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High-efficiency and antibacterial polymeric micelle with high pH sensibility and biocompatibility and preparation method thereof

A technology of biocompatibility and polymer glue, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, antibacterial drugs, etc., which can solve the problem of inapplicable biomedical fields and poor antibacterial effect of polymers , poor antibacterial and antibacterial effects, etc., to achieve good bactericidal effects, improve antibacterial and bactericidal effects, and have a wide range of applications

Inactive Publication Date: 2012-10-03
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Although the polymer prepared above has certain antibacterial and antibacterial effects, its preparation method is relatively complicated, and the antibacterial effect of the polymer is not good. areas, especially difficult to apply to the human body for a long time
[0009] In view of the poor antibacterial and antibacterial effect of the current antibacterial polymers, we propose to use the self-assembly method of amphiphilic block polymers to prepare antibacterial polymeric micelles. antibacterial effect
The micelle can be used as a drug carrier, and has a good antibacterial and bactericidal effect, and the polymer has water solubility and biodegradability. The polymer micelle has good pH sensitivity, and its structure will change with the external pH. Changes due to the transformation of the value, it has a very broad application prospect in the field of biomedicine, and there is no related patent invention at home and abroad

Method used

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  • High-efficiency and antibacterial polymeric micelle with high pH sensibility and biocompatibility and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] (1) Macromolecular initiator PEO 43 -Synthesis of Br

[0035] 10g flake PEO and 250mL toluene were azeotropically distilled to remove excess water, the temperature of the system was lowered to room temperature, and replaced with an ice-water bath, 2mL triethylamine, 1.9mL 2-bromoisobutyryl bromide in 20mL toluene solution were added, The reaction was carried out for 40h, filtered, extracted, and the organic phase was collected, dried, filtered, precipitated, suction filtered, and vacuum-dried to obtain a white powdery macromolecular initiator PEO 43 -Br.

[0036] (2) ATRP synthetic polymer

[0037] 1g macroinitiator PEO 43-Br, 0.033 g catalyst cuprous bromide (CuBr), 0.078 g ligand bpy, 0.5 g monomer diethylaminoethyl methacrylate (DEA), 2 mL methanol solvent into a 50 mL round bottom flask, anhydrous Atom Transfer Radical Polymerization (ATRP) is carried out under the protective conditions of nitrogen or argon without oxygen at a temperature of 60 o C, for 24h. T...

Embodiment 2

[0046] (1) Macromolecular initiator PEO 43 -Synthesis of Br

[0047] 10g flake PEO and 250mL toluene were azeotropically distilled to remove excess water, the temperature of the system was lowered to room temperature, and replaced with an ice-water bath, 2mL triethylamine, 1.9mL 2-bromoisobutyryl bromide in 20mL toluene solution were added, The reaction was carried out for 40h, filtered, extracted, and the organic phase was collected, dried, filtered, precipitated, suction filtered, and vacuum-dried to obtain a white powdery macromolecular initiator PEO 43 -Br.

[0048] (2) ATRP synthetic polymer

[0049] 1g macroinitiator PEO 43 -Br, 0.033 g catalyst cuprous bromide (CuBr), 0.078 g ligand bpy, 0.8 g monomer diethylaminoethyl methacrylate (DEA), 2 mL methanol solvent into a 50 mL round bottom flask, anhydrous Atom Transfer Radical Polymerization (ATRP) is carried out under the protective conditions of nitrogen or argon without oxygen at a temperature of 60 o C, for 30h. ...

Embodiment 3

[0055] (1) Macromolecular initiator PEO 43 -Synthesis of Br

[0056] 10g flake PEO and 250mL toluene were azeotropically distilled to remove excess water, the temperature of the system was lowered to room temperature, and replaced with an ice-water bath, 2mL triethylamine, 1.9mL 2-bromoisobutyryl bromide in 20mL toluene solution were added, The reaction was carried out for 40h, filtered, extracted, and the organic phase was collected, dried, filtered, precipitated, suction filtered, and vacuum-dried to obtain a white powdery macromolecular initiator PEO 43 -Br.

[0057] (2) ATRP synthetic polymer

[0058] 1g macroinitiator PEO 43 -Br, 0.033 g catalyst cuprous bromide (CuBr), 0.078 g ligand bpy, 0.5 g monomer diethylaminoethyl methacrylate (DEA), 2 mL methanol solvent into a 50 mL round bottom flask, anhydrous Atom Transfer Radical Polymerization (ATRP) is carried out under the protective conditions of nitrogen or argon without oxygen at a temperature of 60 o C, for 24h. ...

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Abstract

The invention belongs to the field of macromolecular nano biological medicine materials, and in particular relates to a high-efficiency and antibacterial polymeric micelle with high pH sensibility and biocompatibility and a preparation method thereof. An amphipathic block polymer is subjected to self-assembly by a direct dissolution method to form the micelle; and the surface of the micelle has a large number of positive charges, so that the micelle has the effects of sterilizing and inhibiting bacteria in high efficiency under the condition that other antibiotics are not added. Simultaneously, the micelle has high biocompatibility and biodegradability. The polymeric micelle has high pH sensibility, and a structure of the polymeric micelle is changed with the change of the outside pH value, and multiple medicines can be wrapped by a core-shell structure of the micelle, so the polymeric micelle has a bright application prospect.

Description

technical field [0001] The invention belongs to the field of macromolecule nano biomedical materials, and in particular relates to a pH-sensitive, biocompatible and highly effective antibacterial polymer micelle and a preparation method thereof. Background technique [0002] In recent years, with the development of polymer synthesis methods (ATRP, RAFT, NMP, ROP, click chemistry) and characterization techniques, block polymers with various structures and functions have sprung up. Due to the differences in the properties of different segments of block polymers, block polymers are widely used in many fields. One of the most important applications is that block polymers are assembled into various forms in selective solvents. Nano / micro particles are possible. The main forms of polymer assemblies found so far are: spherical micelles, rod micelles, disc-shaped micelles, spherical vesicles, bowl-shaped vesicles, multilamellar vesicles, large composite vesicles, sheets, tubes, fib...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F220/34C08G65/00C08J3/03A61K31/785A61K47/32A61P31/04
Inventor 杜建忠路航
Owner TONGJI UNIV
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