PEGylation

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PEGylation

The technique of covalently attaching polyethylene glycol (PEG) to a given molecule is known as “PEGylation” and is now a well-established method in the field of targeted drug delivery systems. PEGylation has the ability to enhance the retention time of the therapeutics like proteins, enzymes small molecular drugs, liposomes and nanoparticles by protecting them against various degrading mechanisms active inside a tissue or cell, which consequently improves their therapeutic potential. PEGylation effectively alters the pharmacokinetics (PK) of a variety of drugs and dramatically improves the pharmaceutical values; recent development of which includes fabrication of stimuli-sensitive polymers/smart polymers and polymeric micelles to cope of with the pathophysiological environment of targeted site with less toxic effects and more effectiveness.

PEGylation Figure 1. Structural change of molecule by PEGylation1

Below is a list of our PEGylation Services (include but not limited to the following):

Proteins PEGylation

PEGylation of proteins is a well-established method in the pharmaceutical field, but the significance of PEGylated peptides and proteins for anti-cancer therapy has only been realized in the last several years as more and more PEG conjugates make it to late-phase clinical trials. Enzymes, monoclonal antibodies and cytokines are the three major class of proteins used in anticancer therapy or as adjuvant therapy.

Various PEGylated low molecular weight anti-cancer drugs are currently under development. For example, topoisomerase I inhibitor camptothecin-based drugs (irinotecan, topotecan, SN38, exetecan, etc.) is reported to be useful in the treatment of many solid tumors. However, the hydrophobicity of such material limits their therapeutic efficacy.

Nanoparticles (NPs) are synthetic materials with dimensions from 1 to 1000 nano-meters. NPs have large payloads, stability and the capacity for multiple, simultaneous applications due to their unique size and high surface area:volume ratio. Despite these advantages, the major drawbacks associated with NP drug delivery system for clinical studies are associated with short circulating half-life due to uptake by the reticuloendothelial system (RES) for larger NPs, whereas smaller NPs are subjects to tissue extravazations and renal clearance. Liposomes, solid lipids nanoparticles, dendrimers, polymers, silicon or carbon materials, and gold and magnetic nanoparticles are examples of nano-carriers that have been studied as drug delivery systems in cancer therapy. Therefore, surface modification of the nanoparticles with PEGs of various chain length, shape, density, molecular weight and incorporation of different targeting moieties (ligands, antibodies, etc.) is emerging as a more promising and technologically advanced drug delivery system in anti-cancer therapy.

Smart polymers are defined as polymers that undergo reversible large, physical or chemical changes in response to small external changes in the environmental conditions, such as temperature, pH, light, magnetic or electric field, ionic factors, biological molecules, etc. Smart polymers show promising applications in the biomedical field as delivery systems of therapeutic agents.

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References:

  1. Prajna Mishra., Bismita Nayak., & R.K. Dey. (2016). PEGylation in anti-cancer therapy: An overview. Asian Journal of Pharmaceutical Sciences, 11(3), 337-34.
  2. Chao, S. H., Matthews, S. S., Paxman, R., Aksimentiev, A., Gruebele, M., & Price, J. L. (2014). Two structural scenarios for protein stabilization by PEG. The Journal of Physical Chemistry B, 118(28), 8388-8395.
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