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Journal of Drug Delivery
Volume 2012, Article ID 103973, 17 pages
Review Article

Poly(ethylene glycol)-Prodrug Conjugates: Concept, Design, and Applications

1NCE-Polymer Chemistry Group, Piramal Life Sciences Ltd., 1 Nirlon Complex, Off Western Express Highway, Goregaon (E), Mumbai 400063, India
2Semler Research Center Pvt Ltd., 75A, 15th Cross, I Phase, J. P. Nagar, Bangalore 560078, India

Received 11 October 2011; Revised 3 January 2012; Accepted 5 January 2012

Academic Editor: Abhijit A. Date

Copyright © 2012 Shashwat S. Banerjee et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Poly(ethylene glycol) (PEG) is the most widely used polymer in delivering anticancer drugs clinically. PEGylation (i.e., the covalent attachment of PEG) of peptides proteins, drugs, and bioactives is known to enhance the aqueous solubility of hydrophobic drugs, prolong circulation time, minimize nonspecific uptake, and achieve specific tumor targetability through the enhanced permeability and retention effect. Numerous PEG-based therapeutics have been developed, and several have received market approval. A vast amount of clinical experience has been gained which has helped to design PEG prodrug conjugates with improved therapeutic efficacy and reduced systemic toxicity. However, more efforts in designing PEG-based prodrug conjugates are anticipated. In light of this, the current paper highlights the synthetic advances in PEG prodrug conjugation methodologies with varied bioactive components of clinical relevance. In addition, this paper discusses FDA-approved PEGylated delivery systems, their intended clinical applications, and formulations under clinical trials.