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THE PHARMA REVIEW (SEPTEMBER 2009)

Pegylation: A Technique to Modify Drug Profile

Rakesh R. Somani, Ganesh K. Shinde, Prabhakar Y. Shirodkar, Tanushree Pal, Pravin Naik

Abstract: PEGylation is an important application of polyethylene glycol (PEG), a highly investigated polymer. It involves the covalent attachment of PEG to drugs to solve many tribulations associated with proteinous and non-proteinous drugs. A stable bond is formed between PEG polymer and drug of choice. PEGylation is necessary for the reasons such as increasing the solubility, stability, circulation half-life, for minimizing the rapid kidney clearance, for achieving the controlled release, etc. Advanced PEGylation overcomes the drawbacks of the earlier technology. Four types of bioconjugates of PEG comprise conjugation with peptides and proteins, with lipids, with low molecular weight drugs and with biological macromolecules. PEGylation is widely applied in various fields viz. medical, diagnostic, synthesis of peptides and carrying out some organic synthetic reactions.

Introduction
PEG is a highly investigated polymer and finds its many applications for pharmaceutical purposes. One of the very interesting applications in drug profile modification is PEGylation. It involves the covalent attachment of PEG to drugs to solve many issues faced by protein and nonprotein drugs. PEGylation was first described in the 1970’s by Davies and Abuchowsky and reported in two key papers on albumin and catalase modification.
 
Properties of PEG
Polyethylene glycol has the general formula HO-(CH2-CH2-O) n–CH2-OH with the typical molecular weight ranging into 500-20000. PEG is nontoxic,3 non-immunogenic or poorly immunogenic. It can be used to precipitate proteins and nucleic acids. It forms two-phase system with an aqueous solution of other macromolecules, such as dextran or concentrated salt solutions. PEG’s covalent coupling with proteins, peptides exhibit following properties: Renders protein non-immunogenic and tolerogenic, prolongs the clearance time in vivo when conjugated with drugs, it alters the pharmacokinetics of various drugs, stabilize the physiological function of proteins and bioactive substances, separates biological macromolecules, membranes, cell particles.
 
What is Pegylation?
PEGylation is the technique that involves the modification of a protein, peptide or nonpeptide molecule (drug) by covalent attachment of one or more PEG molecules for the purpose of enhancing therapeutic value. Advanced PEGylation10 involves attaching specific, modified polyethylene glycol (PEG) polymers to biomolecules. The difference between old PEGylation and new or advanced PEGylation are summarized in the Table 1.

 

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