姜黄素-PLGA纳米粒的制备及对人前列腺癌PC-3细胞的体外研究

发布时间：2018-09-12 07:38

【摘要】：目的:制备姜黄素(curcumin,Cur)聚乳酸-羟基乙酸(poly lactic-co-glycolic acid,PLGA)纳米粒(Cur-PLGA-NPs),并考察其理化性质、体外释药特性及对PC-3细胞的体外影响。方法:运用乳化-溶剂挥发法制备Cur-PLGA-NPs,利用透射电镜观察纳米粒的外观形态;动态激光粒度仪分析其粒径大小及分布;超速离心法测定载药率和包封率;透析法观测体外释放效果;采用CCK-8比色法检测其对前列腺癌PC-3细胞的增殖抑制情况,流式细胞仪(FCM)进行细胞凋亡率检测,透射电镜观察细胞超微结构,并与单纯Cur进行比较。结果:透射电镜下姜黄素纳米粒呈圆形或椭圆形,平均粒径为(165.36±24.21)nm,包封率为(83.05±1.07)%,载药率为(10.87±0.58)%,体外药物释放试验显示,Cur-PLGA-NPs在最初的24 h内释放率超过44.02%,10 d累计释放率达84.81%。5~40μmol/L Cur及Cur-PLGA-NPs作用PC-3细胞24~72 h后细胞的抑制率(9.38%~83.62%vs.10.56%~89.53%)。浓度为20μmol/L和40μmol/L的Cur和Cur-PLGA-NPs组间比较,差异有统计学意义(P0.05)。FCM显示同浓度实验组细胞凋亡率与对照组比较,差异具有统计学意义(P0.05)。透射电镜显示Cur-PLGA-NPs作用PC-3细胞后出现典型的细胞凋亡形态学特征。结论:Cur-PLGA-NPs具有良好的药物缓释特性,增强了Cur对PC-3细胞的体外杀伤和抑制增殖能力。
[Abstract]:Aim: to prepare curcumin (curcumin,Cur) polylactic acid-glycolic acid (poly lactic-co-glycolic acid,PLGA) nanoparticles (Cur-PLGA-NPs) and investigate its physicochemical properties, drug release characteristics in vitro and its effect on PC-3 cells in vitro. Methods: Cur-PLGA-NPs, was prepared by emulsification-solvent volatilization method, the morphology of nanoparticles was observed by transmission electron microscope, the particle size and distribution were analyzed by dynamic laser particle size analyzer, the drug loading rate and encapsulation efficiency were determined by ultracentrifugation. CCK-8 colorimetric assay was used to detect the inhibition of proliferation of prostate cancer PC-3 cells, flow cytometry (FCM) was used to detect the apoptosis rate, transmission electron microscope was used to observe the ultrastructure of the cells, and compared with Cur alone. Results: curcumin nanoparticles were round or oval under transmission electron microscope. The average particle size was (165.36 卤24.21) nm, entrapment efficiency was (83.05 卤1.07), and the drug loading rate was (10.87 卤0.58). The in vitro drug release test showed that the cumulative release rate of Cur-PLGA-NPs in the first 24 hours was more than 44.022.The cumulative release rate of PC-3 cells reached 84.81.540 渭 mol/L Cur and the inhibition rate of PC-3 cells after 2472 hours treated by Cur-PLGA-NPs (9.3883.62vs.10.5659.53%). The difference between Cur and Cur-PLGA-NPs groups with 20 渭 mol/L and 40 渭 mol/L was statistically significant (P0.05). FCM showed that the apoptotic rate of the same concentration group was significantly higher than that of the control group (P0.05). Transmission electron microscopy (TEM) showed that typical apoptotic morphological features of PC-3 cells appeared after Cur-PLGA-NPs treatment. Conclusion: the Cur has good sustained release properties and enhances the ability of Cur to kill and inhibit the proliferation of PC-3 cells in vitro.
【作者单位】：贵州医科大学附属医院泌尿外科;
【基金】：国家自然科学基金(30860284) 贵阳市科技攻关(2009筑科农合同字第3-009号) 贵州省教育厅重点项目(黔教科2007027)
【分类号】：R737.25

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