Polyethyleneimine-chitosan-octadecanoic acid grafting, preparation and application

Abstract

The invention provides a polyethyleneimine-chitosan-octadecanoic acid grafting, which is macromolecular substance, wherein parts of free amino groups on a chitosan chain are replaced by stearic acid or polyethyleneimine of which the weight-average molecular weight is 800Da. In the invention, on the basis of chitosan-octadecanoic acid grafting with the function of rapid cell absorbing, the polyethyleneimine with small molecular weight is modified, thereby improving the hydrophobicity of the original chitosan-octadecanoic acid grafting molecular structure, substantially increasing amino, improving the ion buffer capacity of molecular, and overcoming the toxicity of the polyethyleneimine. By the combination of rapid cell absorbing of the chitosan-octadecanoic acid grafting and the strong proton sponge effect of the polyethyleneimine, the invention can be applied to preparing the gene medicine so as to realize the high-level expression of the gene medicine and the effectiveness of oncogene therapy.

Description

technical field [0001] The invention relates to a novel cationic ternary graft and its synthesis method and application, specifically polyethyleneimine-chitosan-stearic acid graft and its synthesis method, and polyethyleneimine-chitosan-stearic acid The graft is used as a non-viral gene carrier in the preparation of gene medicine. Background technique [0002] Gene therapy refers to the transfer of exogenous genes into the diseased cells, and by restoring or increasing gene expression to correct the structural or functional disorder of the human gene, prevent the progression of the disease, kill the diseased cells, and inhibit the genetic material of the exogenous pathogen. copy, so as to achieve the purpose of treatment. Vectors that successfully release foreign genes in vivo are mainly divided into two categories: viral and non-viral vectors. Among them, the modified viral vector has higher transfection efficiency and is the main means of gene therapy. Viral vectors inc...

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Problems solved by technology

Studies have shown that this material has its unique advantages in terms of cytotoxicity and particle size control of dense DNA products; although key technologies including transferrin ligand modification and polyethylene glycol (PEG) grafting are used, but The problem of low transfection efficiency still exists

The previous research work of the inventor shows that the chitosan stearic acid graft obtained by hydrophobic modification of low molecular weight chitosan can form micelles by self-aggregation in aqueous medium, and the graft micelles have the ability of tumor cells to rapidly The function of ingestion, and has the characteristic of cationic, can close gene drug-plasmid DNA through electrostatic interaction, as a kind of non-viral gene carrier material preparation of gene drug research shows that the use of chitosan stearic acid graft prepared Genetic medicines have high gene expression efficiency compared with genetic medicines themselves, yet their expression efficiency is far lower than that of commercially available liposomes (Lipofectamine TM 2000) Expression of the prepared gene medicine

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