PEG Oligonucleotides(PEG -Aptamer,PEG-siRNA,PEG-ASO)

PEG Oligonucleotides(PEG -Aptamer,PEG-siRNA,PEG-ASO)

Oligonucleotide drugs have a short half-life in the body and are easily damaged by various enzymes. The kidney also clears them quickly, which is not conducive to maintaining a certain concentration of drugs. At the same time, oligonucleotides themselves have a strong negative charge and are not easy to approach cell membranes with the same negative charge, thereby reducing their chances of being taken up by cells and lowering their efficacy. PEG modification can effectively solve the above problems.

In the study of antisense nucleic acid (ASO), it was found that the in vivo half-life of ASOs modified with PEG using thiophosphate diester bonds as the backbone was ten times longer than that of ordinary ASOs. At the same time, PEG of macromolecules can increase the molecular weight and volume of oligonucleotide drugs, making it difficult for them to pass through the glomerular filtration membrane, reducing the excretion rate of the kidneys, effectively prolonging the retention time of drugs in the circulatory system, and improving their biological activity. In addition, PEG can also form a three-dimensional protective film in water, wrapping around the surface of oligonucleotide drugs to shield their surface negative charges, facilitating the uptake of oligonucleotide drugs by corresponding cells and improving their effectiveness. Beixin Biotechnology can provide various oligonucleotide PEG (mPEG, DSPE PEG, Chol PEG, Biotin PEG, FITC PEG, DBCO PEG, Azide PEG, etc.) conjugates according to customer needs.

The common coupling methods between PEG and oligonucleotides are as follows: