Biopharma PEG has successfully obtained Drug Master File (DMF) approval from the U.S. Food and Drug Administration (FDA) for our self-developed HZ-PEG-HZ (1K) product (DMF number: 041864). This significant milestone not only demonstrates our company's strong R&D capabilities in high-quality PEG derivatives but also provides reliable and compliant product support to pharmaceutical companies worldwide.
Hydrazide-PEG-Hydrazide (HZ-PEG-HZ) is a bifunctional polyethylene glycol (PEG) derivative featuring hydrazide functional groups (-CONHNH₂) at both ends of the PEG chain. This reactive PEG compound represents a versatile bioconjugation tool that combines the beneficial properties of PEG polymers with the unique reactivity of hydrazide groups.
- •Structure: H₂N-NH-PEG-NH-NH₂
- •Molecular weights available: Typically from 1K to 20K Da
- •Solubility: Water and most polar solvents
Reactivity: The hydrazide groups can form hydrazone bonds with aldehyde or ketone groups under mild aqueous conditions.
Applications
Protein and Peptide Modification
HZ-PEG-HZ serves as an effective tool for protein PEGylation, particularly for site-specific modifications. The compound can conjugate to proteins through several pathways, including oxidation of oligosaccharide residues in glycoproteins, transamination of N-terminal residues, and periodate oxidation of N-terminal serine or threonine residues. PEGylation with HZ-PEG-HZ improves protein solubility, stability, reduces immunogenicity, and extends circulation half-life .
Drug Delivery Systems
The pH-sensitive properties of HZ-PEG-HZ make it valuable for targeted drug delivery applications. Hydrazone bonds are pH-sensitive. They are relatively stable at neutral pH but can hydrolyze (break) under acidic conditions (e.g., in endosomes or lysosomes within cells, or in tumor microenvironments). This "acid-cleavable" property makes HZ-PEG-HZ ideal for designing drug delivery systems that release their payload specifically in acidic environments, improving targeted drug delivery and reducing off-target effects. For example, it can be used to conjugate drugs or targeting ligands to nanoparticles.
Bioconjugation and Crosslinking
HZ-PEG-HZ functions as a heterobifunctional crosslinker for various bioconjugation applications. It enables the attachment of different biomolecules, creation of antibody-drug conjugates, and the development of diagnostic imaging agents. The compound's ability to form reversible linkages makes it particularly useful for applications requiring controlled release or detachment.
Nanotechnology Applications
In nanotechnology, HZ-PEG-HZ is employed for surface functionalization of nanoparticles and solid surfaces. The compound helps reduce non-specific binding of charged molecules and improves biocompatibility of modified surfaces. It has applications in cell culture research, ligand studies, and the development of new materials with enhanced properties.
Conclusion
Hydrazide-PEG-Hydrazide represents a versatile and valuable tool in bioconjugation chemistry and drug delivery applications. Its unique combination of PEG properties with pH-sensitive hydrazone chemistry makes it particularly suitable for developing smart drug delivery systems, protein modifications, and targeted therapeutic applications. As research continues in personalized medicine and targeted therapy, HZ-PEG-HZ is likely to play an increasingly important role in advancing these fields.
Biopharma PEG remains committed to delivering high-quality, reliable PEG products and exceptional customer service. We will continuously strive to improve all aspects of our operations, including product research and development, Good Manufacturing Practices (GMP) compliant production and quality release, and comprehensive customer support. Contact us at sales@biochampeg.com if you are interested.
References:
[1] Hydrazide Derivatives of Poly(ethylene glycol) and Their Bioconjugates, Samuel Zalipsky and Sunitha Menon-Rudolph, Poly(ethylene glycol). August 5, 1997 , 318-341, DOI:10.1021/bk-1997-0680.ch021
[2] Li, C., Li, T., Tian, X., An, W., Wang, Z., Han, B., Tao, H., Wang, J., & Wang, X. (2024). Research progress on the PEGylation of therapeutic proteins and peptides (TPPs). Frontiers in pharmacology, 15, 1353626. https://doi.org/10.3389/fphar.2024.1353626
[3] Kale, A. A., & Torchilin, V. P. (2007). Design, synthesis, and characterization of pH-sensitive PEG-PE conjugates for stimuli-sensitive pharmaceutical nanocarriers: the effect of substitutes at the hydrazone linkage on the ph stability of PEG-PE conjugates. Bioconjugate chemistry, 18(2), 363–370. https://doi.org/10.1021/bc060228x