Drug Release is Determined by the Chain Length of Fatty Acid-Conjugated Anticancer Agent as One Component of Nano-Prodrug

DOI PDF Web Site 被引用文献14件 参考文献21件
  • Koseki Yoshitaka
    Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
  • Ikuta Yoshikazu
    Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
  • Kamishima Takaaki
    Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
  • Onodera Tsunenobu
    Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
  • Oikawa Hidetoshi
    Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
  • Kasai Hitoshi
    Institute of Multidisciplinary Research for Advanced Materials, Tohoku University

書誌事項

公開日
2016
資源種別
journal article
DOI
  • 10.1246/bcsj.20150405
公開者
公益社団法人 日本化学会

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説明

Effective control of drug release from “nano-prodrugs”, which are nanoparticles composed of water-insoluble prodrug compounds is one of the most important determinants of the balance between drug efficacy and side effects. However, the chemical behaviors of nano-prodrugs in relation to drug release are poorly characterized. We created nano-prodrugs using a series of fatty acid ester (C2–C18) derivatives of 7-ethyl-10-hydroxycamptothecin (SN-38) and found that their in vitro cytotoxic activities decreased as the length of the fatty acid chain increased. The cytotoxicities of these nano-prodrugs were unrelated to particle size or efficacy of cellular uptake, but critically depended on their hydrolysis rate within cancer cells. These results indicated that the drug release rate from nano-prodrugs can be controlled successfully by changing the length of the introduced fatty acid chain.

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