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Polymer-drug conjugates for combination anticancer therapy: investigating the mechanism of action.

Pasut, G., Greco, F., Mero, A., Mendichi, R., Fante, C., Green, R. J. and Veronese, F. (2009) Polymer-drug conjugates for combination anticancer therapy: investigating the mechanism of action. Journal of Medicinal Chemistry, 52 (20). pp. 6499-6502. ISSN 0022-2623

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To link to this article DOI: 10.1021/jm900804m

Abstract/Summary

We developed a family of polymer-drug conjugates carrying the combination of the anticancer agent epirubicin (EPI) and nitric oxide (NO). EPI-PEG-(NO)8, carrying the highest content of NO, displayed greater activity in Caco-2 cells while it decreased toxicity against endothelium cells and cardiomyocytes with respect to free EPI. FACS and confocal microscopy confirmed conjugates internalization. Light scattering showed formation of micelle whose size correlated with internalization rate. EPI-PEG-(NO)8 showed increased bioavailability in mice compared to free EPI.

Item Type:Article
Refereed:Yes
Divisions:Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Pharmaceutics Research Group
ID Code:4408
Uncontrolled Keywords:pegylated epirubicin; breast-cancer; chemotherapy; cytotoxicity; release
Publisher:American Chemical Society

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