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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(P<0.05)。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(P<0.05)。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。
OBJECTIVE: To prepare curcumin (Cur) poly-lactic-co-glycolic acid (PL-PLGA-NPs) nanoparticles and investigate their physico-chemical properties, 3 cells in vitro. Methods: Cur-PLGA-NPs were prepared by emulsion-solvent evaporation method. The morphology of nanoparticles was observed by transmission electron microscopy. The particle size and distribution of Cur-PLGA-NPs were analyzed by dynamic laser particle size analyzer. Drug loading rate and entrapment efficiency were determined by ultracentrifugation. (CCK-8) assay was used to detect the proliferation of PC-3 cells. Proliferation of PC-3 cells was detected by flow cytometry (FCM). Cell ultrastructure was observed by transmission electron microscopy Compare with simple Cur. Results: Curcumin nanoparticles were round or oval under the transmission electron microscope. The mean diameter of the nanoparticles was (165.36 ± 24.21) nm. The entrapment efficiency was (83.05 ± 1.07)% and the drug loading rate was (10.87 ± 0.58)%. Drug release test showed that the release rate of Cur-PLGA-NPs in the first 24 h exceeded 44.02%, and the cumulative release rate reached 84.81% after 10 days. The cell inhibitory rate (9.38% -83.62% vs.10.56% -89.53%) of PC-3 cells treated with 5 ~ 40μmol / L Cur and Cur-PLGA-NPs for 24-72h. The Cur and PLGA-NPs concentrations of 20μmol / L and 40μmol / L were significantly different between the two groups (P <0.05). FCM showed the same concentration of experimental group apoptosis rate compared with the control group, the difference was statistically significant (P <0.05). Transmission electron microscopy showed that Cur-PLGA-NPs showed typical apoptotic morphology after PC-3 cells were treated with Cur-PLGA-NPs. CONCLUSION: Cur-PLGA-NPs has good drug release characteristics and enhances the cytotoxicity of Cur on PC-3 cells in vitro and inhibits proliferation.