Terminal modification of polymeric micelles with p-conjugated moieties for efficient anticancer drug delivery.

Biomaterials

PubMedID: 26310358

Liang Y, Deng X, Zhang L, Peng X, Gao W, Cao J, Gu Z, He B. Terminal modification of polymeric micelles with p-conjugated moieties for efficient anticancer drug delivery. Biomaterials. 2015;711-10.
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 p-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 p-p stacking interaction between doxorubicin (DOX) and polymeric micelles. The modification of p-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.