For Research Use Only. Not for Clinical Use.

Creative Biolabs is a leading service provider that focuses on the design and conduct of novel drug molecules. Based on our advanced platforms and extensive experience, now we can provide biotinylated PEG-based half-life extension services for our clients all over the world.

Introduction of PEGylation and Biotinylated PEG

Chemotherapeutics drugs present great potentials for diseases treatment but are always limited by multiple challenges, such as rapid elimination and weak targeting abilities. In recent decades, a series of organic and inorganic nanoparticles (NPs) have been developed to improve tumor specificity and avoid the accumulation of drugs in normal organs so that decrease chemotherapy side effects. PEG is the uncharged hydrophilic polymer with non-toxic and non-immunogenic. Using PEG, the overall size of proteins increased, and therapeutic half-life can be extended.

PEGylation has been considered the most popular protein half-life extension technology. However, PEG is not 100% safe and scientists have been efforts to further develop PEG conjugated therapeutics according to modifying and conjugating PEG to other moieties. Nowadays, a modified PEG was developed by conjugating PEG to streptavidin.

Fig 1. Drug delivery process of PEGylated NPs starting from systemic circulation to tumor targeting and clearance. (Mozar, 2018)

Applications of Biotinylated PEG for Half-Life Extension

Biotinylated PEG has been applied for surface modification of carbon apatite nanoparticle (Co3AP NP) carrying Gemcitabine, which results in enhanced residence time in blood circulation. What’s more, several different avidin-biotin-PEG-CPA complex preparations were successfully prepared with bovine carboxypeptidase A (CPA) as the target enzyme. Depending on the length of the PEG chain, in vitro results show that its half-life can be increased to 3-4 days. In summary, biotinylated PEG has enormous potential as a pharmacokinetics enhancer for therapeutic peptides and proteins.

Advantages of Biotinylated PEG

• The antigenic determinants of the peptide/proteins are hidden.
• Increase peptides/proteins size so that it is not easily cleared by the kidneys.
• PEG itself is non-toxic and non-immunogenic.
• Biotinylated PEG can increase the water solubility of proteins and protect them from proteolytic degradation.

As a leading custom service provider in the field of drug discovery, Creative Biolabs has won a good reputation among our worldwide customers for successfully accomplishing numerous challenging projects including a variety of half-life extension projects. If you are interested in our products or services, please do not hesitate to contact us for more detailed information.

Reference

1. Mozar, F.; Chowdhury, E. Impact of PEGylated nanoparticles on tumor targeted drug delivery. Current pharmaceutical design. 2018, 24(28): 3283-3296.