Dendrimer Fluorination Service

Fluorinated dendrimers not only serve as a new class of efficient gene vectors, but also exhibit better transfection efficiency than ordinary dendrimers. With advanced equipment and experienced scientists, CD BioSciences provides high quality dendrimer fluorination services.

Introduction into Polymer Fluorination

In recent years, polymers have been widely used as non-viral vectors for DNA and siRNA delivery for gene therapy. However, most synthetic polymers are not ideal for gene delivery due to their moderate transfection effect and severe cytotoxicity. Therefore, modification of polymers by various ligands, e.g., lipids, glycans, peptides/proteins, fluorinated compounds, and nanoparticles, is expected to improve their transfection efficiency and cytotoxicity. Among these modification strategies, fluorinated polymers are of increasing interest because of their extra-fluorination effect in gene delivery. Fluorination of polymers is mainly achieved by two strategies: a) grafting fluorine chemicals onto polymers; b) direct copolymerization of fluorine-containing monomers with cationic monomers. In the second strategy, random fluorinated copolymers are much more effective than block copolymers.

Fluorination improves gene delivery efficiency of cationic polymers. (Lv J, et al., 2022)

Dendrimer Fluorination

When the dendrimer undergoes acetylation, PEGylation and glycosylation it can remove the surface cationic charge and reduce cytotoxicity and hemolytic activity. And the dendrimer undergo fluorination mainly to improve transfection efficiency. The fluorinated dendrimers have higher transfection efficiency and lower cytotoxicity and have a promising future in gene delivery. Fluorination can improve the performance of not only PAMAM dendrimers but also other dendrimers, such as poly (propylene mine) (PPI) and polylysine, and other hyperbranched polymers, such as polyethylenimine (PEI).

Advantages of Dendrimer Fluorination

Fluorination has been shown to be an effective strategy that can improve the transfection efficiency of polymers and can be applied to various dendrimers such as PAMAM, polyethylenimine (PEI) and polylysine (PLL). As a class of efficient gene carriers, fluorinated dendrimers exhibit good transfection efficiency attributed to increased cellular uptake, serum stability and endosomal escape, and have the following advantages.

• Excellent Transfection Effect
  One of the main advantages of fluorinated dendrimers is their low surface energy, the formation of complexes with genes at low concentrations and the formation of polymorphs at very low nitrogen to phosphorous (N/P) ratio. It has low cytotoxicity when gene transfection is performed at low N/P. Therefore, compared with other commercial transfection reagents, both in vivo and in vitro, fluorinated dendrimers show high transfection efficacy for gene therapy and effective prevention of tumor growth.
• High Cell/Tissue Penetration Ability
  Perfluorinated lipids (PFLs) have lipophobic and antifouling properties. When dendrimers are modified with PFLs, they can shield the positive charge on the polymer, thus reducing its interaction with biomolecules in tissues, with good uptake and endosomal escape ability.
• Providing Drug Efficacy
  When fluorinated dendrimers are used for drug delivery, they can increase cellular uptake of drugs, improve metabolic stability, enhance drug efficacy, and binding affinity for proteins.
• Significant Permeation Effects
  Fluorinated dendrimers have a significant permeation effect on biological barriers such as mucosal tissues.
• Gene Editing
  As an effective transfection tool, dendrimers undergo fluorination and can be used for in vivo delivery of large plasmids encoding Cas9 proteins and sgRNAs for CRISPR/Cas9 genome editing-based gene therapy.
• Other Advantages
  Fluorination of dendrimers also improves their serum stability and intracellular DNA release with proper size and zeta-potentials.

Synthesis of fluorinated PAMAM dendrimers by grafting heptafluorobutyric acid to the surface of G4-G7 PAMAM dendrimers. (Wang M, et al.,2016)

Our Services

As a fast growing and leading global provider of scientific research services and solutions, CD BioSciences offers you dendrimer fluorination services. We are committed to meeting all your detailed requirements and guarantee that all deliverables are subjected to rigorous quality testing.

Service Process

CD BioSciences is committed to helping our customers meet the growing and evolving demand for dendrimers products. We offer a wide range of services related to dendrimers and ensure quality and reliability of results as well as on-time delivery. If you are interested in our services or have any additional questions, please feel free to contact us, we are happy to hear from you and look forward to working with you.

References

1. Lv J.; et al. Fluorination Promotes the Cytosolic Delivery of Genes, Proteins, and Peptides. Acc Chem Res. 2022, 55: 722-733.
2. Wang M.; Cheng Y. Structure-activity relationships of fluorinated dendrimers in DNA and siRNA delivery. Acta Biomater. 2016, 46: 204-210.