Unlock instant, AI-driven research and patent intelligence for your innovation.

Polypeptide-polyacrylic acid copolymer and its prepn process

A technology of polyacrylic acid and block copolymer, which is applied in the direction of non-active components of polymer compounds, and can solve the problems of insensitivity to changes in pH value and difficulty in effectively controlling the molecular weight of polyacrylic acid

Inactive Publication Date: 2010-02-10
EAST CHINA UNIV OF SCI & TECH
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The former has the defect of insensitivity to changes in the pH value of the application environment, while the latter has the problem that the molecular weight of polyacrylic acid is difficult to effectively control

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Polypeptide-polyacrylic acid copolymer and its prepn process
  • Polypeptide-polyacrylic acid copolymer and its prepn process
  • Polypeptide-polyacrylic acid copolymer and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Add 20 grams of γ-benzyl-L-glutamate (PBLG) and 11 g of 4-dimethylaminopyridine (DMAP) into a three-necked flask with 50 ml of anhydrous tetrahydrofuran (THF), stir until completely dissolved, and place in an ice-salt bath Slowly add 5ml of α-bromoisobutyryl bromide dropwise to the above solution through a constant pressure funnel, and keep stirring. At this time, a white precipitate will form, and then stir and react at room temperature for 20 hours. The precipitate was filtered, and the filtrate was dialyzed with deionized water in a dialysis bag with a molecular weight cut-off of 3,500 for three days, and the deionized water was changed every three hours, and finally freeze-dried to obtain a white powdery solid, that is, the macromolecular initiator PBLG-Br.

[0030] Get synthetic dry good macroinitiator PBLG-Br, as the macroinitiator of synthesizing diblock copolymer, take cuprous bromide / pentamethyldiethylenetriamine (CuBr / PMDETA) as catalyst system, at 80 The bulk...

Embodiment 2

[0040] Dissolve 20 grams of γ-methyl-L-glutamate (PMLG) and 10 g of pyridine with 50 ml of anhydrous tetrahydrofuran (THF). After completely dissolving, add 5 ml of bromobutyryl bromide for amidation reaction to synthesize a macromolecular initiator PMLG-Br, adding tert-butyl acrylate, adopts bulk method to obtain polypeptide-poly-tert-butyl acrylate block copolymer through atom transfer radical polymerization (coordinating agent is 2,2'-bipyridyl, catalyst is CuCl) , and then hydrolyzed with trifluoroacetic acid to remove the tert-butyl ester to obtain a PBLG-PAA block copolymer, the structure of which is shown in formula (7).

[0041]

[0042] In formula (7), m=50, n=126.

Embodiment 3

[0044] Dissolve 20 grams of γ-ethyl-L-glutamate (PELG) and 8 g of triethylamine in 50 ml of anhydrous tetrahydrofuran (THF). After completely dissolving, add 5 ml of bromopropionyl bromide for amidation reaction to synthesize macromolecules Initiator PELG-Br, adding tert-butyl acrylate, adopts bulk method to obtain polypeptide-poly-tert-butyl acrylate through atom transfer radical polymerization (coordinating agent is pentamethyldiethylenetriamine (PMDETA), catalyst is CuCl) block copolymer, and then use trifluoroacetic acid to hydrolyze and remove the tert-butyl ester to obtain a PBLG-PAA block copolymer, the structure of which is shown in formula (8).

[0045]

[0046] In formula (8), m=645, n=68.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention relates to one kind of biodegradable polypeptide-polyacrylic acid copolymer in the structure as shown and its preparation process. The block copolymer is prepared through the first acylating polypeptide as the initial material, the subsequent atom transferring free radical polymerization of the acylated polypeptide and tert-butyl acrylate or tert-butyl methacrylate, and finalhydrolysis of the obtained polymer to obtain the target product. The biodegradable polypeptide-polyacrylic acid block copolymer may be used as the nanometer level release-controlling carrier of hydrophobic medicine. Compared with available polypeptide copolymer, the present invention has the advantages of precisely controlled hydrophilic component content and hydrophobic component content, simplepreparation and low cost.

Description

technical field [0001] The invention relates to a biodegradable polypeptide-polyacrylic acid copolymer and a preparation method thereof. Background technique [0002] Amphiphilic polypeptide copolymers, the nanomicelles formed by self-assembly have a narrow particle size distribution, and the numerous peptide bonds on the main chain are easily broken and degraded by proteases in vivo to generate non-toxic small molecules, which are widely used Copolymers for the preparation of nano drug carriers. [0003] The existing polypeptide copolymers used to prepare nano-drug carriers (drug-loaded micelles) are mainly amphiphilic polyether / polypeptide block copolymers (Chinese Journal of Pharmaceutical Sciences. 2002, 37 (7): 509-512) and Polypeptide graft copolymer with hydrophilic segment polyacrylic acid as main chain and hydrophobic polypeptide as side chain (such as polyacrylic acid / polypeptide graft copolymer reported in CN 1900144A). The former has the defect of insensitivity...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00C08F8/12C08G69/48A61K47/42C08F20/10A61K47/34
Inventor 刘峰杜海兵贲进肖建华严诚林嘉平
Owner EAST CHINA UNIV OF SCI & TECH