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A novel micelle-encapsulated platinum(II) anticancer agent

Title
A novel micelle-encapsulated platinum(II) anticancer agent
Authors
Jadhav V.B.Jun Y.J.Song J.H.Park M.K.Oh J.H.Chae S.W.Kim I.-S.Choi S.-J.Lee H.J.Sohn Y.S.
Ewha Authors
손연수이화정
SCOPUS Author ID
손연수scopus; 이화정scopus
Issue Date
2010
Journal Title
Journal of Controlled Release
ISSN
0168-3659JCR Link
Citation
vol. 147, no. 1, pp. 144 - 150
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A hydrophobic and water-insoluble platinum(II) compound, cis-(cha)2Pt(NO3)2 was encapsulated by macromolecular micelles self-assembled from an amphiphilic cyclotriphosphazene [NP(MPEG750)(GlyPheLeu)2Et]3 (CP750). The micelle-encapsulated platinum(II) compound exhibited outstanding pharmacokinetics in rats by showing long blood circulation and much larger systemic exposure (AUC=43.5μgh/ml) compared with the free carboplatin (AUC=4.32μgh/ml). Biodistribution study of the micellar platinum(II) compound using male Sprague-Dawley rats has shown excellent tumor to tissue ratios of 4.03 at 2h post injection and 4.67 at 24h post injection. Furthermore, the micellar platinum(II) compound exhibited more than 6 times higher cellular uptake in human cervical (HeLa) and lung (A549) tumor cells compared with the free platinum compound. Also it is surprising that the micellar platinum(II) compound displayed specifically high cytotoxicity against the stomach tumor cells (SNU638), which are one of the least responsive to chemotherapeutic agents currently in clinical use. The acute toxicity study has shown that the LD50 values of free and the micellar cis-(cha)2Pt(NO3)2 are approximately 70mg/kg and 90mg/kg, respectively. Thus the platinum compound encapsulated by cyclotriphosphazene micelles is a promising candidate for preclinical studies. © 2010 Elsevier B.V.
DOI
10.1016/j.jconrel.2010.07.101
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자연과학대학 > 화학·나노과학전공 > Journal papers
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