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Biodegradable Block Copolymer-Doxorubicin Conjugates via Different Linkages: Preparation, Characterization, and In Vitro Evaluation
Hu, Xiuli; Liu, Shi; Huang, Yubin; Chen, Xuesi; Jing, Xiabin
2010-08-01
Source PublicationBIOMACROMOLECULES
ISSN1525-7797
Volume11Issue:8Pages:2094-2102
AbstractDoxorubicin (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 a carbamate linkage and an acid-labile hydrazone linkage, respectively. Mutifunctional mixed micelles consisting of Dox-containing copolymer mPEG-b-P(LA-co-DHP/Dox) and folic acid-containing copolymer mPEG-b-P(LA-co-DHP/FA) were successfully prepared by coassembling the two component copolymers. The mixed micelles had well-defined core shell structure and their diameters were in the range of 70-100 nm. Both Dox-conjugates (via carbamate or hydrazone linkage) showed pH-dependent release behavior, and the micelles with hydrazone linkage showed more pH-sensitivity compared to those with carbamate linkage. The in vitro cell uptake experiment by CLSM and flow cytometry showed preferential internalization of FA-containing micelles by human ovarian cancer cell line SKOV-3 than that without FA. Flow cytometric analysis was conducted to reveal the enhanced cell apoptosis caused by the FA-containing micelles. These results suggested that these micelles containing both chemotherapeutic and targeting ligand could be a promising nanocarrier for targeting the drugs to cancer cells and releasing the drug molecules inside the cancer cells.
DOI10.1021/bm100458n
Indexed BySCI
Language英语
WOS IDWOS:000280583400026
PublisherAMER CHEMICAL SOC
Citation statistics
Cited Times:120[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.iccas.ac.cn/handle/121111/69262
Collection中国科学院化学研究所
Corresponding AuthorJing, Xiabin
AffiliationChinese Acad Sci, Changchun Inst Appl Chem, State Key Lab Polymer Phys & Chem, Changchun 130022, Peoples R China
Recommended Citation
GB/T 7714
Hu, Xiuli,Liu, Shi,Huang, Yubin,et al. Biodegradable Block Copolymer-Doxorubicin Conjugates via Different Linkages: Preparation, Characterization, and In Vitro Evaluation[J]. BIOMACROMOLECULES,2010,11(8):2094-2102.
APA Hu, Xiuli,Liu, Shi,Huang, Yubin,Chen, Xuesi,&Jing, Xiabin.(2010).Biodegradable Block Copolymer-Doxorubicin Conjugates via Different Linkages: Preparation, Characterization, and In Vitro Evaluation.BIOMACROMOLECULES,11(8),2094-2102.
MLA Hu, Xiuli,et al."Biodegradable Block Copolymer-Doxorubicin Conjugates via Different Linkages: Preparation, Characterization, and In Vitro Evaluation".BIOMACROMOLECULES 11.8(2010):2094-2102.
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