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Bioactive Polymeric Metallosomes Self-Assembled through Block Copolymer–Metal Complexation

2012; American Chemical Society; Volume: 134; Issue: 32 Linguagem: Inglês

10.1021/ja304615y

1943-2984

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

Nanoparticle-Based Drug Delivery

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.