Amphipathic three block copolymer and its preparation method and application

A triblock and copolymer technology, which is used in pharmaceutical formulations, medical preparations with inactive ingredients, etc.

Inactive Publication Date: 2008-09-17
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies on PEG / aliphatic polyester / cationic polymer amphiphilic triblock copolymers have not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Add 0.01 g of potassium hydride into the polymerization reactor, weigh 0.4986 g of polyethylene glycol monomethyl ether with a relative molecular mass of 2000 according to the requirements of the equivalent substance mass, and prepare it into a tetrahydrofuran solution and inject it into the polymerization reactor. React at 25°C for 2 hours; inject 1.4959g of lactide into the polymerization reactor, inject 0.4986g of methacrylic acid-N,N-dimethylaminoethyl ester after 2 hours of reaction, continue the reaction for 2 hours, add degassed methanol to terminate the reaction ; Precipitate and purify the triblock copolymer dissolved in tetrahydrofuran with a large amount of n-hexane at 0°C, repeat the precipitation three times, and then dry it in a vacuum oven at 40°C to obtain a compound with good biocompatibility, biodegradability and pH sensitive cationic amphiphilic triblock copolymer.

[0020] The amphiphilic tri-block copolymer prepared in this example self-assembled in...

Embodiment 2

[0022] Add 0.1 g of potassium hydride into the polymerization reactor, weigh 4.9863 g of polyethylene glycol monomethyl ether with a relative molecular mass of 2000 according to the requirements of the equivalent substance mass, and prepare it into a tetrahydrofuran solution and inject it into the polymerization reactor. React at 25°C for 2 hours; inject 1.0685g of lactide into the polymerization reactor, inject 1.0685g of methacrylic acid-N,N-dimethylaminoethyl ester after 2 hours of reaction, continue the reaction for 2 hours, add degassed methanol to terminate the reaction ; Precipitate and purify the triblock copolymer dissolved in tetrahydrofuran with a large amount of n-hexane at 0°C, repeat the precipitation three times, and then dry it in a vacuum oven at 40°C to obtain a compound with good biocompatibility, biodegradability and pH sensitive cationic amphiphilic triblock copolymer.

Embodiment 3

[0024] Add 0.05 g of potassium hydride into the polymerization reactor, weigh 2.4931 g of polyethylene glycol monomethyl ether with a relative molecular mass of 2000 according to the requirements of the equivalent substance mass, and prepare it into a tetrahydrofuran solution and inject it into the polymerization reactor. React at 25°C for 2 hours; inject 3.4281g of lactide into the polymerization reactor, inject 0.3116g of methacrylic acid-N,N-dimethylaminoethyl ester after 2 hours of reaction, continue the reaction for 2 hours, add degassed methanol to terminate the reaction ; Precipitate and purify the triblock copolymer dissolved in tetrahydrofuran with a large amount of n-hexane at 0°C, repeat the precipitation three times, and then dry it in a vacuum oven at 40°C to obtain a compound with good biocompatibility, biodegradability and pH sensitive cationic amphiphilic triblock copolymer.

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Abstract

The invention relates to a polyethylene glycol/aliphatic polyester/cationic polymer amphiphilic triblock copolymer. The copolymer contains a hydrophilic non-ionic polymer block, a hydrophobic block and a pH-sensitive cationic polymer block. Potassium hydride is taken as an initiator, the polyethylene glycol and the aliphatic polyester monomers and the cationic monomer are sequentially added in a polymerization reactor for respective reaction, methanol is added for terminating the reaction; n-hexane is used for the precipitation and the purification of the triblock copolymer in tetrahydrofuran, the precipitation is repeated for 3 times, and a product undergoes the vacuum drying. The copolymer can form a micelle or a nanoparticle by self-assembly in a water medium, wherein, a core of a loading hydrophobic drug is formed by clustering the hydrophobic cationic polyester block, the polyethylene glycol block is assembled into a hydrophilic shell, thus having the functions of stabilizing the micelle and effectively avoiding the capture and protein absorption of a reticuloendothelial system of an organism; the cationic polymer block can be further acted with DNA, protein, peptide and other biological macromolecules, thus forming the biodegradable and pH-sensitive drug-loading polymer micelle or the nanoparticle which can be further dispersed,.

Description

technical field [0001] The invention relates to an amphiphilic tri-block copolymer, its preparation method and application, in particular to a polyethylene glycol / aliphatic polyester / cation polymer amphiphilic tri-block copolymer, its preparation method and application. Background technique [0002] Aliphatic polyesters represented by polylactic acid and polycaprolactone have good biocompatibility and excellent drug permeability, are an ideal hydrophobic drug carrier, and have been used in vaccines, cell growth inhibition Controlled release of protein and polypeptide drugs such as drug and insulin. Aliphatic polyester nanoparticles have a hydrophobic surface, making them easy to be adsorbed by proteins and recognized and captured by macrophages of the reticuloendothelial system. Therefore, it is very necessary to carry out hydrophilic modification on the surface of aliphatic polyester nanoparticles. The aliphatic polyester blocked by a hydrophilic polyethylene glycol (PEG)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08G65/48C08G63/91C08G63/66A61K47/30
Inventor 邓联东董岸杰翟英雷蔺晓娜
Owner TIANJIN UNIV
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