cRGD-Functionalized Polymer Micelles for Targeted Doxorubicin Delivery

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 t...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2004-11, Vol.43 (46), p.6323-6327
Main Authors: Nasongkla, Norased, Shuai, Xintao, Ai, Hua, Weinberg, Brent D., Pink, John, Boothman, David A., Gao, Jinming
Format: Article
Language:English
Subjects:
antitumor agents
bioorganic chemistry
Biopolymers - chemistry
Cell Line, Tumor
Cyclization
Doxorubicin - administration & dosage
drug delivery
Drug Delivery Systems
Humans
Magnetic Resonance Spectroscopy
Micelles
Microscopy, Atomic Force
Molecular Structure
Oligopeptides - chemistry
peptides
Sarcoma, Kaposi - pathology
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Summary: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200460800