Bioactive polymeric metallosomes self-assembled through block copolymer-metal complexation

Kensuke Osada, Horacio Cabral, Yuki Mochida, Sangeun Lee, Kazuya Nagata, Tetsuya Matsuura, Megumi Yamamoto, Yasutaka Anraku, Akihiro Kishimura, Nobuhiro Nishiyama, Kazunori Kataoka

Research output: Contribution to journalArticlepeer-review

80 Citations (Scopus)


Spontaneous formation of polymeric metallosomes with uniform size (∼100 nm) was found to occur in aqueous medium through the reaction of an anticancer agent, (1,2-diaminocyclohexane)platinum(II) (DACHPt), with a Y-shaped block copolymer of ω-cholesteroyl-poly(l-glutamic acid) and two-armed poly(ethylene glycol) (PEGasus-PLGA-Chole). Circular dichroism spectrum measurements revealed that the PLGA segment forms an α-helix structure within the metallosomes, suggesting that secondary-structure formation of metallocomplexed PLGA segment may drive the self-assembly of the system into vesicular structure. These metallosomes can encapsulate water-soluble fluorescent macromolecules into their inner aqueous phase and eventually deliver them selectively into tumor tissues in mice, owing to the prolonged blood circulation. Accordingly, fluorescent imaging of the tumor was successfully demonstrated along with an appreciable antitumor activity by DACHPt moieties retained in the vesicular wall of the metallosomes, indicating the potential of metallosomes as multifunctional drug carriers.

Original languageEnglish
Pages (from-to)13172-13175
Number of pages4
JournalJournal of the American Chemical Society
Issue number32
Publication statusPublished - Aug 15 2012
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry


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