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Ternary complex nanometer system and preparation method and application thereof

A ternary compound and system technology, applied in the field of pharmacy, can solve the problems of easily induced drug resistance and single therapy of anti-tumor active small molecule compounds, so as to avoid poor quality uniformity, highly synergistic therapeutic functions, and simple industrial transformation technology Effect

Active Publication Date: 2019-05-28
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Technical problem to be solved: In order to overcome the deficiencies in the prior art, solve the defect that anti-tumor active small molecule compounds are easy to induce drug resistance in monotherapy, and improve the technical bottleneck of iron compounds used in tumor therapy drugs, the present invention provides a compound based on iron- Ternary composite nanosystem of small molecule anti-tumor active compound containing benzene ring-polyphenolic compound and its preparation method and application

Method used

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  • Ternary complex nanometer system and preparation method and application thereof
  • Ternary complex nanometer system and preparation method and application thereof
  • Ternary complex nanometer system and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0035] Embodiment 1: Preparation of Ferric Chloride / Tannic Acid / Doxorubicin Hydrochloride Ternary Composite Nanosystem

[0036] Accurately weigh ferric chloride, tannic acid, and doxorubicin hydrochloride in purified water according to a weight ratio of 4:2:5, and vortex to mix the ferric chloride solution and tannic acid solution prepared above. Mix and stir, inject anhydrous ethanol with a volume 5 times the total volume of the mixed solution of ferric chloride and tannic acid under stirring conditions, and continue stirring for 1 to 60 minutes. Add the doxorubicin hydrochloride solution to the above stirring system and continue to stir for 1-60 minutes, then add ammonia water with a volume 0.2 times the total volume of the mixed solution of ferric chloride and tannic acid, centrifuge, add water to the precipitate and redissolve, ultrasonic probe 8 ~30min to prepare a ternary composite nano system.

Embodiment 2

[0037] Example 2: Preparation of ferric citrate / tea polyphenol / daunorubicin hydrochloride ternary composite nanosystem

[0038] Accurately weigh ferric citrate, tea polyphenols, and daunorubicin hydrochloride in purified water according to the ratio of 4:6:9 by weight, vortex and mix, and mix the ferric citrate solution and tea polyphenols solution prepared above Mix and stir, inject anhydrous methanol with a volume 10 times the total volume of the ferric citrate and tea polyphenol mixed solution under stirring conditions, and continue stirring for 1 to 60 minutes. Add the daunorubicin hydrochloride solution to the above stirring system, continue to stir for 1-60 minutes, then add urea whose volume is twice the total volume of the mixed solution of ferric citrate and tea polyphenols, centrifuge, add water to the precipitate and redissolve, and ultrasonicate in a water bath 8 to 30 minutes to prepare a ternary composite nano system.

Embodiment 3

[0039] Example 3: Preparation of ferric citrate / tea polyphenol / doxorubicin hydrochloride ternary composite nanosystem

[0040] Accurately weigh ferric citrate, tea polyphenols, and doxorubicin hydrochloride in purified water according to a ratio of 4:6:9 by weight, vortex and mix, and mix the ferric citrate solution and tea polyphenols solution prepared above Mix and stir, inject anhydrous isopropanol with a volume 30 times the total volume of the ferric citrate and tea polyphenol mixed solution under stirring conditions, and continue stirring for 1 to 60 minutes. Add the doxorubicin hydrochloride solution to the above stirring system, continue to stir for 1-60 minutes, then add urea with a volume 0.4 times the total volume of the mixed solution of ferric citrate and tea polyphenols, centrifuge, add water to the precipitate and redissolve, and use the probe to sonicate 8 to 30 minutes to prepare a ternary composite nano system.

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Abstract

The invention discloses a ternary complex nanometer system and a preparation method and application thereof. The system comprises an iron compound, a benzene-ring-containing micromolecule antineoplastic active compound and a polyphenol compound; a weight ratio of the iron compound to the benzene-ring-containing micromolecule antineoplastic active compound to the polyphenol compound is (1 to 4):(2to 10):(5 to 20). Relative to the prior art, according to the invention, different micromolecule compounds or medicines can be stably assembled only by a physical assembling means; the formed complexnanometer medicine not only has an antineoplastic treatment effect of the micromolecule antineoplastic active compound, but also has a ferroptosis treatment effect that the iron compound reacts with the polyphenol compound are mediated on the basis of an intracellular Fenton reaction; moreover, the novel complex nanometer medicine formed by the preparation method disclosed by the invention furtherhas an outstanding photothermal effect; chemotherapy, ferroptosis treatment and photothermal therapy can be integrated into one whole body, take a synergistic effect, beneficiate each other and achieve an all-in-one combined antineoplastic treatment effect.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a novel antitumor pharmaceutical preparation, specifically a ternary composite nanosystem based on an iron compound-a small molecule antitumor active compound containing a benzene ring-polyphenolic compound and its preparation method and application. Background technique [0002] Cancer is one of the major diseases that threaten human health at present. As the main body of clinical cancer treatment, traditional chemotherapy drugs often fail to obtain satisfactory therapeutic effects due to low bioavailability and multi-drug resistance. Therefore, they are often used clinically. Combined medication. The combined use of chemotherapeutic drugs can produce synergistic effects and improve the therapeutic effect; and due to the different mechanisms of action of chemotherapeutic drugs, the emergence of multidrug resistance can be prevented to a certain extent. However, chemotherapy combination th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/194A61K31/704A61K31/136A61K31/403A61K31/337A61K31/519A61K31/196A61K31/4178A61K31/4745A61K47/10A61K47/46A61K47/22A61K47/26A61P35/00
CPCA61K31/136A61K31/194A61K31/196A61K31/337A61K31/403A61K31/4178A61K31/4745A61K31/519A61K31/704A61K47/10A61K47/22A61K47/26A61K47/46A61P35/00
Inventor 姚静熊慧蒋志杰
Owner CHINA PHARM UNIV
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