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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].