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Double-pH-response amphiphilic copolymer and preparation method and application thereof

An amphiphilic copolymer and a technology of the copolymer are applied in the field of the amphiphilic copolymer and its preparation, and can solve the problems of reducing the amount of the drug, weakening the efficacy of the drug and the like

Active Publication Date: 2017-01-11
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, recent studies have shown that while the hydrophilic shell provides protection for the drug delivery system, it also inhibits the uptake of the drug system by tumor cells (pinocytosis, phagocytosis, etc.), reducing the amount of drugs entering the cell. amount, thereby weakening the efficacy of the drug

Method used

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  • Double-pH-response amphiphilic copolymer and preparation method and application thereof
  • Double-pH-response amphiphilic copolymer and preparation method and application thereof
  • Double-pH-response amphiphilic copolymer and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0090] Example 1: Preparation of dual pH-responsive amphiphilic copolymer MPEG-Dliable-PAE-g-Chol

[0091] (1) Preparation of pH-responsive hydrophilic macromer MPEG-Dliable: put a stirring bar in a 50mL three-necked round-bottom flask, seal it with a reverse-mouthed rubber stopper, put nitrogen gas into one side port, and vent gas from the other side port , under inert gas protection and anhydrous conditions, the solvent DCM (15mL), catalyst DCC (41mg, 0.2mmol), DMAP (6.1mg, 0.05mmol), monomer MPEG (80mg, 0.02mmol), small molecule single Add FA (45mg, 0.3mmol) into the bottle, dissolve fully under stirring conditions, react at room temperature for 24 hours, filter the reaction solution to remove the precipitate, collect the filtrate and concentrate it by rotary evaporation and slowly add it to ten times the amount (volume ratio ) in cold isopropanol, put it in the refrigerator for 2h, collect the precipitate, wash the precipitate with isopropanol and diethyl ether to obtain a...

Embodiment 2

[0097] Example 2: Preparation of dual pH-responsive amphiphilic copolymer MPEG-Dliable-PAE-g-Chol

[0098] (1) Preparation of pH-responsive hydrophilic macromer MPEG-Dliable: put a stirring bar in a 50mL three-necked round-bottom flask, seal it with a reverse-mouthed rubber stopper, put nitrogen gas into one side port, and vent gas from the other side port , under inert gas protection and anhydrous conditions, solvent DCM (15mL), catalyst DCC (51.25mg, 0.25mmol), DMAP (12.2mg, 0.1mmol), monomer MPEG (40mg, 0.01mmol), small molecule Monomer FA (75 mg, 0.5 mmol) was added into the bottle, fully dissolved under stirring conditions, and reacted at room temperature for 24 hours, the reaction solution was filtered to remove the precipitate, the collected filtrate was concentrated by rotary evaporation and slowly added to ten times the amount (volume ) in cold isopropanol, put it in the refrigerator for 2h, collect the precipitate, wash the precipitate with isopropanol and diethyl et...

Embodiment 3

[0101] Example 3: Preparation of dual pH-responsive amphiphilic copolymer MPEG-Dliable-PAE-g-Chol

[0102] (1) Preparation of pH-responsive hydrophilic macromer MPEG-Dliable: put a stirring bar in a 50mL three-necked round-bottom flask, seal it with a reverse-mouthed rubber stopper, put nitrogen gas into one side port, and vent gas from the other side port , under inert gas protection and anhydrous conditions, the solvent DCM (15mL), catalyst DCC (10.25mg, 0.05mmol), DMAP (18mg, 0.15mmol), monomer MPEG (200mg, 0.05mmol), small molecule single FA (112.5mg, 0.75mmol) was added to the bottle, fully dissolved under stirring, and reacted at room temperature for 24 hours, the reaction solution was filtered to remove the precipitate, the filtrate was collected by rotary evaporation and concentrated, and then slowly added to ten times the amount (volume ) in cold isopropanol, put it in the refrigerator for 2h, collect the precipitate, wash the precipitate with isopropanol and diethyl ...

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Abstract

The invention relates to double-pH-response amphiphilic copolymer, the molecular formula of the double-pH-response amphiphilic copolymer is MPEG-Dliable-PAE-g-Chol, and the structure of the double-pH-response amphiphilic copolymer is as shown in formula I. The double-pH-response amphiphilic copolymer is copolymerized by hydrophilic block methoxy polyethylene glycol, hydrophobic cholesterol and pH response block poly(beta-amino ester). The double-pH-response amphiphilic copolymer has the advantages that the double-pH-response amphiphilic copolymer can self-assemble in an aqueous solution to obtain a nanoscale micellar system, the inner layer of the nanoscale micellar system is a hydrophobic core modified by cholesterol, the middle of the nanoscale micellar system is a pH-sensitive-response PAE layer, the shell of the nanoscale micellar system is hydrophilic block MPEG, the hydrophilic shell is connected sensitive middle layer through a pH-sensitive benzimide bond, the cell intake of a micelle drug-loading system is increased effectively while the requirements of high entrapment performance, stable system structure, long in-vivo circulation time, stability under neutral conditions and controllable drug release under weak acid conditions of hydrophobic drugs are satisfied, and accordingly drug bioavailability is increased, and a tumor treatment effect is optimized.

Description

technical field [0001] The invention belongs to the technical field of high molecular polymer materials for biomedicine, and in particular relates to a double pH-responsive amphiphilic copolymer and its preparation method and application. Background technique [0002] Tumor (cancer) is formed by the body under the action of various tumorigenic factors, and the cells of local tissues lose their normal regulation of their growth at the gene level, resulting in abnormal proliferation and differentiation. Once a tumor is formed, it does not stop growing due to the elimination of the cause. Its growth is not subject to normal physiological regulation of the body, but destroys normal tissues and organs, especially malignant tumors. Compared with benign tumors, their growth speed is faster and they show invasive growth. , prone to hemorrhage, necrosis, ulcers, etc., and often distant metastasis, resulting in body weight loss, weakness, anemia, loss of appetite, fever, and severe da...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/02C08G65/332C08G65/333A61K9/107A61K47/34A61K9/19
CPCA61K9/1075A61K9/19A61K47/34C08G65/3326C08G65/33306C08G81/025
Inventor 陈春英张灿阳徐梦真刘晶
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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