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Hepatic Targeting Service

Creative Biolabs can assist customers with the design and synthesis service of hepatic targeting drug delivery system (HTDDS). Through effective design and synthesis scheme, nucleic acid drugs can concentrate on the diseased parts of the liver and exert their curative effect, improving the specificity and selectivity of drug. Creative Biolabs works with its clients to realize HTDDS to reduce drug dosage and dosing frequency, reduce the toxicity and optimize the efficacy parameters. According to the guiding mechanism, the HTDDS can be divided into passive targeting, active targeting and physicochemical targeting. Creative Biolabs has extensive experience in the innovative development of high-end targeted nucleic acid drug formulations and has assisted customers to complete efficient and specific small nucleic acid drug delivery services.

Creative Biolabs provides solutions for optimization of nucleic acid drugs, including design and synthesis service of HTDDS. Creative Biolabs has experienced scientific and technical personnel to help customers accelerate the process of nucleic acid drug discovery.

We provide but are not limited to:

  • Triantennary N-acetyl Galactosamine. Triantennary N-acetyl galactosamine is a high affinity ligand for liver cell surface specific asialoglycoprotein receptor (ASGPR). Through the modification of triantennary N-acetyl galactosamine, Creative Biolabs can help our clients achieve the performance improvements of second generation antisenseoligonucleotides (ASOs) in the liver.
    • The modified ASOs have high affinity with ASGPR, which improves the targeted delivery ability of ASOs to liver cells.
    • Upon entry into liver cells, the modified conjugate metabolizes and releases ancestral ASO.
    • In terms of using ASOs to therapeutically inhibit the expression of liver target genes, the results of this analysis can be translated into human trials. This method can provide the possibility to improve the treatment index of ASOs, reduce the treatment cost and support the once-a-month drug delivery regimen.
  • Nucleic acid drug liposomes. Creative Biolabs can modify nucleic acid drug with galactose to prepare liposomes to achieve the liver active targeting delivery.
    • Creative Biolabs can provide thin-film dispersion method service and repeated homogenization method service to prepare the conventional liposome (CL) of AsODN.
    • Service of liposomes labeled with fluorescent dye-soluble DiI is provided.
    • Creative Biolabs can provide validation of targeting design, including in vivo tissue distribution of liposomes, evaluation of targeting properties and validation of targeting properties of hepatocytes in order to better optimize and design nucleic acid drug liposomes.
  • Retinol - c - PEI/ASO complexes. Creative Biolabs can provide carrier design and synthesis service for transport of ASO. By linking small molecular weight polyethylene imide (PEI,1.3KD) with retinol activated by CDI (N,N' -carbonyl diimidazole), the carrier for liver targeted delivery can be provided.
    • The retinol binding protein (RBP) is the single carrier of retinol, Hepatic stellate cells (HSCs) can effectively absorb the RBP-bound retinol in the blood.
    • This service allows the drug carrier to bind to albumin in the bloodstream, thereby taking advantage of the albumin's natural transport capacity to prevent the carrier from being quickly cleared by the body's filtration system and increase its accumulation in the liver.

Advantages of our services:

  • Perfect experimental skills.
  • High cost performance.
  • Impeccable biotechnology services.

References

  1. Prakash TP, et al. Targeted delivery of antisense oligonucleotides to hepatocytes using triantennary N-acetyl galactosamine improves potency 10-fold in mice. Nucleic Acids Res. 2014, 42(13):8796-8807.
  2. Watanabe T, et al. Liver target delivery of small interfering RNA to the HCV gene by lactosylated cationic liposome. J Hepatol. 2007, 47(6):744-750.

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

Online Inquiry

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