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Table 2 The influence of polymer conjugation on the pharmacokinetics and pharmacodynamics of DFO

From: Polymeric nanocarriers for the treatment of systemic iron overload

-DFO Conjugate

Pharmacodynamic effect

Pharmacokinetic effect

Dextran-DFO [44]

LD50 increased from 250 mg/kg to 4000 mg/kg, reduction of pulmonary hypotension in dogs

Increased circulation half-life

Starch-DFO (40SDO2) [47]

Reduced retinal toxicity in albino rats, Reduction of pulmonary hypotension in dogs

Increased in vivo iron excretion efficiency, increased circulation half-life. Excess free iron binding capacity in healthy males

PEG-Methacrylate-DFO [46]

Reduced endothelial cell toxicity

--

HPG-DFO [48]

Increased in vivo LD50

Increased in vivo iron mobilization efficiency in mice Increased circulation half-life in mice

Decreased clearance

  1. Conjugated forms of DFO are associated with reduced toxicity both in vitro and in vivo. Dextran-DFO, HES-DFO and HPG-DFO demonstrated significantly higher plasma half-lives than unconjugated DFO [44,46-48].