Characterization of Novel pH-Sensitive Polymeric Micelles Prepared by the Self-Assembly of Amphiphilic Block Copolymer with Poly-4-vinylpyridine Block Synthesized by Mechanochemical Solid-State Polymerization

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概要

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• We fabricated novel pH-sensitive polymeric micelles consisting of amphiphilic block copolymer containing pyridyl groups as side chains in the hydrophobic block. The number average particle diameter of the polymeric micelles at pH 7 was approximately 200 nm. A decrease in pH resulted in deformation of the polymeric micelles over a very narrow pH range (between pH 5.7 and 5.6). Interestingly, micellization and demicellization occurred reversibly in this narrow pH range. Polymeric micelles incorporating 5-fluorouracil (5FU) were also prepared. Decreasing the pH of this polymeric micelle solution from 7 to 5.5 resulted in the rapid release of 5FU at pH 5.6; the drug was completely released within 30 min. These results suggest that deformation of the polymeric micelles caused the rapid release of 5FU.

• 公益社団法人　日本薬学会の論文

著者

• Kondo S

  Hoechst Japan Co. Ltd.

• Kondo Shigemi

  Nissui Pharmaceutical Co. Ltd.

• 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 Pharmaceutical Physical Chemistry, Faculty of Pharmaceutical Science, Matsuyama Univer

• Kondo Shin-ichi

  Dep. Of Pharmaceutical Physical Chemistry Gifu Pharmaceutical Univ.

• Yamamoto Keitarou

  Laboratory of Pharmaceutical Physical Chemistry, Gifu Pharmaceutical University

• Sawama Yuka

  Laboratory of Pharmaceutical Physical Chemistry, Gifu Pharmaceutical University

• Yamauchi Yukinori

  Department of Pharmaceutical Physical Chemistry, College of Pharmaceutical Sciences, Matsuyama University

• Kuzuya Masayuki

  Department of Pharmaceutical Physical Chemistry, College of Pharmaceutical Sciences, Matsuyama University

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