pH-Responsive polymeric micelles have been investigated as drug carriers for chemotherapy. Ligand-mediated polymeric micelles, which can penetrate the target tumors due to their high binding affinity to a specific receptor on the surface of tumors, were developed to achieve targeted drug delivery. In this study, biotin-conjugated methoxypoly(ethylene glycol)-grafted-poly(β-amino ester) was prepared for active and pH-sensitive tumor targeting. These polymers were modified by cholesteryl chloroformate to improve the hydrophobicity of the micelle core. The structure of the biotin-conjugated polymer was confirmed by (1)H NMR spectroscopy, and the existence of biotin at the surface of the polymeric micelles was evaluated by an 4'-hydroxyazobenzene-2-carboxylic acid/avidin (HABA/avidin) binding assay at different pHs. The micelle properties were determined by dynamic light scattering and the result showed that the mean size of the polymeric micelles was approximately 20 nm. For cancer therapy, doxorubicin (DOX) was loaded into the polymeric micelles with a high loading efficiency. From the in vitro cellular uptake results, the biotin-conjugated polymeric micelles can effectively release doxorubicin at acidic tumor cells compared to the micelles without biotin. Overall, biotin-conjugated pH-responsive polymeric micelles have great potential to be used as drug carriers.
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