High Drug Loading and Sub-Quantitative Loading Efficiency of Polymeric Micelles Driven by Donor–Receptor Coordination Interactions

• DOI: 10.1021/jacs.7b12776
• Publication Date: 2018-01-13T20:09:16Z
• Authors: Shixian Lv; Yuchen Wu; Kaimin Cai; Hua He; Yongjuan Li; Min Lan; Xuesi Chen; Jianjun Cheng; Lichen Yin
• Keywords: Phenylboronic acid; Camptothecin

Polymeric micelles are extensively used for the delivery of hydrophobic drugs, which, however, suffer from unsatisfactory drug loading, colloidal uniformity, formulation stability, and release. Herein, we demonstrate a convenient strategy to prepare with ultrahigh loading via incorporation polymer-drug coordination interactions. An amphiphilic copolymer containing pendant phenylboronic acid as electron acceptor unit was synthesized, which afforded donor-acceptor doxorubicin obtain (∼50%), nearly quantitative efficiency (>95%), uniform size, stability. Besides, encapsulated can be effectively selectively released in response high reactive oxygen species levels cancer cells, potentiated anticancer efficacy reduced systemic toxicity. Apart doxorubicin, current platform could extended other drugs electron-donating groups (e.g., epirubicin irinotecan), rendering simple robust enabling polymeric cancer-specific