Construction and in vitro and in vivo Preliminary Evaluation of Biotin-poloxamer Conjugate Polymeric Mi-celles for Epirubicin / 中国药师

ABSTRACT

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 wasEPI-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.