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Synthesis and antitumor activity of novel thermosensitive platinum(II)-cyclotriphosphazene conjugates

Title
Synthesis and antitumor activity of novel thermosensitive platinum(II)-cyclotriphosphazene conjugates
Authors
Song S.-C.Lee S.B.Lee B.H.Ha H.-W.Lee K.-T.Sohn Y.S.
Ewha Authors
손연수
SCOPUS Author ID
손연수scopus
Issue Date
2003
Journal Title
Journal of Controlled Release
ISSN
0168-3659JCR Link
Citation
vol. 90, no. 3, pp. 303 - 311
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Thermosensitive cyclotriphosphazenes bearing alkoxy poly(ethylene glycol) and amino acid esters as side groups could be functionalized to chelate the antitumor (diamine)platinum(II) moiety through the dicarboxylate group of the amino acid substituent on the cyclic phosphazene ring. Surprisingly, like the precursor cyclotriphosphazenes, these (diamine)platinum(II)-cyclotriphosphazene conjugates were also found to exhibit variable lower critical solution temperatures (LCST) in the wide range of 12 to 92°C. Furthermore, the present conjugates have shown outstanding in vitro and in vivo antitumor activities due to controlled release of the antitumor (diamine)platinum(II) moiety with hydrolytic degradation of the phosphazene ring. A few of these conjugates have shown LCSTs below body temperature, and it has been shown from a model animal experiment that the conjugates with a LCST below body temperature may be applied to local drug delivery by direct intratumoral injection. © 2003 Elsevier B.V. All rights reserved.
DOI
10.1016/S0168-3659(03)00199-8
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자연과학대학 > 화학·나노과학전공 > Journal papers
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