cRGD-Functionalized Polymer Micelles for Targeted Doxorubicin Delivery

Authors

  • Norased Nasongkla,

    1. 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
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    • These authors contributed equally to this work

  • Xintao Shuai Dr.,

    1. 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
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    • These authors contributed equally to this work

  • Hua Ai Dr.,

    1. 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
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  • Brent D. Weinberg,

    1. 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
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  • John Pink Dr.,

    1. Department of Radiation Oncology, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA
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  • David A. Boothman Prof.,

    1. Department of Radiation Oncology, Case Western Reserve University, 10 900 Euclid Avenue, Cleveland, Ohio 44 106, USA
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  • Jinming Gao Prof. Dr.

    1. 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
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  • This 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.

Abstract

original image

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.

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