Song, R Jun, YJ Kim, JI Jin, C Sohn, YS 2024-01-21T04:42:15Z 2024-01-21T04:42:15Z 2021-09-03 2005-06-20 0168-3659 https://pubs.kist.re.kr/handle/201004/136356 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 (t(1/2 beta)=6.2 h and AUC=4020 nmol h/ml) compared with carboplatin ((1/2 beta) =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. (c) 2005 Elsevier B.V. All rights reserved. English ELSEVIER SCIENCE BV VASCULAR-PERMEABILITY ANTITUMOR-ACTIVITY MOLECULAR-WEIGHT DRUG-DELIVERY LIPOSOME SIZE COMPLEXES POLYMERS BIODISTRIBUTION ELECTROLYTES THERAPEUTICS Synthesis, characterization, and tumor selectivity of a polyphosphazene-platinum(II) conjugate Article 10.1016/j.jconrel.2005.03.016 1 JOURNAL OF CONTROLLED RELEASE, v.105, no.1-2, pp.142 - 150 JOURNAL OF CONTROLLED RELEASE 105 1-2 142 150 scie scopus 000230576600013 2-s2.0-20444427224 Chemistry, Multidisciplinary Pharmacology & Pharmacy Chemistry Pharmacology & Pharmacy Article VASCULAR-PERMEABILITY ANTITUMOR-ACTIVITY MOLECULAR-WEIGHT DRUG-DELIVERY LIPOSOME SIZE COMPLEXES POLYMERS BIODISTRIBUTION ELECTROLYTES THERAPEUTICS polyphosphazene platinum conjugate anticancer drug tumor selectivity