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Issue 12, 2016
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Design of systems based on 4-armed star-shaped polyacids for indomethacin delivery

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Abstract

The 4-armed star-shaped copolymers containing methyl (meth)acrylate (MMA, MA) and (meth)acrylic acid (MAA, AA) units were synthesized by ATRP with the use of pentaerythritol (PTL) derivatives as tetrafunctional initiators and by post-polymerization modification to deprotect acidic units. The resultant MMA/MAA, MMA/AA, and MA/MAA based stars were varied by composition of arms using various initial proportions of comonomer pairs. The amphiphilic copolymers were self-assembled by dialysis or solvent evaporation methods into particles, which were also loaded with indomethacin (IMC). The sizes of polymeric aggregates were in the range of 100–200 nm, whereas drug loading efficiency was 10–85%. The in vitro release of IMC in phosphate buffer solution (PBS) demonstrated a higher rate of drug release at pH 5.0 than at 7.4. Drug release profiles can be adjusted by the content of the hydrophilic fraction (15–98%) and distribution of acidic units among arm chains (statistical vs. gradient vs. reverse gradient) as indicated by the broad range of the maximum drug release (10–85%).

Graphical abstract: Design of systems based on 4-armed star-shaped polyacids for indomethacin delivery

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Publication details

The article was received on 27 Jul 2016, accepted on 10 Oct 2016 and first published on 11 Oct 2016


Article type: Paper
DOI: 10.1039/C6NJ02346K
Citation: New J. Chem., 2016,40, 10002-10011
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    Design of systems based on 4-armed star-shaped polyacids for indomethacin delivery

    D. Neugebauer, J. Odrobińska, R. Bielas and A. Mielańczyk, New J. Chem., 2016, 40, 10002
    DOI: 10.1039/C6NJ02346K

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