Biodegradable block copolymer-doxorubicin conjugates via different linkages: preparation, characterization, and in vitro evaluation.
作者： Xiuli Hu , Shi Liu , Yubin Huang , Xuesi Chen , Xiabin Jing
DOI: 10.1021/BM100458N
关键词:
摘要: Doxorubicin (Dox) was conjugated onto a biodegradable block copolymer methoxy-poly(ethylene glycol)-block-poly(lactide-co-2,2-dihydroxymethylpropylene carbonate (mPEG-b-P(LA-co-DHP)) via carbamate linkage and an acid-labile hydrazone linkage, respectively. Mutifunctional mixed micelles consisting of Dox-containing mPEG-b-P(LA-co-DHP/Dox) folic acid-containing mPEG-b-P(LA-co-DHP/FA) were successfully prepared by coassembling the two component copolymers. The had well-defined core shell structure their diameters in range 70-100 nm. Both Dox-conjugates (via or linkage) showed pH-dependent release behavior, with more pH-sensitivity compared to those linkage. vitro cell uptake experiment CLSM flow cytometry preferential internalization FA-containing human ovarian cancer line SKOV-3 than that without FA. Flow cytometric analysis conducted reveal enhanced apoptosis caused micelles. These results suggested these containing both chemotherapeutic targeting ligand could be promising nanocarrier for drugs cells releasing drug molecules inside cells.
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