期刊
BIOMATERIALS
卷 71, 期 -, 页码 1-10出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.biomaterials.2015.08.032
关键词
Polymeric micelle; Conjugated moieties; Drug delivery; Chrysin; pi-pi stacking interaction
资金
- National Science Foundation of China [51222304, 31170921, 51403137]
- Ministry of Education of China [20130181110038]
- Sichuan University [2014SCU11015]
High drug loading content is the critical factor to polymeric micelles for efficient chemotherapy. Small molecules of cinnamic acid, 7-carboxymethoxy coumarin and chrysin with different pi-conjugated moieties were immobilized on the terminal hydroxyl groups of PCL segments in mPEG-PCL micelles to improve drug loading content via the evocation of pi-pi stacking interaction between doxorubicin (DOX) and polymeric micelles. The modification of pi-conjugated moieties enhanced the capability of crystallization of mPEG-PCL block copolymers. The drug loading content increased dramatically from 12.9% to 25.5% after modification. All the three modified mPEG-PCL micelles were nontoxic to cells. Chrysin modified polymeric micelles exhibited the most efficient anticancer activity. The in vivo anticancer activity of 10 mg/kg DOX dose of chrysin modified micelle formulation for twice injections was comparable to that of 5 mg/kg dose of free DOX center dot HCl for four injections under the circumstance of same total DOX amount. The systemic toxicity of DOX loaded chrysin modified micelles was significantly reduced. This research provided a facile strategy to achieve polymeric micelles with high drug loading content and efficient anticancer activity both in vitro and in vivo. (C) 2015 Elsevier Ltd. All rights reserved.
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