cRGD-Functionalized Polymer Micelles for Targeted Doxorubicin Delivery (pages 6323–6327)
Norased Nasongkla, Xintao Shuai, Hua Ai, Brent D. Weinberg, John Pink, David A. Boothman and Jinming Gao
Version of Record online: 23 NOV 2004 | DOI: 10.1002/anie.200460800
Targeting micelles: Cyclic pentapeptide cRGDfK (red triangles), which targets integrin αvβ3, was conjugated to the outer shell of doxorubicin-loaded (red hexagons) polymeric micelles by using a post-micelle modification method. The modified micelles significantly enhanced their internalization (up to 30-fold) by receptor-mediated endocytosis in tumor endothelial cells overexpressing the αvβ3 receptor.