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A kind of anti-drug-resistant tumor targeting preparation, preparation method and application

A targeting and preparation technology, which is applied in the field of preparation, pharmaceutical preparations, and targeted preparations against drug-resistant tumors, can solve problems such as limiting the application of tumor treatment, and achieve the effect of reducing toxic and side effects

Active Publication Date: 2017-04-05
哈尔滨医大药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The above problems have always limited its application in tumor treatment. The current technical problem that needs to be solved urgently is to provide a drug delivery system for doxorubicin to overcome the problem that a single drug cannot exert good efficacy against drug-resistant tumors.

Method used

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  • A kind of anti-drug-resistant tumor targeting preparation, preparation method and application
  • A kind of anti-drug-resistant tumor targeting preparation, preparation method and application
  • A kind of anti-drug-resistant tumor targeting preparation, preparation method and application

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Embodiment 1

[0027] The structure of the targeted preparation of the anti-drug-resistant tumor effect of this embodiment is as follows: figure 1 shown. The targeting preparation consists of four parts: A, B, C and D. Part A is gold nanoparticles, part B is polyethylene glycol, part C is hydrazone bond, and part D is doxorubicin.

[0028] One, the present embodiment prepares the targeting preparation of anti-drug-resistant tumor according to the following methods:

[0029] Step 1. Preparation of citrate-protected gold nanoparticles: Dissolve 50 mg of sodium citrate in 50 mL of deionized water, add 0.615 mL of chloroauric acid with a concentration of 0.02 g / mL, and then add 1.2 mL of boron with a concentration of 0.1 M sodium hydride. Stir for 30 minutes to obtain wine red citrate-protected gold nanoparticles with a particle size of 5 nm.

[0030] Step 2. Preparation of polyethylene glycol (molecular weight: 2,000)-protected gold nanoparticles: 4 mL of a polyethylene glycol (molecular wei...

Embodiment 2

[0053] This embodiment prepares the targeted preparation of anti-drug-resistant tumor according to the following method, and the experimental results are shown in Example 1:

[0054] Step 1. Preparation of citrate-protected gold nanoparticles: Dissolve 50 mg of sodium citrate in 50 mL of deionized water, add 0.615 mL of chloroauric acid with a concentration of 0.02 g / mL, and then add 1.2 mL of sodium sulfite with a concentration of 0.1 M . Stir for 30 minutes to obtain wine red citrate-protected gold nanoparticles with a particle size of 10 nm.

[0055] Step 2. Preparation of polyethylene glycol (molecular weight: 5,000)-protected gold nanoparticles: 4 mL of polyethylene glycol (molecular weight: 5,000) aqueous solution with a concentration of 0.28 mM and 3 mL of citrate-protected gold nanoparticles were mixed and stirred for 1 h. Deionized water was dialyzed for 72 hours to obtain polyethylene glycol-protected gold nanoparticles.

[0056] Step 3. Preparation of doxorubicin ...

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Abstract

The invention relates to a medicinal preparation, particularly relates to a targeting preparation for resisting drug-resistant tumor, as well as a preparation method and application thereof, and belongs to the technical field of pharmaceuticals. The targeting preparation for resisting drug-resistant tumor comprises a part A which is gold nanoparticles, a part B which is polyethylene glycol, a part C which is a hydrazone bond, and a part D which is a chemotherapeutic drug. The targeting gold nanoparticle drug delivery system prepared by linking amycin and gold nanoparticles via hydrazone bond has acid sensitivity, and can specifically release amycin to an environment with pH less than 6 to realize specific response to microenvironment (lysosome and endosome, pH less than 6) in drug-resistant tumor. The targeting preparation provided by the invention meets the needs for drug-resistant tumor therapy and can be used for reducing toxic and adverse side effects of amycin.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a targeted preparation for resisting drug-resistant tumors, a preparation method and application thereof, and belongs to the technical field of pharmacy. Background technique [0002] At present, chemotherapy has become an indispensable and important treatment method for malignant tumors along with surgical treatment and radiotherapy. In the process of clinical chemotherapy, new chemotherapy drugs have emerged in recent years, but the failure of chemotherapy for malignant tumors is not uncommon. The main reason is the phenomenon of multidrug resistance (MDR) formed after long-term use of anticancer drugs. MDR refers to the cross-resistance to other anti-tumor drugs that have not been exposed to, have different structures and different mechanisms of action when tumor cells develop resistance to a certain therapeutic drug during chemotherapy. MDR is a major problem in cancer treatme...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/704A61K47/60A61P35/00
Inventor 靳翔
Owner 哈尔滨医大药业股份有限公司
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