中国药房2016，Vol.27Issue(31)：4425-4428,4.DOI:10.6039/j.issn.1001-0408.2016.31.31
地塞米松纳米胶束的制备及体外抗肿瘤作用研究
Preparation of Dexamethasone Nano-micelles and Study on Its in vitro Anti-tumor Effect
摘要
Abstract
OBJECTIVE:To prepare Dexamethasone(Dex)nano-micelles(called Dex micelles for short),and to study its in vitro anti-tumor effect. METHODS:Using γ-PGA as carrier,DMSO as organic solvent,Dex micelles were prepared by dialysis method. The morphology,particle size,Zeta potential,PDI,CMC,drug-loading amount and entrapment efficiency (EE) of mi-celle were observed and detected. Drug release of Dex micelles and Dex were compared under pH 5.5,7.4. The effects of free Dex,γ-PGA,Dex micelles and prednisolone(positive control)(0.05,0.1,0.2,0.5,1.0 μmol/ml)on the survival rate of human lung adenocarcinoma A549 cells were compared. The uptake amount of A549 cells to 0.5 μmol/ml Dex micelles and free Dex were compared at 4,37 ℃. RESULTS:Prepared Dex micelles were spheroidal and completely round with particle size of(76.25±3.74) nm,Zeta potential of 5.0 mV,PDI of 0.163 ± 0.38,CMC of 7.609 μg/ml,drug-loading amount of (9.56 ± 0.92)% and EE of (89.25 ± 1.36)%. Compared with free Dex,the duration of drug release for Dex micelles prolonged under pH 5.5,7.4. When the concentration ranged 0.05-0.2 μmol/ml,the effects of free Dex,γ-PGA,Dex micelles and prednisolone on cellular survival rate had no statistically significant difference(P>0.05). When the concentration was 0.5,1.0 μmol/ml,survival rate of A549 cells treat-ed with Dex micelles was significantly lower than that treated with free Dex or prednisolone (P<0.05). At 4 ℃,the uptake amount of A549 cells to Dex micelles and free Dex had no statistically significant difference (P>0.05). At 37 ℃,the uptake amount of A549 cells to Dex micelles was significantly higher than that of cells to free Dex,and that of A549 cells to Dex micelles and free Dex at 4 ℃. CONCLUSIONS:Prepared Dex micelles can prolong the duration of drug release of Dex,and decrease the survival rate of A549 cells and cellular uptake efficacy.关键词
地塞米松/γ-聚谷氨酸/纳米胶束/制备/抗肿瘤Key words
Dexamethasone/γ-glutamic acid/Nano-micelles/Preparation/Anti-tumor分类
医药卫生引用本文复制引用
侯杰荣,侯思奎,杨欣,姚小东..地塞米松纳米胶束的制备及体外抗肿瘤作用研究[J].中国药房,2016,27(31):4425-4428,4.基金项目
四川省教育厅重点项目 （）
