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目的:把生物素接枝到泊洛沙姆上制备包载表柔比星(EPI)的生物素-泊洛沙姆(BP)胶束.方法:分别对包载EPI的BP胶束的粒径、Zeta电位、表面形态、载药量、包封率及药物释放等方面进行考察和表征.用骨髓白血病HL-60细胞株评估包载EPI的BP胶束的体外细胞毒性.裸鼠皮下注射HL-60细胞建立肿瘤模型,考察包载EPI的BP胶束抑制肿瘤的影响.结果:这些纳米粒子的尺寸约为100 nm.荧光显微镜观察得出生物素结合的胶束有助于细胞摄取.抑制肿瘤体积增长的顺序:包载EPI的BP胶束>包载EPI的单胺封端的泊洛沙姆(MATP)胶束>包载EPI的泊洛沙姆胶束>单纯EPI.结论:与非靶向胶束相比,BP胶束表现出显著的的抗肿瘤活性和低毒性.拥有增强通透性和滞留性(EPR)效应和肿瘤靶向两大优势, BP胶束可能发展成为一个新的运载化疗药物的途径.尚需进一步进行其他细胞实验和大动物实验证明该肿瘤靶向技术.“,”Objective:To prepare biotin-poloxamer(BP) conjugate micelles for epirubicin through biotin conjugated on poloxam-er. Methods:Epirubicin(EPI) was encapsulated in BP micelles. The EPI-loaded BP micelles were characterized by its particle size, zeta potential,surface morphology,as well as the efficiency of drug loading and drug encapsulation and drug release. Marrow leukemia HL-60 cells were used to evaluate the cell cytotoxicity of EPI-loaded BP micelles in vitro. The tumor model in nude mice was estab-lished through the subcutaneous injection of HL-60 cells, and then the inhibitory effect of EPI-loaded BP micelles on tumor volume growth was investigated.Results:It was found that the average particle size of EPI-loaded BP micelles was about 100 nm. In addition, the enhanced cellular uptake ability of EPI-loaded BP micelles was proved by fluorescence microscope observation. The efficiency order of the tumor volume growth inhibition was:EPI-loaded BP micelles > EPI-loaded MATP micelles> EPI-loaded poloxamer micelles>EPI. BP micelles showed significant antitumor activity and low toxicity when compared with the non-targeted micelles. Conclusion:With the advantages of EPR effect and tumor-targeting potential,BP conjugate micelles might be developed as a new system for chemo-therapeutics. However,the tumor targeting technique should be demonstrated further by the other cell experiments and large animal ex-periments.