PEGylation of siRNA

Name: PEGylation of siRNA
Brand: BOC Sciences

Article Body

BOC Sciences has developed and synthesized a large number of PEGylated siRNA molecules for pharmaceutical and biotechnology companies. We are proud to leverage our expertise and state-of-the-art technology to advance our clients' drug development programs. We have established an internal PEGylation platform to provide specific PEGylation designs according to customer requirements, and complete experiments according to specifications according to customer needs. We believe that we will continue to be a high-quality PEGylation service provider of siRNA in the next few years.

Introduction of siRNA PEGylation

PEGylation of siRNA

Small interfering RNA (siRNA) is a type of double-stranded RNA molecule artificially designed and synthesized. The sequence of siRNA can vary according to the sequence of the target mRNA, so with proper design, siRNA can silence a variety of genes of interest. This property has sparked interest in the use of siRNA for biomedical research and drug development. However, due to their special structures, siRNAs cannot be directly used for nucleic acid therapy. Surface coating with polyethylene glycol (PEG) can reduce toxicity, increase the structural stability of siRNA and prolong its circulation time in blood.

siRNA PEGylation Service Content

Design Active Derivatives of PEG

Provide custom design services for various complex PEG derivatives (monofunctional, homologous bifunctional, heterologous bifunctional, fluorescent, lipid, multi-arm (4-arm and 8-arm), monodisperse, polydisperse).

PEG Modified Conjugation Technology Development

Support a variety of coupling pathways, mainly including amino reaction (acylation modification of N-terminal amino group, acylation modification of lysine side chain amino group, alkylation modification of N-terminal amino group), carboxyl and active ester reaction, sulfhydryl reaction, click chemistry reaction, thiol reaction, etc.

Fig. 1. Synthetic schemes of siRNA conjugated with PEG via (A) cleavable linkage and (B) noncleavable linkage.^[1]

Purification of PEGylated siRNA

Separation and purification through PEGylation degree and positional isomerism can remove various impurities in one step while maintaining a high loading capacity.

Analytical Method Development

Provide a series of method evaluations including PEGylated siRNA structure identification, homogeneity analysis, drug metabolism and pharmacokinetic analysis, etc.

Process Optimization and Scale-up

Develope a suitable protocol to provide you with mg to g scale PEG-modified siRNA amplification, in line with GMP standards.

siRNA PEGylation Service Process

Process	Content
PEG molecule selection	Screen PEG molecules with appropriate molecular weight and functional groups to ensure better structural stability.
Active group screening	Screen the modification site away from the active site of siRNA to ensure that the siRNA can get higher activity retention.
Reaction system development	Determine the modification ratio, reaction time, temperature, buffer system, pH, etc.
Purification/characterization	Purification by ion exchange chromatography, density gradient centrifugation, molecular sieve, HPLC, etc.
Impurity removal	Removal of unmodified siRNA residues using the separation process.
Product in vitro property testing	Detection of purity and activity, circulation half-life, stability, etc.

By utilizing our advanced and innovative PEGylation technology, BOC Sciences offers a wide variety of modified siRNAs, and they are delivered just in time. In addition, we also provide customers with flexible and diverse synthetic specifications, which can be customized in large quantities. We aim to meet a variety of research needs in biology, diagnostics, personal medicine, drug discovery and more.

To find out how our team can help you overcome the PEGylation challenges of siRNA, please contact us today.

Reference

Jung S, et al. Gene silencing efficiency of siRNA-PEG conjugates: Effect of PEGylation site and PEG molecular weight. Journal of Controlled Release Official Journal of the Controlled Release Society, 2010, 144(3): 306-313.

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