Development of A Novel Polymeric Prodrug Synthesized Using Plasma-Induced Radicals of Polycrystalline Carbohydrates

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  • Yamauchi Yukinori
    Department of Pharmaceutical Physical Chemistry, College of Pharmaceutical Sciences, Matsuyama University
  • Doi Naoki
    Laboratory of Pharmaceutical Physical Chemistry, Gifu Pharmaceutical University
  • Kondo Shin-ichi
    Laboratory of Pharmaceutical Physical Chemistry, Gifu Pharmaceutical University
  • Sasai Yasushi
    Laboratory of Pharmaceutical Physical Chemistry, Gifu Pharmaceutical University
  • Kuzuya Masayuki
    Department of Health & Welfare, Chubu Gakuin University

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<p>A crystalline acrylic-type polymerizable monomer of diclofenac (DF) was synthesized by linking DF molecule to 2-hydroxyethyl acrylate (HEA). Then, the monomer was polymerized in solid state by vibratory milling with plasma-irradiated lactose powders as postprocessing-free initiators. The characterization of the resulting polymeric prodrug powders by ESR and XRPD analysis confirmed their synthesis successfully. Hydrolysis study of the polymeric prodrugs was carried out in three different buffer solutions (pH 1.2, 6.8 and 8.5) at 37℃. The in vitro release profiles indicated that drug release from the polymeric prodrugs was in sustained manner and highly dependent on pH, in which ca. 9%, 25% and 48% of DF was released in 12 h at pH 1.2, pH 6.8 and pH 8.5, respectively. The results suggested that the studied polymeric prodrug systems in the present investigation can be applied to make a formulation for clinical administration of other drugs as carriers in controlled drug release.</p>

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