cRGD-Functionalized Polymer Micelles for Targeted Doxorubicin Delivery†
Norased Nasongkla
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
These authors contributed equally to this work
Search for more papers by this authorXintao Shuai Dr.
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
These authors contributed equally to this work
Search for more papers by this authorHua Ai Dr.
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
Search for more papers by this authorBrent D. Weinberg
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
Search for more papers by this authorJohn Pink Dr.
Department of Radiation Oncology, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA
Search for more papers by this authorDavid A. Boothman Prof.
Department of Radiation Oncology, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA
Search for more papers by this authorJinming Gao Prof. Dr.
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
Search for more papers by this authorNorased Nasongkla
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
These authors contributed equally to this work
Search for more papers by this authorXintao Shuai Dr.
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
These authors contributed equally to this work
Search for more papers by this authorHua Ai Dr.
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
Search for more papers by this authorBrent D. Weinberg
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
Search for more papers by this authorJohn Pink Dr.
Department of Radiation Oncology, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA
Search for more papers by this authorDavid A. Boothman Prof.
Department of Radiation Oncology, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA
Search for more papers by this authorJinming Gao Prof. Dr.
Department of Biomedical Engineering, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA, Tel: (+1) 216-368-1083, Fax: (+1) 216-368-4969
Search for more papers by this authorThis research is supported by the National Institutes of Health (R01-CA-90 696). N.N. acknowledges the Royal Thai Government for a predoctoral fellowship support. X.T.S. acknowledges fellowship support from the Ohio Biomedical Research and Technology Trust fund. We thank Dr. Steven Eppell and Zhilei Liu for their help with atomic force microscopy.
Graphical Abstract
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.
Supporting Information
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