Dendrimer Acetylation Service

Acetylation is another way to reduce the toxicity of dendrimers, using the introduction of acetyl functional groups to the ends of dendrimers, which neutralizes the positive charge on their surfaces. With advanced equipment and experienced scientists, CD BioSciences offers high quality dendrimer acetylation services.

Introduction into Acetylation

In organic chemistry, acetylation is an organic esterification reaction with acetic acid by introducing an acetyl functional group (acetoxy group, CH3CO) into an organic compound - i.e., replacing the acetyl group with a hydrogen atom. Such compounds are termed acetate esters or simply acetates.

Dendrimer Acetylation

As a new class of artificial macromolecules, dendrimers have a tree-like topological structure, nanoscale size, excellent mono-dispersity, and well-defined numbers of interior pocket and surface functionality. Dendrimers have been widely used in biomedical fields in the past decade. Drugs and genes can either be encapsulated in interior pockets inside of dendrimers through non-covalent strategies such as hydrophobic, ionic, and hydrogen-bond interactions, or conjugated to the surface functionalities of dendrimers by covalent methods. In addition, dendrimers can effectively improve drug solubility and stability, reduce drug side effects, and adjust drug pharmacokinetics and pharmacodynamics.

Acetylation, PEGylation and glycosylation are all effective strategies to remove the cationic charge from the surface of dendrimers and reduce their cytotoxicity and hemolytic activity. Acetylation of dendrimers refers to a method of introducing acetyl functional groups to their termini, which can be easily tailored by adding appropriate amounts of acetic anhydride. The acetylation is efficient and simple compared to PEGylation, resulting in a lower ideal amount of acetylation by choosing the right ratio of acetic anhydride to dendrimer, in addition to a lower spatial site resistance of acetylation. Thus, acetylation is a simple and efficient method and one of the most advantageous.

Synthesis Route of Acetylated and Surface Acetylated and Interior-functionalized Dendrimers (with 1,3-Propane Sultone). (Hu J, et al., 2011)

Characteristics of Dendrimers After Acetylation

Acetylated dendrimers have increased water solubility, which is important in pharmacological and biological applications, in addition to the following characteristics.

• Reduced Cytotoxicity
  Acetylation of dendrimers can maintain high permeability and greatly reduce cytotoxicity.
• Improve Drug-carrying Capacity
  Acetylated dendrimers can not only improve drug-carrying capacity, but also improve drug pharmacokinetics.
• Cannot Load Hydrophobic Drugs
  The surface charge of dendrimers plays an important role in drug loading and delivery, especially in improving the water solubility of hydrophobic drugs due to the neutralization of surface amines on cationic dendrimers. Therefore, the acetylated dendrimers have limitations when used as drug carriers and cannot be loaded with hydrophobic drugs.
• Uncontrolled Drug Release
  The charge characteristics inside the dendrimer after acetylation depend on the pH value, and the internal quaternized amine will be deprotonated and uncharged under physiological conditions, resulting in the sudden release of the wrapped drug after administration.

Service Process

As a pioneer in biotechnology, CD BioSciences has grown to become one of the largest independent biotechnology companies in the world and is connected to millions of researchers and partners worldwide. CD BioSciences is experienced in organic chemistry and can provide you with dendrimer acetylation 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.

Reference

1. Hu J.; et al. Design of interior-functionalized fully acetylated dendrimers for anticancer drug delivery. Biomaterials. 2011, 32: 9950-9.