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Targeting preparation for resisting drug-resistant tumor, as well as preparation method and application thereof

A tumor and drug resistance technology, applied in the field of pharmaceutical preparations, targeted preparations for anti-drug-resistant tumors, and preparation, can solve problems such as restricting the application of tumor treatment, and achieve the effect of reducing toxic and side effects

Active Publication Date: 2014-05-07
哈尔滨医大药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Targeting preparation for resisting drug-resistant tumor, as well as preparation method and application thereof
  • Targeting preparation for resisting drug-resistant tumor, as well as preparation method and application thereof
  • Targeting preparation for resisting drug-resistant tumor, as well as preparation method and application thereof

Examples

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Embodiment 1

[0027] The structure of the targeted preparation for anti-drug-resistant tumor effect of this embodiment is as follows figure 1 Shown. The targeted preparation is composed 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] 1. In this example, a targeted preparation for anti-drug-resistant tumors was prepared according to the following method:

[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 min to obtain wine red citrate-protected gold nanoparticles with a particle size of 5 nm.

[0030] Step 2. Preparation of gold nanoparticles protected by polyethylene glycol (molecular weight 2000): Take 4 mL of 0.28 mM polyethylene glycol (molecular weight 200...

Embodiment 2

[0053] In this example, a targeted preparation against drug-resistant tumors was prepared according to the following method, and the experimental results are shown in Example 1:

[0054] Step 1. Preparation of gold nanoparticles protected by citrate: 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 min to obtain wine-red citrate-protected gold nanoparticles with a particle size of 10 nm.

[0055] Step 2. Preparation of gold nanoparticles protected by polyethylene glycol (molecular weight 5000): Take 4 mL of 0.28 mM polyethylene glycol (molecular weight 5000) aqueous solution and 3 mL of citrate-protected gold nanoparticles, mix and stir for 1 hour. After 72 hours of deionized water dialysis, gold nanoparticles protected by polyethylene glycol were obtained.

[0056] Step 3. Preparation of adriamycin hydrazone bond: Dissol...

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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 a targeted preparation for resisting drug-resistant tumors, a preparation method and application, 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 chemotherapeutic drugs have appeared in recent years, but the failure of malignant tumor chemotherapy is not uncommon. The main reason is the tumor multidrug resistance (MDR) phenomenon formed after long-term application of antitumor drugs. MDR means that in the course of chemotherapy, when tumor cells develop resistance to a certain therapeutic drug, they have cross-resistance to other anti-tumor drugs that have not been exposed to, have different structures, and have different mechanisms of action. MDR is a major proble...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K47/48A61P35/00
Inventor 靳翔
Owner 哈尔滨医大药业股份有限公司
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