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Amino-acid-based polyesteramine micelles and preparation method and application thereof

A technology based on polyester amine micelles and polyester amine glue, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., and can solve the problem of poor structural stability, high toxicity, antibacterial Single function and other problems, to achieve the effect of stable structure, controllable structure and good biocompatibility

Inactive Publication Date: 2018-11-06
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The problem to be solved by the present invention is: the existing amino acid-based polyester amine micelles have single antibacterial function, poor structural stability and high toxicity

Method used

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  • Amino-acid-based polyesteramine micelles and preparation method and application thereof
  • Amino-acid-based polyesteramine micelles and preparation method and application thereof
  • Amino-acid-based polyesteramine micelles and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] An amino acid-based antibacterial micelle, comprising an amino acid-based polyester amine high polymer, the micelle formed by the self-assembly of the high polymer, its preparation method is:

[0032] a) Synthesis of amino acid-based polyester amine random copolymer:

[0033] 0.132 moles of L-lysine, 0.132 moles of p-toluenesulfonic acid monohydrate, 0.06 moles of 1,4-butanediol and 250 milliliters of toluene were put into a round bottom flask, and stirred at 110°C overnight. After the product was cooled to room temperature, it was filtered, and isopropanol was added to react at 40°C. The product was precipitated at -20°C overnight and then dried to obtain Lys-4. Similarly, Arg-4, Phe-4 can be synthesized. Dissolve 7.76 grams of NA, 7.28 grams of PB, and 3.48 grams of Lys-4 in 20 milliliters of N,N-dimethylacetamide solvent, add 9.09 grams of triethylamine, and react overnight at 80°C. The ester was precipitated three times and dried for 24 hours to obtain an amino a...

Embodiment 2

[0037] An amino acid-based antibacterial micelle, comprising an amino acid-based polyester amine high polymer, the micelle formed by the self-assembly of the high polymer, its preparation method is:

[0038] a) Synthesis of amino acid-based polyester amine random copolymer:

[0039] 0.132 moles of L-lysine, 0.132 moles of p-toluenesulfonic acid monohydrate, 0.06 moles of 1,4-butanediol and 250 milliliters of toluene were put into a round bottom flask, and stirred at 110°C overnight. After the product was cooled to room temperature, it was filtered, and isopropanol was added to react at 40°C. The product was precipitated at -20°C overnight and then dried to obtain Lys-4. Similarly, Arg-4, Phe-4 can be synthesized. Dissolve 7.76 grams of NA, 7.28 grams of PB, and 3.48 grams of Lys-4 in 20 milliliters of N,N-dimethylacetamide solvent, add 9.09 grams of triethylamine, and react overnight at 80°C. The ester was precipitated three times and dried for 24 hours to obtain an amino a...

Embodiment 3

[0043] A degradable amino acid-based antibacterial micelle, comprising an amino acid-based polyester amine high polymer, the micelle formed by the self-assembly of the high polymer, its preparation method is:

[0044] a) Synthesis of amino acid-based polyester amine random copolymer:

[0045] 0.132 moles of L-lysine, 0.132 moles of p-toluenesulfonic acid monohydrate, 0.06 moles of 1,4-butanediol and 250 milliliters of toluene were put into a round bottom flask, and stirred at 110°C overnight. After the product was cooled to room temperature, it was filtered, and isopropanol was added to react at 40°C. The product was precipitated at -20°C overnight and then dried to obtain Lys-4. Similarly, Arg-4, Phe-4 can be synthesized. Dissolve 0.1 g of levofloxacin, 7.76 g of NA, 7.28 g of PB, and 3.48 g of Lys-4 in 20 ml of N,N-dimethylacetamide solvent, add 9.09 g of triethylamine, and react overnight at 80°C. The product was precipitated three times in ethyl acetate and dried for 24 h...

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Abstract

The invention discloses amino-acid-based polyesteramine micelles, a preparation method and application thereof in treating infection wounds. The amino-acid-based polyesteramine micelles are antibacterial micelles prepared by synthesizing amino-acid-based polyesteramine random copolymer from various natural amino acids, and wrapping or grafting the copolymer with an antibacterial drug. The preparation method includes: preparing amino-acid-based polyesteramine random copolymer; synthesizing polyesteramine copolymer grafted with an antibacterial drug, namely antibacterial polyesteramine; preparing polyesteramine solution with the polyesteramine random copolymer, mixing the polyesteramine solution with an antibacterial drug solution to obtain antibacterial micelles I; alternatively, preparingantibacterial polyesteramine solution with antibacterial polyesteramine to obtain antibacterial micelles II. Various copolymer materials can be synthesized herein by changing the ratio of raw components to a hydrophobic unit; compared with block copolymers, the amino-acid-based polyesteramine micelles have the advantages of good simplicity of preparation process, controllable structure and the like. The micelles prepared herein are of nano structure, have more stable structure and can gain improved antibacterial property.

Description

technical field [0001] The invention relates to an amino acid-based polyester amine micelle, a preparation method and its application, in particular to an amino acid-based polyester amine micelle that can be used to treat infected wounds, a preparation method and its application, and belongs to biodegradable functional materials technology field. Background technique [0002] In daily life, various pathogenic microorganisms are widely distributed and can grow and multiply rapidly under certain conditions. The existence of such bacteria will not only cause the decomposition, deterioration and corruption of materials, but also seriously endanger human health. . Bacterial wound infection is prone to occur during the treatment of chronic wounds, and has become one of the difficult problems to solve today. Bacterial wound infection is often due to the existence of bacterial biofilm, which can not only resist the destruction and decomposition of external drugs, but also produce ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K9/107A61K47/59A61K45/00A61P31/04
CPCA61K9/1075A61K45/00A61K47/59A61K47/6907A61P31/04
Inventor 吴德群朱婕韩华李发学王学利俞建勇
Owner DONGHUA UNIV
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