Background: PEGylation, association of poly(ethylene glycol) (PEG) to drug molecules or drug-bearing particles, is one of the most promising techniques on the way to improve the pharmacokinetic features of a drug which, in turn, leads to pharmacodynamic improvements.
Objective: The aim of this review is to describe PEGylation as a procedure for alteration of drug molecular structure with the main emphasis on its pharmacokinetic consequences.
Methods: After a brief but concise overview of the history and chemistry of PEGylation, the boundary of this literature survey is confined to the findings and reports on the impact of PEGylation on biodistribution and bioelimination of therapeutic molecules.
Conclusion: It is concluded, based on the whole body of the data in literature, that the main results of PEGylation on pharmacokinetic properties of the drug include prolongation of lifespan in circulation, alterations in drug elimination pathway(s) and changes in drug biodistribution profile, among others, which all are derived from the structural changes that occur in the drug molecule, mainly reversible attachment of a large polymeric moiety to parent drug.