HPMA Copolymer–Doxorubicin–Gadolinium Conjugates: Synthesis, Characterization, and in vitro Evaluation

Authors

  • Bahar Zarabi,

    1. Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland 21201, USA
    2. Center for Nanomedicine and Cellular Delivery, University of Maryland, Baltimore, Maryland 21201, USA
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  • Anjan Nan,

    1. Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland 21201, USA
    2. Center for Nanomedicine and Cellular Delivery, University of Maryland, Baltimore, Maryland 21201, USA
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  • Jiachen Zhuo,

    1. Department of Radiology, University of Maryland, Baltimore, Baltimore, Maryland 21201, USA
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  • Rao Gullapalli,

    1. Center for Nanomedicine and Cellular Delivery, University of Maryland, Baltimore, Maryland 21201, USA
    2. Department of Radiology, University of Maryland, Baltimore, Baltimore, Maryland 21201, USA
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  • Hamidreza Ghandehari

    Corresponding author
    1. Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland 21201, USA
    2. Center for Nanomedicine and Cellular Delivery, University of Maryland, Baltimore, Maryland 21201, USA
    3. Current Address: Departments of Pharmaceutics and Pharmaceutical Chemistry and Bioengineering, University of Utah, Salt Lake City, Utah 84108, USA
    • Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland 21201, USA. Fax: (+1) 801 585-0575
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Abstract

This study describes the synthesis, characterization, and in vitro evaluation of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer–gadolinium (Gd)–doxorubicin (Dox) conjugates. Copolymers of HPMA were derivatized to incorporate side chains for Gd chelation and Dox conjugation. The conjugates were characterized by their side chain contents, T1 relaxivity (r1), stability, and in vitro cytotoxicity. High stability and relaxivity of these conjugates coupled with low toxicity show their potential for monitoring the in vivo fate of HPMA-based drug delivery systems by magnetic resonance imaging techniques.

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