Terminal modification of polymeric micelles with π-conjugated moieties for efficient anticancer drug delivery. (December 2015)

• Record Type: Journal Article
• Authors: Liang, Yan; Deng, Xin; Zhang, Longgui; Peng, Xinyu; Gao, Wenxia; Cao, Jun; Gu, Zhongwei; He, Bin
• Is Part Of: Biomaterials. Volume 71(2015)
• Page Start: 1
• Page End: 10
• Publication Date: 2015-12
• Subjects: Polymeric micelle -- Conjugated moieties -- Drug delivery -- Chrysin -- π-π stacking interaction; Biomedical materials -- Periodicals; Biocompatible Materials -- Periodicals; Biomatériaux -- Périodiques; 610.28
• DOI: 10.1016/j.biomaterials.2015.08.032
• Languages: English
• ISSNs: 0142-9612

Abstract

Abstract: 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 π-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 π-π stacking interaction between doxorubicin (DOX) and polymeric micelles. The modification of π-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·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.