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Issue 11, 2017
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HDAC inhibitor conjugated polymeric prodrug micelles for doxorubicin delivery

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Abstract

Amphiphilic diblock copolymers bearing histone deacetylase inhibitors (HDACis) (4-phenyl butyric acid and valproic acid) were synthesized by ring-opening polymerization of γ-4-phenylbutyrate-ε-caprolactone (PBACL), γ-valproate-ε-caprolactone (VPACL), and ε-caprolactone (CL) from a poly(ethylene glycol) (PEG) macroinitiator. These amphiphilic diblock copolymers self-assembled into stable pro-drug micelles and demonstrated excellent biocompatibility. High loading of doxorubicin (DOX) up to 5.1 wt% was achieved. Optimized micelles enabled sustained drug release in a concentration-dependent manner over time to expand the therapeutic window of cytotoxic small molecule drugs.

Graphical abstract: HDAC inhibitor conjugated polymeric prodrug micelles for doxorubicin delivery

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Publication details

The article was received on 22 Nov 2016, accepted on 18 Feb 2017 and first published on 20 Feb 2017


Article type: Paper
DOI: 10.1039/C6TB03038F
Citation: J. Mater. Chem. B, 2017,5, 2106-2114
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    HDAC inhibitor conjugated polymeric prodrug micelles for doxorubicin delivery

    S. A. Senevirathne, K. E. Washington, J. B. Miller, M. C. Biewer, D. Oupicky, D. J. Siegwart and M. C. Stefan, J. Mater. Chem. B, 2017, 5, 2106
    DOI: 10.1039/C6TB03038F

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