期刊
POLYMER CHEMISTRY
卷 5, 期 3, 页码 854-861出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3py00861d
关键词
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资金
- National Science Fund for Distinguished Young Scholars [51025312]
- National Basic Research Program of China [2011CB606203]
- Research Fund for the Doctoral Program of Higher Education of China [20110101110037, 20120101130013]
- Open Project of State Key Laboratory of Supramolecular Structure and Materials [skIssm201316]
- [NSFC-21174126]
- [51303154]
- [51333005]
A biodegradable and endosomal pH-sensitive polymeric prodrug poly(5-methyl-5-allyloxycarbonyl-1,3-dioxan-2-one)-graft-12-acryloyloxy dodecyt phosphorylcholine-co-6-maleimidocaproyl-doxorubicin (PMAC-graft-(ADPC-co-Mal-DOX) was synthesized by ring-opening polymerization CROP) and click reaction. DOX was conjugated to the polymer by hydrazone bonds which would result in a pH-sensitive controlled release of drug. The polymeric prodrug can form a self-assembled micellar structure which was confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM). Flow cytometry and fluorescence microscopy results demonstrated that prodrug micelles could be internalized by cancer cells remarkably. In vitro drug release studies showed that the release of DOX was faster at endosomal pH (pH = 5.0) than at normal physiological environment (pH = 7.4). Moreover, this prodrug exhibited high cytotoxicity against HepG2 cells and HeLa cells, indicating its great potential for cancer therapy.
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