Polymeric micelles for cancer therapy: 3 C's to enhance efficacy

During the past few years, polymeric micelles (PM), which can accommodate various different hydrophobic anticancer agents within their core, have received substantial attention as EPR-targeted drug delivery systems for cancer therapy. PM can be modified to confer several attractive properties, such as stimuli-responsiveness and active targeting. However, PM still face challenges of instability in systemic circulation and premature drug leakage, often leading to improper in vivo efficacy. These shortcomings have triggered research toward the development of next-generation PM. Here, we propose a 3C approach for making PM more effective, encompassing (core-) crosslinking, covalent drug entrapment and integration therapies based on intrinsically active targeting ligands, and we show that the integration of these three concepts within one PM formulation leads to nanomedicines with substantially improved in vivo efficacy. (C) 2012 Elsevier Ltd. All rights reserved.