEYWORDS： | Glycyrrhetinic acid nanoparticle；Anti-solvent |
| 阅读数： | 376 次 |
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