Custom Oligonucleotides-Cyclodextrin Conjugation Service

Polycationic polymers such as cyclodextrin constitute one of the most promising approaches for gene and nucleic acid drug delivery and site-directed delivery using non-viral vectors. Based on our advanced research platform and powerful technology, Creative Biolabs provides customized services to meet the different purposes of customers, forming stable drug carriers while greatly improving the accuracy of targeted delivery and site-specific release.

Custom Oligonucleotides Cyclodextrin Conjugation

Gene therapy and RNA interference technologies have not only become powerful tools for functional genomics and vaccine drug development but also allow rapid discovery and validation of drug targets at the cellular level. This technology can be achieved by nuclear delivery of short hairpin RNA or cytoplasmic delivery of small double-stranded interfering RNA oligonucleotides, however, there is still a lack of effective methods to deliver nucleic acids to designated tissues and cells. At present, more viral vectors are used as the main delivery system for short hairpin RNA (shRNA), but polycationic nucleic acid delivery methods like conjugation with cyclodextrin can also provide sufficient protection for nucleic acid drugs to cross various barriers and screen.

Cyclodextrin

Cyclodextrins (CyD) are natural cyclic oligomers composed of 6-8 glucose units linked by glycosidic bonds that have a ring-shaped structure with a hydrophobic cavity and allow the inclusion of sterically compatible molecules within it. Although CyD has high molecular weight and hydrophilicity, which makes it difficult to enter cells, conjugation with cyclodextrin can significantly improve the solubility, dissolution and bioavailability of drugs. Various CyD-bearing polymers and polyrotaxanes and CyD-based nanoparticles have been approved and used for nucleic acid/oligonucleotide delivery.

Fig. 1 Chemical structures of several types of cyclodextrins.¹

Oligonucleotides Cyclodextrin Conjugation Methods

As very promising oligonucleotide delivery molecules, many attempts have been made to design and evaluate CyD conjugates for polymerization methods of nucleic acid or oligonucleotide carriers. β-CyD polycation with seven glucose units can be assembled with diamond PEG or diamond PEG transferrin and used as a carrier to bind modified siRNA. Through a chemoenzymatic click strategy, CyD can be combined with dendrimers to form polymers after mono-6-O-naphthalenesulfonylated, which still retain the terminal modifiable amine functional groups of the dendrimers and allow them to interact with other molecules. Nucleic acids or oligonucleotides can act as a sustainable pDNA carrier and delivery system after conjugation with PEG molecules.

Creative Biolabs is committed to providing stable, high-quality and customizable cyclodextrin-oligonucleotide conjugation services to customers all over the world. According to your project, we can synthesize nucleic acid fragments of specific sequences for you and stably conjugate them with different types of cyclodextrins. In addition to this, a range of available crosslinkers are also at your disposal.

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