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Cholesterol modified amphiphilic pH response pennicuius copolymer as well as preparation and micelle of copolymer

An amphiphilic and copolymer technology, which is applied in the direction of drug combination, emulsion delivery, organic active ingredients, etc., can solve problems such as difficult to obtain effects, and achieve the effect of enhancing loading performance, enhancing stability, and increasing stability

Active Publication Date: 2014-12-24
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, many studies have been conducted on the above-mentioned problems, and various polymer monomers are combined and copolymerized to obtain multifunctional copolymers, but it is still difficult to obtain the desired effect

Method used

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  • Cholesterol modified amphiphilic pH response pennicuius copolymer as well as preparation and micelle of copolymer
  • Cholesterol modified amphiphilic pH response pennicuius copolymer as well as preparation and micelle of copolymer
  • Cholesterol modified amphiphilic pH response pennicuius copolymer as well as preparation and micelle of copolymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Preparation of cholesterol-modified amphiphilic pH-responsive brush copolymer Chol-P(HEMA-co-DEA)-b-PPEGMA

[0058] (1) Preparation of amphiphilic pH-responsive brush copolymer P(HEMA-co-DEA)-b-PPEGMA: a stir bar and copper bromide (22.3mg, 1.0mmol) were placed in a 50mL dry eggplant-shaped bottle, Seal it with a reverse rubber stopper, vacuumize and pass argon three times. The solvent toluene (20mL), monomer HEMA (1.30g, 10mmol), DEA (6.48g, 35mmol), and ligand HMTETA (0.31mL, 1.2mmol) were sequentially added into the bottle with a syringe, and stirred for 10min to form the catalyst complex. Then the reducing agent Sn(Oct) 2 (0.40 g, 1.0 mmol) was dissolved in 2 mL of toluene and added to the reaction flask. After stirring for 5min, the initiator EBriB (0.15mL, 1.08mmol) was quickly added dropwise with a syringe. After stirring and reacting in an oil bath at 60°C for 6h, the monomer PEGMA (4.75g, 10mmol) was added, and the reaction was continued for 30h. ...

Embodiment 2

[0062] Example 2: Preparation of cholesterol-modified amphiphilic pH-responsive brush copolymer Chol-P(HEMA-co-DEA)-b-PPEGMA

[0063] (1) Preparation of amphiphilic pH-responsive brush copolymer P(HEMA-co-DEA)-b-PPEGMA: a stir bar and copper bromide (26.8mg, 0.8mmol) were placed in a 50mL dry eggplant-shaped bottle, Seal it with a reverse rubber stopper, vacuumize and pass argon three times. The solvent toluene (20mL), monomer HEMA (1.30g, 10mmol), DEA (6.475g, 40mmol), and ligand HMTETA (0.31mL, 1.2mmol) were sequentially added into the bottle with a syringe, and stirred for 10min to form the catalyst complex. Then the reducing agent Sn(Oct) 2 (0.486 g, 1.2 mmol) was dissolved in 2 mL of toluene and added to the reaction flask. After stirring for 5min, the initiator EBriB (0.17mL, 1.2mmol) was quickly added dropwise with a syringe. After stirring and reacting in an oil bath at 70°C for 5h, the monomer PEGMA (14.25g, 30mmol) was added and the reaction was continued for 24h. ...

Embodiment 3

[0065] Example 3: Preparation of cholesterol-modified amphiphilic pH-responsive brush copolymer Chol-P(HEMA-co-DEA)-b-PPEGMA

[0066](1) Preparation of amphiphilic pH-responsive brush copolymer P(HEMA-co-DEA)-b-PPEGMA: a stir bar and copper bromide (26.8mg, 0.12mmol) were placed in a 50mL dry eggplant-shaped bottle, Seal it with a reverse rubber stopper, vacuumize and pass argon three times. The solvent toluene (20mL), monomer HEMA (4.68g, 36mmol), DEA (2.775g, 15mmol), and ligand HMTETA (0.31mL, 1.2mmol) were sequentially added into the bottle with a syringe, and stirred for 10min to form the catalyst complex. Then the reducing agent Sn(Oct) 2 (0.486 g, 1.2 mmol) was dissolved in 2 mL of toluene and added to the reaction flask. After stirring for 5min, the initiator EBriB (0.17mL, 1.2mm o l), after stirring and reacting in an oil bath at 90° C. for 7 h, the monomer PEGMA (14.25 g, 30 mmol) was added, and the reaction was continued for 48 h. Cool the reaction solution to r...

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Abstract

The invention belongs to the technical field of preparation of biomedical high molecular polymer materials and discloses a cholesterol modified amphiphilic pH response pennicuius copolymer and a preparation method and a micelle system prepared based thereof. The copolymer has a structure shown in the formula I in the specification, wherein x is 10-36, y is 15-40 and z is 8-30. The copolymer is obtained by virtue of irregular copolymerization of a hydrophilic block hydroxyethyl methylacrylate, hydrophobic cholesterol and pH response block methacrylic acid N, N-diethyl aminoethyl combined with hydrophilic poly(ethylene glycol) methyl ether methacrylate. The copolymer is dissolved in a solvent to obtain a nanoscale micelle system, wherein the inner layer is a cholesterol modified hydrophobic chain segment, the middle layer is a pH response chain segment and the shell is a hydrophilic chain segment, so that the function of high entrapment performance, stable existence of a neutral condition and quick release in a weak acidic condition is achieved. By adjusting the proportions of the blocks in the polymer, the release rates of medicines can be regulated to satisfy the release requirements on different drugs.

Description

technical field [0001] The invention belongs to the technical field of preparation of biomedical polymer materials, and in particular relates to a cholesterol-modified amphiphilic pH-responsive brush copolymer, a preparation method and a micelle system prepared based on the same. Background technique [0002] Cancer is a disease that seriously threatens human health. Among the existing cancer treatment methods, chemotherapy has the best effect. However, chemotherapy drugs are also a double-edged sword. On the one hand, it has an irreplaceable role in cancer treatment. On the other hand, while it kills cancer cells, it also has great toxic side effects on normal cells. Most of the existing anti-cancer chemical drugs have defects such as poor water solubility, low bioavailability, and non-specific distribution in the body. [0003] In order to overcome the above-mentioned defects, make anticancer drugs achieve effective doses and reduce side effects on normal tissues, a new t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F220/34C08F220/28C08F8/00A61K47/34A61K9/107A61K31/704A61P35/00
Inventor 章莉娟姚娜张灿阳林文静赵斌
Owner SOUTH CHINA UNIV OF TECH
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