Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9774682 | Journal of Controlled Release | 2005 | 9 Pages |
Abstract
A new amphiphilic poly(organophosphazene) was synthesized by stepwise nucleophilic substitutions with a hydrophilic methoxy poly(ethylene glycol) with an average molecular weight of 350 (MPEG350) and a hydrophobic glycyl-l-glutamate as side groups, and then an antitumor (dach)platinum(II) (dach: trans-(±)-1,2-diaminocyclohexane) moiety was conjugated to the polymer using the dipeptide as a spacer. This polymeric platinum conjugate was found to be accumulated in the tumor tissue to a remarkably greater extent than in the normal tissue (tumor/tissue ratio >4), probably due to the excellent EPR effect and the long circulating properties of the polymer conjugate (t1/2β = 6.2 h and AUC = 4020 nmol h/ml) compared with carboplatin (t1/2β = 0.42 h and AUC = 120 nmol h/ml). The polymer conjugate also exhibited high in vitro cytotoxicity comparable to cisplatin against several human tumor cells tested.
Related Topics
Physical Sciences and Engineering
Materials Science
Biomaterials
Authors
Rita Song, Yong Joo Jun, Ju Ik Kim, Changbae Jin, Youn Soo Sohn,