Nanoparticulate platinum(II) anticancer drug: Synthesis and characterization of amphiphilic cyclotriphosphazene-platinum(II) conjugates

Ji Young Yu, Yong Joo Jun, Soo Hyun Jang, Hwa Jeong Lee, Youn Soo Sohn

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22 Scopus citations

Abstract

Novel cyclotriphosphazene-platinum(II) conjugates were prepared by hydrolysis and platination of the amphiphilic cyclotriphosphazenes grafted with equimolar hydrophilic methoxy-poly(ethylene glycol) (MPEG) and hydrophobic oligopeptide. These macromolecular conjugates were found to form stable nanoparticles with a mean diameter of approximately 90-200 nm depending on the hydrophobicity of the conjugated (diamine)platinum moieties. The nanoparticulate platinum(II) conjugates have shown temperature and concentration dependent particle sizes. However, the particle sizes of the conjugates were found to decrease to a certain size as the solution concentration was decreased but remained stable even at 10 μM, which is enough for systemic delivery by injection. The conjugates exhibited lower in vitro cytotoxicity than cisplatin but reasonably good activity against selected human tumor cell lines.

Original languageEnglish
Pages (from-to)1931-1936
Number of pages6
JournalJournal of Inorganic Biochemistry
Volume101
Issue number11-12
DOIs
StatePublished - Nov 2007

Keywords

  • Antitumor agent
  • Cyclotriphosphazene
  • Platinum conjugate
  • Tumor selectivity

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