Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 20, Pages 6499-6502Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm900804m
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Funding
- British Council (Exchange Programme Award to Pasut-Greco)
- MIUR [03035]
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We developed a family of polymer-drug conjugates carrying the combination of the anticancer agent epirubicin (EPI) and nitric oxide (NO). EPIPEG-(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.
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