Synthesis, characterization, and <i>in vivo</i> disposition of iodinatable polyethylene glycol derivatives: Differences <i>in vivo</i> as a function of chain length

Abstract

Abstract A series of iodinatable water soluble polyethylene glycol (PEG) derivatives were prepared for use as model hydrophilic drugs. Polyethylene glycol diamine 6000 was coupled to methyl p ‐hydroxybenzimidate, and PEG 1900‐ and PEG 5000‐monomethyl ethers were coupled to tyramine and histamine. The derivatives underwent facile iodination with the chloramine‐T reaction and were stable under a wide range of conditions. The larger derivatives showed rapid renal clearance, but the 1900 MW compounds underwent significant clearance via the bile.