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用反相微乳液法和交联法制备了带负电的交联淀粉纳米颗粒(StNP),经过叶酸活性物质(FA-PEG-NH2)修饰,成功制备了叶酸-淀粉纳米颗粒(FA-PEG/StNP).原子力显微镜和Zeta-Sizer粒度仪检测表明所得颗粒的平均直径约为130nm.FA-PEG/StNP与抗癌药物多柔比星(DOX)经渗透结合,获得了载药叶酸-淀粉纳米颗粒,用紫外分光光度法检测发现纳米颗粒结合DOX的饱和量为28μg/mg,并对药物DOX具有明显的缓释效果.经过与肝癌细胞BEL7404共培养实验发现:载药FA-PEG/StNP和载药StNP的半致死浓度LC50比DOX的半致死浓度明显提高,表明FA-PEG/StNP和StNP都能显著降低DOX的细胞毒性.而含相同量药物DOX的载药FA-PEG/StNP和载药StNP与肝癌细胞BEL7404共培养发现:前者的细胞致死率是后者的3倍,结果证实了修饰在颗粒上的FA能显著提高颗粒对肝癌细胞的靶向作用,使更多药物作用于肿瘤细胞,提高了作用效果.所制备的叶酸-淀粉纳米颗粒具有药物缓释、靶向识别、降低毒副作用的特点,可以作为肿瘤靶向性药物载体.
The negatively charged cross-linked starch nanoparticles (StNP) were prepared by reverse microemulsion method and cross-linking method. Folic acid-starch nano-particles were successfully prepared by FA-PEG-NH2 modification. StNP) .Atomic force microscopy and Zeta-Sizer particle sizer showed that the average diameter of the resulting particles was about 130 nm.FFA-PEG / StNP was conjugated with the anticancer drug doxorubicin (DOX) The results showed that the saturation amount of nanoparticles bound DOX was 28μg / mg and the drug release was significantly slowed down by UV spectrophotometry.The results of co-culture with hepatoma BEL7404 showed that FA-PEG / StNP and The median lethal concentration (LC50) of LC50 of drug-loaded StNP was significantly higher than that of DOX, indicating that FA-PEG / StNP and StNP significantly decreased the cytotoxicity of DOX, while FA-PEG / StNP containing the same amount of drug DOX The co-culture of StNP and hepatoma cell BEL7404 found that the former cell death rate was three times that of the latter, and the results confirmed that the FA modified on the particle could significantly improve the targeting effect of the particle on the liver cancer cell and make more drugs act on the tumor Cells, to improve the effect of the prepared folic acid - Starch nanoparticles with drug release, targeted identification, reducing the side effects of toxic characteristics, can be used as a tumor targeting drug carrier.