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PH response/hydrophobic group random copolymerization polymer, and preparation method and application thereof

A hydrophobic group and random copolymerization technology, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulations, powder delivery, etc., can solve the problems of increasing the pH response area and incomplete drug release.

Inactive Publication Date: 2013-05-08
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This pH-responsive / hydrophobic group random copolymerized amphiphilic polymer molecular brush structure can increase the pH-responsive area in the self-assembled micelles, effectively relieve the burst release under the premise of maintaining high drug loading, and make the pH-responsive -Micelle swelling-drug release presents a synchronous process, thereby improving the pH response sensitivity and release efficiency of micelles, improving the controlled release performance of micellar drug-loaded systems, and effectively solving the problem of drug release in previous materials. Thorough problem

Method used

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  • PH response/hydrophobic group random copolymerization polymer, and preparation method and application thereof
  • PH response/hydrophobic group random copolymerization polymer, and preparation method and application thereof
  • PH response/hydrophobic group random copolymerization polymer, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] (1) Synthesis of P(HEMA- co - t BMA)-Br (A:B=14:86, A represents the terminal hydroxyl group HEMA, B represents the pH response group t BMA, the ratio is mass percentage, the same below). Take a 50 mL reaction bottle, put the stirring bar and CuBr 2 (11.2 mg) was placed in a reaction bottle, sealed and then vacuum-passed argon three times. Sequentially inject solvent toluene (20 mL), hydroxyl-terminated monomer HEMA (1.2 mL) and pH-responsive monomer t Add BMA (9.430 mL) and ligand PMDETA (104 mL) into the reaction flask, and stir for 10 min to form the catalyst complex. Then the reducing agent Sn(Oct) 2 (202.5 mg) was added to the reaction flask, stirred for 5 min, and then the initiator EBriB (147 mL) was added, and then transferred to a 70°C oil bath and stirred for 2 h. After the reaction was completed, cool to room temperature, add 50 mL of tetrahydrofuran for dilution, and then remove the catalyst by filtering through a neutral alumina column, using tetrahy...

Embodiment 2

[0117] (1) Synthesis of P(HEMA- co - t BA)-Br (A:B=11:89). Take a 50 mL reaction bottle, put the stirring bar and CuBr 2 (22.3 mg) was placed in a reaction bottle, sealed and then vacuum-passed argon three times. The solvent anisole (20 mL), monomeric HEMA (0.6 mL) and t BA (6.035 mL) and ligand bpy (312.4 mg) were added into the reaction flask, and stirred for 10 min to form the catalyst complex. Then the reducing agent Sn(Oct) 2 (405.1 mg) was added to the reaction flask, stirred for 5 min, and then the initiator EBriB (147 mL) was added, and then transferred to a 60°C oil bath and stirred for 4 h. After the reaction was completed, cool to room temperature, add 50 mL of tetrahydrofuran for dilution, and then remove the catalyst by filtering through a neutral alumina column, using tetrahydrofuran as the eluent. The obtained solution was concentrated by rotary evaporation, then slowly added to 300 mL 0 °C methanol / water (1:1 volume ratio) for precipitation, washed twice...

Embodiment 3

[0141] (1) Synthesis of P(HEMA- co - t BMA)-Br (A:B=9:91). Take a 50 mL reaction bottle, put the stirring bar and CuBr 2 (8.9 mg) was placed in a reaction bottle, sealed and then vacuum-passed argon three times. The solvent toluene (20 mL), monomeric HEMA (1.2 mL) and t Add BMA (15.1 mL) and ligand PMDETA (83.5 mL) into the reaction flask, and stir for 10 min to form the catalyst complex. Then the reducing agent Sn(Oct) 2 (162 mg) was added to the reaction flask, stirred for 5 min, and then the initiator EBriB (147 mL) was added, then transferred to an 80°C oil bath and stirred for 1 h. After the reaction was completed, cool to room temperature, add 50 mL of tetrahydrofuran for dilution, and then remove the catalyst by filtering through a neutral alumina column, using tetrahydrofuran as the eluent. The obtained solution was concentrated by rotary evaporation, then slowly added to 300 mL 0 °C methanol / water (1:1 volume ratio) for precipitation, washed twice with deionize...

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Abstract

The invention discloses a pH response / hydrophobic group random copolymerization polymer, and a preparation method and application thereof. A hydrophobic group and pH response group random copolymer is obtained through electron transfer activator regeneration-atom transfer radical polymerization and ring-opening polymerization, and a pH response amphiphilic polymer brush is prepared by triggeringthe activators regenerated by electron transfer (ARGET) atom transfer radical polymerization (ATRP) of hydrophilic macromolecule monomers by the hydrophobic group and pH response group random copolymer used as macroinitiator, and performing selective hydrolysis reaction. The proportion of functional groups in the polymer molecule is easy to adjust and control; and a synthesis process is simple and the yield is high. Polymer micelle with an inner core formed by hydrophobic groups and a pH response groups, and an outer shell formed by hydrophilic groups can be obtained by a dialysis method; anda water insoluble medicament can be entrapped in the inner core of the micelle, the medicament can be subjected to sustained release in gastric juice, and can be released quickly and controllably under intestinal canal conditions.

Description

technical field [0001] The invention relates to the field of high molecular polymer materials for biomedicine, in particular to a pH responsive / hydrophobic group random copolymer and its preparation method and application. Background technique [0002] It is well known that oral administration is more acceptable to patients due to its low cost, flexible dose adjustment, ease of use, outpatient use, and better patient tolerance, thereby effectively improving treatment outcomes. However, because more than half of the drugs are hydrophobic or have poor water solubility (such as camptothecin, paclitaxel, nifedipine, etc.), resulting in poor absorption after oral administration and low bioavailability in the gastrointestinal tract, oral treatment of such drugs Applications still face enormous challenges. [0003] The nano-core-shell micelles formed by amphiphilic copolymers have many advantages, such as providing good stability in vivo and in vitro, improving the apparent water ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00C08F8/12C08G63/08C08F220/28C08F220/18C08G65/00A61K47/30A61K9/14
Inventor 章莉娟杨友强林文静郭新东
Owner SOUTH CHINA UNIV OF TECH
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