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

    Research output: Contribution to journalArticlepeer-review

    32 Citations (Scopus)

    Abstract

    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.

    Original languageEnglish
    Pages (from-to)540-545
    Number of pages6
    JournalBulletin of the Chemical Society of Japan
    Volume89
    Issue number5
    DOIs
    Publication statusPublished - 2016

    ASJC Scopus subject areas

    • Chemistry(all)

    Fingerprint

    Dive into the research topics of 'Drug release is determined by the chain length of fatty acid-conjugated anticancer agent as one component of nano-prodrug'. Together they form a unique fingerprint.

    Cite this