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Selective tumor targeting by enhanced permeability and retention effect. Synthesis and antitumor activity of polyphosphazene-platinum (II) conjugates
- Title
- Selective tumor targeting by enhanced permeability and retention effect. Synthesis and antitumor activity of polyphosphazene-platinum (II) conjugates
- Authors
- Jun Y.J.; Kim J.I.; Jun M.J.; Sohn Y.S.
- Ewha Authors
- 손연수
- SCOPUS Author ID
- 손연수
- Issue Date
- 2005
- Journal Title
- Journal of Inorganic Biochemistry
- ISSN
- 0162-0134
- Citation
- Journal of Inorganic Biochemistry vol. 99, no. 8, pp. 1593 - 1601
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- Nanosized polyphosphazene-platinum (II) conjugates with a wide range of molecular weight from 24,000 to 115,000 were synthesized to study their tumor selectivity by enhanced permeability and retention (EPR) effect and their antitumor activity. It has been found from biodistribution study that the present polyphosphazene-Pt(II) conjugates exhibit high tumor selectivity by EPR effect with the tumor to tissue ratio (TTR) from 3.6 to 13 depending on the molecular size. These polymer conjugates have shown excellent in vivo antitumor activity against both murine and human cancer cell lines. In particular, xenograft trials of the conjugates have shown outstanding tumor inhibition effect on the stomach cancer cell line, YCC-3, which is one of the least responsive to the anticancer agents currently in clinical use, although the reason is not clearly explainable yet. The high in vivo activity seems to be attributed to the controlled-release of the antitumor active platinum (II) moiety, [GlyGluPt(dach] (dach = trans-(±)-1,2-diaminocyclohexane) from the phosphazene backbone by degradation in aqueous solution. © 2005 Elsevier Inc. All rights reserved.
- DOI
- 10.1016/j.jinorgbio.2005.04.019
- Appears in Collections:
- 자연과학대학 > 화학·나노과학전공 > Journal papers
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