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A kind of nanoparticle loaded with doxorubicin hydrochloride and its preparation method and application

A technology of doxorubicin hydrochloride and nano-particles, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., and can solve the effects of chemotherapy drugs on tissue and organ damage, drug activity, and side effects and other problems, to achieve the effect of preventing toxic side effects and myocardial cell damage, stable release curve, and high loading capacity

Active Publication Date: 2020-04-10
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

[0002] Cancer has become a serious disease that endangers human health in today's society. For the treatment of cancer, chemical drug therapy is the most commonly used clinical method at present. Chemotherapy is a systemic treatment. After the drug enters the human body, the chemotherapy drug will follow the blood The circulatory system covers most of the tissues and organs in the body. Although chemotherapy drugs can cause certain damage to tumors, they can also cause certain damage to normal tissues and organs in the body.
[0003] Using nanoparticles to load chemotherapy drugs to achieve efficient treatment of tumors is a commonly used method to reduce drug toxicity and improve drug targeting. High molecular polymers have good biocompatibility, so they are widely used in For the transportation of antitumor drugs, polyethylene glycol-polylactic acid-polyglycolic acid block copolymer (PEG-co-PLGA) commonly used in the prior art can form nanomicelles to coat various drug molecules, and has certain The biodegradability of the drug, the sustained release effect of the drug can be achieved during the degradation process, so it is often used as a load of anti-tumor drugs. Adriamycin is a commonly used anti-tumor drug, but the nano-micelle formed by PEG-co-PLGA When doxorubicin is coated, its drug loading capacity is very low. It is often necessary to chemically link doxorubicin and PEG-co-PLGA molecular chains through chemical bonds to increase the drug loading capacity. The above chemical means may affect the drug activity. have an impact, and even have toxic side effects

Method used

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  • A kind of nanoparticle loaded with doxorubicin hydrochloride and its preparation method and application
  • A kind of nanoparticle loaded with doxorubicin hydrochloride and its preparation method and application
  • A kind of nanoparticle loaded with doxorubicin hydrochloride and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0049] The nanoparticle 1 was prepared by the following steps:

[0050] Step (1), dissolve 20mg polyethylene glycol-polylactic acid-polyglycolic acid block polymer with number average molecular weight of 25000Da (containing 15mg polyethylene glycol block with number average molecular weight of 7000Da) in 4mL of dichloride In methane, solution A is obtained, and 2 mg of molecular formula is C 60 (OH) 22 The fullerol is dissolved in 1L of water to obtain solution B;

[0051] In step (2), 0.4 mg of doxorubicin hydrochloride was added to the solution B obtained in step (1), and a magnetic stirrer was used to stir at a speed of 100 rev / min for 24h in a dark environment at room temperature, and the mixture was uniform;

[0052] Step (3), take 40 mL of the solution after the uniform mixing in step (2) and add it to the solution A obtained in step (1) to obtain a mixed solution. The mixed emulsifier composed of Pluronic F68 emulsifier and polyvinyl alcohol 1799 with a mass ratio of...

Embodiment 2

[0054] The nanoparticles 2 were prepared by the following steps:

[0055] The only difference from Example 1 is that in step (1), the amount of polyethylene glycol-polylactic acid-polyglycolic acid block polymer added is 120 mg, and the number-average molecular weight is 15,000 Da, which contains 108 mg of 3,000 Da. polyethylene glycol blocks.

[0056] In Example 2, the nanoparticles 2 were obtained.

Embodiment 3

[0058] The nanoparticles 3 were prepared by the following steps:

[0059] The only difference from Example 1 is that the amount of fullerol added in step (1) is 5 mg.

[0060] Example 3 The nanoparticles 3 were obtained.

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Abstract

The invention provides a nanometer particle loaded with doxorubicin hydrochloride. The nanometer particle has a core-shell structure; an inner core is prepared from fullerenols; an outer shell is a polyethyleneglycol-polylactic acid-polyglycolic acid block polymer; the doxorubicin hydrochloride is loaded on the surface of the fullerenols inner core; the structure formula of the fullerenols is C2n(OH)m, wherein the n is a positive integer between 30 and 60; m is a positive integer being greater than or equal to 6; the obtained nanometer particles has the proper particle diaemters; the slow release of doxorubicin hydrochloride can be realized; the release curve is stable; the release is similar to linear release. Compared with a conventional treatment method using polymeric micelles as medicine carriers or a conventional treatment method not using a medicine carrying system, the nanometer particle has the advantages that the stability is high; the loaded quantity is high; the nanometer particle diameter in the blood plasma is not obviously changed in two weeks. By using the prepared particle as the doxorubicin hydrochloride carrier, the toxic and side effects and myocardial cell injury due to sudden release of the medicine can be effectively prevented; the nanometer particle is suitable for further popularization and application.

Description

technical field [0001] The invention relates to the field of nanocomposite materials, in particular to a nanoparticle loaded with doxorubicin hydrochloride and a preparation method and application thereof. Background technique [0002] Cancer has become a serious disease that endangers human health in today's society. For the treatment of cancer, chemotherapy is the most commonly used method in clinical practice. Chemotherapy is a systemic treatment method. The circulatory system covers most tissues and organs in the body. Although chemotherapy drugs can cause certain damage to tumors, chemotherapy drugs can also cause certain damage to normal tissues and organs in the body. [0003] The use of nanoparticles to load chemotherapeutic drugs to achieve efficient tumor treatment is a commonly used method to reduce drug toxicity and improve drug targeting. High molecular polymers have good biocompatibility, so they are widely used in For the transportation of antitumor drugs, po...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/10A61K31/704A61P35/00
CPCA61K9/5123A61K9/5146A61K31/704
Inventor 陈春英唐敬龙吴雁刘颖
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA