Construction and in vitro and in vivo Preliminary Evaluation of Biotin-poloxamer Conjugate Polymeric Mi-celles for Epirubicin
- VernacularTitle:包载表柔比星的生物素化泊洛沙姆聚合物胶束的构建与体内外初步评价
- Author:
Xiaoxiao LIN
1
;
Guangyong LIN
;
Zhengfeng LIN
Author Information
1. 温州医科大学附属第二医院 浙江温州325027
- Keywords:
Biotin-poloxamer conjugate;
Epirubicin;
Micelles
- From:
China Pharmacist
2018;21(2):241-245
- CountryChina
- Language:Chinese
-
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 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.
