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Polyethylenimine-aliphatic polyester graft polymer as well as preparation method and nanometer particle thereof

A polyethyleneimine and aliphatic polyester technology, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, powder delivery, etc., can solve problems such as easy light-induced fading, improve biological activity, wide application prospects, Toxicity reduction effect

Inactive Publication Date: 2013-06-26
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, traditional organic fluorescent dyes also have some insurmountable defects in application, such as easy photofading, high toxicity, etc.

Method used

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  • Polyethylenimine-aliphatic polyester graft polymer as well as preparation method and nanometer particle thereof
  • Polyethylenimine-aliphatic polyester graft polymer as well as preparation method and nanometer particle thereof
  • Polyethylenimine-aliphatic polyester graft polymer as well as preparation method and nanometer particle thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0064] This embodiment is used to illustrate the synthesis of polyethyleneimine-polylactic acid graft polymer of the present invention:

[0065] (1) 0.1mmol of dried polyethyleneimine (purchased from Sigma-Aldrich, with a weight average molecular weight of 25,000) having a structure shown in formula (5) was mixed uniformly with 150mL dimethyl sulfoxide to obtain a mixture, and The mixture was uniformly mixed with 0.15 mol lactide (purchased from Alfar Aesar, with a purity of 97%, analytically pure), and dissolved for 1 h under nitrogen protection. Add 8 mL of triethylamine, and react at 85° C. for 15 h under the protection of nitrogen to obtain a mixture containing a reaction product of polyethyleneimine-polylactic acid grafted polymer. The dimethyl sulfoxide in the reaction product of this mixture was removed, and the reaction product after removing dimethyl sulfoxide was precipitated in 500mL water to obtain a solid product; Dry it in the oven for 48 hours, then extract it ...

Embodiment 2

[0070] This embodiment is used to illustrate the synthesis of polyethyleneimine-polyglycolide graft polymer of the present invention:

[0071] (1) 5mmol of dried polyethylenimine (purchased from Sigma-Aldrich company, with a weight average molecular weight of 600) having a structure shown in formula (5) is mixed with 150mL tetrahydrofuran to obtain a mixture, and the mixture is mixed with 75mmol Glycolide (purchased from Alfar Aesar, with a purity of 97%, analytically pure) was mixed uniformly and dissolved for 1 h under nitrogen protection. Add 1.5 mL of ethanolamine, and react at 70° C. for 10 h under the protection of nitrogen to obtain a mixture containing a reaction product of polyethyleneimine-polyglycolide graft polymer. The tetrahydrofuran in the mixture was removed, and the reaction product after the removal of tetrahydrofuran was precipitated in 500mL of water to obtain a solid product; the solid product was washed with water three times in turn, dried in a vacuum ov...

Embodiment 3

[0076] This embodiment is used to illustrate the synthesis of polyethyleneimine-polycaprolactone graft polymer of the present invention:

[0077] (1) 500 μmol of dried polyethyleneimine (purchased from Sigma-Aldrich, with a weight-average molecular weight of 15,000) having a structure shown in formula (5) is mixed with 150 mL N, N-dimethylformamide to obtain a mixture , and the mixture was uniformly mixed with 0.5 mol caprolactone (purchased from AlfarAesar Company, with a purity of 97%, analytically pure), and dissolved for 1 h under nitrogen protection. Add 5 mL of diethanolamine, and react at 80° C. for 12 h under the protection of nitrogen to obtain a mixture containing a reaction product of polyethyleneimine-polycaprolactone grafted polymer. N,N-dimethylformamide in the mixture was removed, and the reaction product after removing N,N-dimethylformamide was precipitated in 500mL of water to obtain a solid product; the solid product was washed with water three times successi...

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Abstract

The invention discloses a polyethylenimine-aliphatic polyester graft polymer as well as a preparation method of the polyethylenimine-aliphatic polyester graft polymer and a preparation method of a nanometer particle. The polyethylenimine-aliphatic polyester graft polymer has a structure as shown in formula (1), wherein a is an integral number from 10 to 500, b is the integral number from 10 to 500, R1-R3 are independently selected from one or more of the structures as shown in formula (2) to formula (4), n is the integral number from 12 to 240, x is the integral number from 12 to 240 and y is the integral number from 12 to 240. The polyethylenimine-aliphatic polyester graft polymer provided by the invention has excellent fluorescence performance and biocompatibility, and has extensive application in the medicine loading field and the cell tracking field.

Description

technical field [0001] The invention relates to a polyethyleneimine-aliphatic polyester graft polymer, a preparation method thereof and a nano particle. Background technique [0002] Polyethyleneimine is a kind of cationic polymer, which mainly has two types: linear and branched; linear polyethyleneimine contains all secondary amines, while branched polyethyleneimine has primary amines, secondary amines and Tertiary amino group. Polyethyleneimine is a very potential transfection reagent. Linear and branched polyethyleneimine and its corresponding derivatives have been widely used in gene therapy research, but the toxicity of polyethyleneimine limits its clinical application. Pastor-Perez studies have shown that linear and branched polyethyleneimine can autofluoresce; among them, linear polyethyleneimine has a strong fluorescence, and the quantum yield can reach 6%; while branched polyethyleneimine is only 1% (L . Pastor-Perez, Macromol. Rapid Commun. 2007, 28, 1404). The...

Claims

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Application Information

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IPC IPC(8): C08G63/685C08G63/08C08G73/04A61K9/14A61K47/34
Inventor 梁兴杰吴雁孙云曹伟鹏
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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