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Targeting Delivery Analysis Service

Nucleic acid drug is one of new gene therapy drugs. Its development is restricted by its poor biological stability, easy to be degraded by nuclease in vivo, low bioavailability and low concentration of aggregation in target tissues. The targeting delivery technology solves the problem of stability and targeting delivery of nucleic acid drugs to a certain extent, which greatly promotes the development of nucleic acid drugs. Using vector technology and targeting delivery system, Creative Biolabs can help clients improve the biological activity of nucleic acid drugs, improve distribution in vivo, enhance targeting and uptake ability to cells and improve the concentration and bioavailability of drugs in target tissues.

Creative Biolabs is a leading biotechnology services platform, providing the discovery and optimization of nucleic acid drug candidates. Our researchers are all from accredited organizations and institutions and are rigorously trained to ensure that the quality of targeting delivery study service meets national standards.

Classification of targeting delivery system of nucleic acid drugs:

  • Polypeptide protein delivery vector.
  • Targeting delivery system mediated by ligand based on specific receptor.
  • Liposome. This classification includes common cationic lipid bilayer, liposome DOTAP, lipofectine and pH sensitive liposome.
  • Cationic polymer compound. This classification includes polyethyleneimine (PEI) and polyamide - amine (PAMAM).
  • Dendrimers (DEN) and various polymers. This classification includes polycyanoacrylate nanoparticles and polylactic acid nanoparticles.
  • Active targeting nanoparticles. Through targeting molecular modifications, active targeting nanoparticles can improve the concentration and bioavailability of drugs in target tissues. The targeting molecular includes sialic acid protein, polysaccharide, epidermal growth factor, folic acid, transferrin, body hormone and monoclonal antibody.

We provide but are not limited to:

  • Peptide modification. The peptide modification includes covalent conjugation and non-covalent conjugation.
    • Covalent conjugation. By means of covalent bonds such as disulfide bonds, thioether bonds, mercaptan maleimide and diester phosphate bonds, polypeptides are covalently conjugated to oligonucleotic acid molecules and other carriers. Such conjugates can be completed by solid phase synthesis and liquid phase synthesis with high reaction efficiency. The advantage of covalent conjugation is that it provides well-defined, single compounds and simplifies drug development. This strategy is more suitable for the modification of phosphorodiamidate morpholino oligomers (PMO) and peptide nucleic acids (PNA).
    • Non-covalent conjugation. Non-covalent conjugation is the process by which polypeptides and their derivatives are complexed with negatively charged oligonucleotide molecules to form complexes by the non-covalent bond. When the oligonucleotides are connected by non-covalent bonds, there is no need to modify the end of the oligonucleotides. Complexes can be formed by simple mixing. This method can effectively prevent the degradation of oligonucleotides by nucleases, so it is widely used.
  • Aptamer-cationic polymer-siRNA system. Cationic polymers can be self-assembled into particles by electrostatic adsorption with nucleic acid to prevent nucleic acid from being degraded by nuclease. This strategy is easy to synthesize, stable to store, high gene load rate and low immunogenicity, which can be used in our gene vector research. Creative Biolabs introduces polyethyleneimine (PEI) as a non-viral vector. PEI has a unique "proton sponge" effect. Compared with liposomes, PEI has higher charge density and stronger buffering capacity, which is beneficial to protect the encapsulated nucleic acid from lysosomal lysis and assist the release of nucleic acid from the endosome.

References

  1. Jiang D, et al. DNA nanomaterials for preclinical imaging and drug delivery. J Control Release. 2016, 239:27-38.
  2. Parlea L, et al. Cellular Delivery of RNA Nanoparticles. ACS Comb Sci. 2016, 18(9):527-547.

*For Research Use Only. Not for use in diagnostic procedures.

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