Objective To study the anti-tumor activity of chemical conjugation of doxorubicin in polymeric micelles ( DOX-P ) in vitro. Methods The structure of DOX-P was investigated by NMR. The Tm and Tc of DOX-P were observed by DSC. The A549 cellular uptake was detected by fluorescence microscopy and flow cytometry. The cytotoxic activity of the micelles and free DOX against A549/DOX cells was compared by MTT method. Results Doxorubicin was distributed in the micelle core. The Tm and Tc of DOX-P were decreased. Fluorescence microscope observation and flow cytometry analysis supported the enhanced cellular uptake and enhanced DOX anti-tumor activity. The cytotoxic activity of the micelles against A549/DOX cells was greater than that of free DOX. Conclusion The micelle is prepared successfully. Better anti-tumor activity of DOX-P in vitro can be observed, which can circumvent the multi-drug resistance ( MDR ) of A549/DOX cells.%目的 制备泊洛沙姆多柔比星(阿霉素)偶联物(DOX-P)胶束并考察其体外抗肿瘤活性.方法 核磁光谱法考察泊洛沙姆多柔比星偶联物胶束结构,差示扫描量热法(差热分析,DSC)观察聚合物的Tm和TC.流式细胞术和荧光显微术观察人肺腺癌细胞A549对DOX-P胶束的摄取量,MTT法比较游离DOX和DOX-P胶束对A549/DOX细胞的细胞毒性.结果 核磁光谱法证实多柔比星处于胶束核心,DSC表明DOX-P 的Tm和TC降低,荧光显微镜观察和流式细胞仪分析均支持胶束能够增强耐药细胞对多柔比星的吸收,MTT法表明DOX-P胶束对耐多柔比星的人肺腺癌细胞A549/DOX的毒性大于游离多柔比星.结论 所制备的DOX-P胶束偶联成功,体外抗肿瘤活性良好,且能克服A549/DOX细胞的多药耐药性.
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