What Is PEGylation?
PEGylation is the process of attaching chains of polymer PEGs to molecules, most typically peptides, proteins and antibody fragments, to improve the safety and efficiency of many therapeutic drugs. It produces changes in physicochemical properties, including changes in conformation, electrostatic binding, and hydrophobicity. These physical and chemical changes increase the systemic retention of the therapeutic agent. In addition, it can affect the binding affinity of therapeutic molecules to cellular receptors and can alter absorption and distribution patterns.
PEGylation can bring some important pharmacological advantages to the unmodified form by increasing the molecular weight of the molecule, such as improved drug solubility, reduced dose frequency, potentially reduced toxicity, undiminished efficacy, extended circulating life, increased drug stability, and enhanced protection against proteolytic degradation.
The Application of PEGylation Reagents
1. PEGylated protein drugs: PEGylated protein drugs can extend drug half-life, reduce immunogenicity, while maximizing the retention of its biological activity. As a therapeutic drug, polyethylene glycol (PEG) modified proteins are more effective than unmodified proteins. The modification pathway of PEGylated protein drug mainly includes amino modification (including acylation modification of N-terminal amino group, acylation modification of lysine side chain amino group, alkylation modification of N-terminal amino group), carboxyl modification, thiol modification, and the like. At present, the research on PEGylated protein drugs at home and abroad mainly focuses on adenosine deaminase, asparaginase, interferon, granulocyte colony-stimulating factor, interleukin, etc. More than 40 drugs are undergoing clinical research.
2. PEGylated peptide-based compounds: PEGylated peptide-based compounds, such as the PEGylated products of furrow calcitonin, epidermal growth factor, have longer half-life and higher biological activity than the parent drug. In particular, peptide compounds are easier to achieve than proteins in fixed-point modification of polyethylene glycol. The most common application in the PEGylation study of peptide compounds is mPEG.
3. PEGylated liposomes: Ordinary immunoliposomes are limited in their ability to be cleared due to their short half-life in the blood, which limits their development. PEGylated long-circulating liposomes (stealth liposomes) increase the blood circulation time of liposomes, which not only can escape the capture of the reticuloendothelial system, but also improve the passive targeting. It has been widely used in liposome pharmaceutical preparations. (Advantages and Disadvantages of PEGylated Liposomes in Drug Delivery System)
4. PEGylated organic small molecule drugs: many small molecule drugs, especially the anti-tumor drugs, use PEGylation technology to improve its biocompatibility. The polyethylene glycol (PEG) supported small molecules can transfer many of its excellent properties to the conjugate which make the polymer has excellent biocompatibility. Thus, the polymer can be dissolved in the tissue fluid, and can be quickly excreted by the body without any toxic side effects. Many anti-tumor drugs are modified by high molecular weight PEG to achieve passive targeted administration of tumor tissue.
5. Other applications: PEGylated affinity ligands and cofactors are used in aqueous two-phase distribution systems for the purification and analysis of biological macromolecules and cells. PEGylated sugars can be used as new drug materials and drug carriers. Oligonucleotide PEGylation can increase solubility, resistance to nucleases, and cell membrane permeability. Biomaterial PEGylation reduces thrombus formation and reduces protein and cell adhesion.
Biochempeg provides PEGylation services for proteins, peptides, liposomes and other molecules. Our R&D chemists will perform your PEGylation service in a professional and efficient manner to provide you with high-quality PEGylated products in a short period of time.