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目的:本研究旨在构建一种转铁蛋白修饰负载阿霉素(DOX)的磁纳米粒靶向递药系统,以提高阿霉素作用的靶向性。方法:采用化学共沉淀法制备转铁蛋白修饰负载阿霉素的磁性纳米粒(DOX@MNP),采用zeta电位及纳米粒度分析仪测定DOX@MNP的粒径及其zeta电位,透析法评价DOX@MNP的体外释药特征。通过MTT实验,研究DOX@MNP与游离DOX对A549细胞的细胞毒性,通过激光共聚焦显微镜和流式细胞仪观察A549细胞对DOX@MNP与游离DOX的摄取情况。结果:DOX@MNP的释药具有p H依赖性。MTT实验结果显示,DOX@MNP与游离DOX具有相当的细胞毒性;激光共聚焦显微镜和流式细胞仪检测结果显示A549细胞对DOX和DOX@MNP的摄取没有明显差异。结论:本文构建了一种转铁蛋白修饰包载阿霉素的磁纳米粒,体外结果显示其具有与游离DOX相当的细胞毒性,为进一步进行体内实验奠定了基础。
OBJECTIVE: This study aimed to construct a magnetic nanoparticle targeted delivery system with transferrin modified with doxorubicin (DOX) to enhance the targeting of doxorubicin. METHODS: DOX @ MNP was prepared by chemical coprecipitation with transferrin to prepare doxorubicin-loaded magnetic nanoparticles (DOX @ MNP). The particle size and zeta potential of DOX @ MNP were measured by zeta potential and nanoparticle analyzer. Dialysis was used to evaluate DOX @ MNP in vitro release characteristics. The cytotoxicity of DOX @ MNP and free DOX on A549 cells was studied by MTT assay. The uptake of DOX @ MNP and free DOX by A549 cells was observed by laser confocal microscopy and flow cytometry. Results: DOX @ MNP release was p H-dependent. The results of MTT showed that DOX @ MNP and DOX had considerable cytotoxicity. Confocal laser scanning microscopy and flow cytometry showed that A549 cells did not show significant uptake of DOX and DOX @ MNP. CONCLUSION: In this paper, we constructed a magnetic nanoparticle coated with transferrin and adriamycin-loaded, and showed cytotoxicity comparable to that of free DOX in vitro, which laid the foundation for further in vivo experiments.