Drug release is determined by the chain length of fatty acid-conjugated anticancer agent as one component of nano-prodrug

Yoshitaka Koseki, Yoshikazu Ikuta, Takaaki Kamishima, Tsunenobu Onodera, Hidetoshi Oikawa, Hitoshi Kasai

    研究成果: Article査読

    30 被引用数 (Scopus)

    抄録

    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 (C2C18) 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 nanoprodrugs can be controlled successfully by changing the length of the introduced fatty acid chain.

    本文言語English
    ページ(範囲)540-545
    ページ数6
    ジャーナルBulletin of the Chemical Society of Japan
    89
    5
    DOI
    出版ステータスPublished - 2016

    ASJC Scopus subject areas

    • 化学 (全般)

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