Preparation method of pH (potential of hydrogen)/reduction response cascade release magnetic targeting drug carrier with core-shell structure

A core-shell structure, magnetic targeting technology, applied in medical preparations containing active ingredients, drug combinations, pharmaceutical formulations, etc., can solve the problems of premature drug release and controlled release effect, poor stability, carrier toxicity, etc. The effect of curative effect, improving enrichment, and reducing toxic and side effects

Inactive Publication Date: 2017-12-01
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the problems of poor stability, premature drug release (unsatisfactory controlled release effect), and toxicity of the carrier itself in the existing drug carriers, and provide a pH / reduction dual-responsive magnetic target with a core-shell structure Preparation method of drug-loaded nanoparticles

Method used

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  • Preparation method of pH (potential of hydrogen)/reduction response cascade release magnetic targeting drug carrier with core-shell structure
  • Preparation method of pH (potential of hydrogen)/reduction response cascade release magnetic targeting drug carrier with core-shell structure
  • Preparation method of pH (potential of hydrogen)/reduction response cascade release magnetic targeting drug carrier with core-shell structure

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 1. Referring to the literature (Biomaterials, 2009, 30:4716-4722), synthesize superparamagnetic ferric oxide nanoparticles SPION-COOH with surface carboxylation. Specific steps are as follows:

[0022] Weigh FeCl respectively according to the molar ratio of 2:1.1 3 ·6H 2 O and FeCl 2 4H 2 O, dissolved in HCl solution at pH 1.7. Under nitrogen protection and high-speed stirring, the mixed solution was injected into a three-necked flask filled with NaOH solution at a rate of 65mL / h. After the injection was completed, the temperature was raised to 78°C and kept at a constant temperature for 1 hour. Wash the obtained magnetic fluid to neutrality through magnetic separation, and finally disperse it with HCl solution with pH=3 and freeze-dry to obtain SPION. Weigh a certain amount of SPION and sodium citrate according to the mass ratio of 10:7, dissolve them in deionized water, react with ultrasound for 2 hours, and obtain SPION-COOH after magnetic separation.

[0023] ...

Embodiment 2

[0032] 1. Referring to the literature (Biomaterials, 2009, 30:4716-4722), synthesize superparamagnetic ferric oxide nanoparticles SPION-COOH with surface carboxylation. Specific steps are as follows:

[0033] Weigh FeCl respectively according to the molar ratio of 2:1.1 3 ·6H 2 O and FeCl 2 4H 2 O, dissolved in HCl solution at pH 1.7. Under nitrogen protection and high-speed stirring, the mixed solution was injected into a three-necked flask filled with NaOH solution at a rate of 60 mL / h. After the injection was completed, the temperature was raised to 78°C and kept at a constant temperature for 1 hour. The obtained magnetic fluid was washed with water to neutrality through magnetic separation, and finally dispersed with HCl solution with pH 3 and freeze-dried to obtain SPION. Weigh a certain amount of SPION and sodium citrate according to the mass ratio of 10:7, dissolve them in deionized water, react with ultrasound for 2 hours, and magnetically separate to obtain SPION...

Embodiment 3

[0040] 1. Referring to the literature (Biomaterials, 2009, 30:4716-4722), synthesize superparamagnetic ferric oxide nanoparticles SPION-COOH with surface carboxylation. Specific steps are as follows:

[0041] Weigh FeCl respectively according to the molar ratio of 2:1.1 3 ·6H 2 O and FeCl 2 4H 2 O, dissolved in HCl solution at pH 1.7. Under nitrogen protection and high-speed stirring conditions, the mixed solution was injected into a three-necked flask filled with NaOH solution at a rate of 75mL / h. After the injection was completed, the temperature was raised to 78°C and kept at a constant temperature for 1 hour. The obtained magnetic fluid was washed with water to neutrality through magnetic separation, and finally dispersed with HCl solution with pH 3 and freeze-dried to obtain SPION. Weigh a certain amount of SPION and sodium citrate according to the mass ratio of 10:7, dissolve them in deionized water, react with ultrasound for 2 hours, and magnetically separate to ob...

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Abstract

The invention relates to a preparation method of a pH (potential of hydrogen) / reduction response cascade release magnetic targeting drug carrier with a core-shell structure. Firstly, Dex-SS-NH2 and Dex-COOH and SPION-COOH are synthesized, secondly, the Dex-SS-NH2 and the SPION-COOH are combined with anti-cancer drugs such as DOX*HCl to obtain magnetic nanoparticles with reduction responsiveness, and the magnetic nanoparticles serve as a core and are subjected to electrostatic self-assembly with the Dex-COOH to obtain pH / reduction double-responsiveness drug carrying nanoparticles. The nanoparticles have good biocompatibility and superparamagetism, can stimulate responsiveness release under pH / reduction double action, improve curative effects, reduce toxic and side effects and have a wide application prospect in the field of biomedicine.

Description

technical field [0001] The invention belongs to the technical field of functional nanometer materials, and in particular relates to a preparation method of a magnetic targeting drug carrier with a pH / reduction response gradient release with a core-shell structure. Background technique [0002] Nano-drug carriers, especially stimuli-responsive nano-drug carriers, have attracted widespread attention as an effective drug delivery system. Stimulus-responsive drug carriers can respond to signals from external stimuli, such as small changes in the physical or chemical environment, and achieve the purpose of controlled release of drugs through corresponding changes in their own structures. The pH of different tissues and organs in the human body is different, and the pH between tumor tissue and normal tissue is also different. Usually the tumor tissue presents a weakly acidic environment (pH around 6.5), which is slightly lower than that of normal tissue (around 7.4), the pH of th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/02A61K31/704A61P35/00
Inventor 喻发全薛亚楠陶丽君周洋王建芝蔡宁谌伟明
Owner WUHAN INSTITUTE OF TECHNOLOGY
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