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PH-responsive adriamycin carrier-free nano-drug as well as preparation method and application thereof

A nano-drug and doxorubicin technology, applied in the field of biomedical nano-materials, can solve the problems of low drug loading and high toxicity of organic solvents, and achieve the effects of clear components, easy quality control, and green and simple preparation process.

Pending Publication Date: 2020-12-04
TAIYUAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the present invention, the carboxyl-rich citrate and the amine group on doxorubicin are hydrogen-bonded to form nano-medicines, so as to solve the problems of low drug loading and high toxicity of organic solvents in the prior art

Method used

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  • PH-responsive adriamycin carrier-free nano-drug as well as preparation method and application thereof
  • PH-responsive adriamycin carrier-free nano-drug as well as preparation method and application thereof
  • PH-responsive adriamycin carrier-free nano-drug as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of pH-responsive doxorubicin carrier-free nanomedicine

[0032] (1) Take a brown reaction bottle, first add 1.0mL of 1.0M sodium citrate solution, then add 200μg of DOX to it, and use an ultrasonic instrument to fully dissolve and mix the material evenly;

[0033] (2) The above mixed solution was placed on an infrared heating electromagnetic stirrer at room temperature and protected from light for 6 hours;

[0034] (3) Centrifuge at 12000rpm at high speed after the reaction is finished, and wash 4 times with sodium citrate solution, and freeze-dry to obtain the target product after washing. Collect all washing solutions in brown reagent bottles and store them in the dark until the drug loading of doxorubicin is determined. The absorbance of doxorubicin at 486nm was detected by ultraviolet-visible spectroscopic method, and the adsorption amount of DOX was calculated. The calculation shows that the loading rate of doxorubicin can be as high as 94.25±3.43%.

Embodiment 2

[0036] Preparation of pH-responsive doxorubicin carrier-free nanomedicine

[0037] (1) Take a brown reaction bottle, first add 1.0mL of 1.0M sodium citrate solution, then add 600μg DOX to it, and use an ultrasonic instrument to fully dissolve and mix the material evenly;

[0038] (2) The above mixed solution was placed on an infrared heating electromagnetic stirrer at room temperature and protected from light for 6 hours;

[0039] (3) Centrifuge at 12000rpm at high speed after the reaction is finished, and wash 4 times with sodium citrate solution, and freeze-dry to obtain the target product after washing. Collect all washing solutions in brown reagent bottles and store them in the dark until the drug loading of doxorubicin is determined. The absorbance of doxorubicin at 486nm was detected by ultraviolet-visible light spectrometry, and the adsorption amount of DOX was calculated. The calculation shows that the loading rate of doxorubicin can be as high as 94.85%±3.12%.

Embodiment 3

[0041] Preparation of pH-responsive doxorubicin carrier-free nanomedicine

[0042] (1) Take a brown reaction bottle, first add 1.0mL of 1.0M sodium citrate solution, then add 1000μg of DOX to it, and use an ultrasonic instrument to fully dissolve and mix the material evenly;

[0043] (2) The above mixed solution was placed on an infrared heating electromagnetic stirrer at room temperature and protected from light for 6 hours;

[0044] (3) Centrifuge at 12000rpm at high speed after the reaction is finished, and wash 4 times with sodium citrate solution, and freeze-dry to obtain the target product after washing. Collect all washing solutions in brown reagent bottles and store them in the dark until the drug loading of doxorubicin is determined. The absorbance of doxorubicin at 486nm was detected by ultraviolet-visible spectroscopic method, and the adsorption amount of DOX was calculated. The calculation shows that the loading rate of doxorubicin can be as high as 95.76±1.93%. ...

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Abstract

The invention provides a pH-responsive doxorubicin carrier-free nano-drug as well as a preparation method and application thereof The preparation method of the pH-responsive doxorubicin carrier-free nano-drug is characterized in that citrate rich in carboxyl is combined with amido on doxorubicin through hydrogen bonds to prepare the pH-responsive doxorubicin carrier-free nano-drug. The pH-responsive doxorubicin carrier-free nano-drug avoids toxic and side effects caused by introduction of a nano-carrier, has the advantages of high safety, strong stability, strong drug release capability and the like, is mild in reaction conditions, green and simple in synthesis process, cheap and easily available in raw materials and easy for industrial large-scale production, and can be applied to preparation of antitumor drugs.

Description

technical field [0001] The invention relates to the technical field of biomedical nanomaterials, in particular to a pH-responsive doxorubicin carrier-free nanomedicine, a preparation method thereof, and an application of the medicine in the preparation of antitumor medicines. Background technique [0002] At present, the main treatment methods for cancer include surgery, chemotherapy, and radiotherapy, as well as molecular targeted therapy that has emerged in recent years. But in fact, these treatment methods all have certain disadvantages. They cannot eradicate all cancer cells, and will cause cancer recurrence, and at the same time, some normal cells will be damaged, causing toxic and side effects to the body. [0003] At present, the nanotechnology drug delivery system is a hot spot in medical research. It loads anti-tumor drugs with hydrogen bond force, accurately delivers the drugs to the lesion, reduces the toxicity of free doxorubicin, and realizes accurate diagnosis ...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/69A61K31/704A61P35/00
CPCA61K47/542A61K47/6929A61K31/704A61P35/00
Inventor 李林张彩凤宋吉祥
Owner TAIYUAN NORMAL UNIV
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