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Multi-drug self-aggregation composite nanoparticles as well as preparation method and application thereof

A composite nanoparticle and self-aggregation technology, applied in nanotechnology, nanomedicine, nanotechnology, etc., can solve the problems of well-studied toxic and side effects of carrier materials, no tumor killing effect, and increase the cost of pharmaceutical preparations, and achieve good synergistic treatment. High effect, stability and bioavailability, enhanced killing ability

Active Publication Date: 2014-02-05
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

[0005] Although drug carriers have many advantages, however, drug nanocarriers are only used as drug delivery tools and do not have tumor killing effects. The potential toxic and side effects of carrier materials are difficult to study clearly, so their clinical applications are greatly limited.
Moreover, due to the introduction of nano-carriers, the drug loading capacity is greatly reduced, additional metabolic burden is added, the cost of pharmaceutical preparations is increased, and more potential safety issues that are not yet understood

Method used

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  • Multi-drug self-aggregation composite nanoparticles as well as preparation method and application thereof
  • Multi-drug self-aggregation composite nanoparticles as well as preparation method and application thereof
  • Multi-drug self-aggregation composite nanoparticles as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0066] First, this example describes the preparation method of multi-drug self-polymerization composite nanoparticles, the method is as follows:

[0067] 1) Preparation of hydrophobic anticancer drug molecules into precursor nanofiber suspension: Add 100 μL of 0.5 mmol / L ethanol solution of 10-hydroxycamptothecin dropwise to 1 mL of deionized water in a 50°C water bath, stir magnetically for 5 minutes and then let stand , to obtain a precursor nanofiber suspension.

[0068] 2) Add 20 μL of 5 mmol / L doxorubicin hydrochloride aqueous solution dropwise to the precursor nanofiber suspension, the molar ratio of doxorubicin hydrochloride to 10-hydroxycamptothecin is 2:1, stir in a water bath at 50°C for 1 hour, and then ultrasonically disperse 30min.

[0069] 3) It is also preferred to remove free drug by centrifugation at 7500 g for 20 min, and then re-dissolve the drug nanoparticles on the filter membrane with deionized water.

[0070] The multi-drug self-polymerization composit...

Embodiment 2

[0074] This example describes that the preparation method of multi-drug self-polymerization composite nanoparticles is different from Example 1, but it can also realize the preparation of 10-hydroxycamptothecin / doxorubicin double-drug self-polymerization composite nanoparticles, the method is as follows:

[0075] Add 20 μL of 5 mmol / L doxorubicin hydrochloride aqueous solution and 100 μL of 0.5 mmol / L 10-hydroxycamptothecin ethanol solution (the molar ratio of doxorubicin hydrochloride to 10-hydroxycamptothecin is 2:1) dropwise into 1 mL of 50°C water bath After magnetic stirring for 1 h in deionized water, ultrasonic dispersion was performed for 30 min.

[0076] It is also preferred to remove free drug by ultrafiltration at 7500 g for 20 min followed by redissolving the drug nanoparticles on the filter membrane with deionized water.

[0077] The multi-drug self-aggregation composite nanoparticles prepared in this example were characterized by scanning electron microscopy, flu...

Embodiment 3

[0079] This example describes that the preparation method of multi-drug self-polymerization composite nanoparticles is not exactly the same as in Example 1, wherein changing the drug solvent and reaction conditions can also achieve the preparation of 10-hydroxycamptothecin / doxorubicin double-drug self-polymerization composite nanoparticles Preparation, the method is as follows:

[0080] 1) Preparation of hydrophobic anticancer drug molecules into precursor nanofiber suspension: add 100 μL of 0.5 mmol / L dimethyl sulfoxide (DMSO) solution of 10-hydroxycamptothecin dropwise to 1 mL of deionized water in a 60°C water bath , after 20 min of magnetic stirring, the precursor nanofiber suspension was obtained.

[0081] 2) Add 20 μL of 10 mmol / L doxorubicin hydrochloride aqueous solution dropwise to the precursor nanofiber suspension, the molar ratio of doxorubicin to 10-hydroxycamptothecin is 4:1, stir in a water bath at 60°C for 0.5h, and then ultrasonically disperse for 20min .

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Abstract

The invention discloses multi-drug self-aggregation composite nanoparticles as well as a preparation method and an application thereof. The multi-drug self-aggregation composite nanoparticles are formed by compounding at least one hydrophobic drug molecule and at least one water-soluble drug molecule, and are obtained through the following steps: dissolving the hydrophobic drug molecule in a good solvent to obtain a hydrophobic drug molecule solution; sequentially or simultaneously adding the hydrophobic drug molecule solution and the water-soluble drug molecule solution into a poor solvent of the hydrophobic drug molecule; heating, and performing magnetic stirring and ultrasonic treatment. The multi-drug self-aggregation composite nanoparticles contain no carrier, have high drug loading capacity and have no potential toxic or side effect brought by the carrier; the preparation method of the multi-drug self-aggregation composite nanoparticles are easy to operate and can be widely applied; the obtained nano-drug has a uniform size and a synergistic treatment effect.

Description

technical field [0001] The invention relates to the technical field of drug nanoparticles, in particular to a multidrug self-polymerization composite nanoparticle, its preparation method and application. Background technique [0002] Cancer has become one of the major threats to human health, and effective treatment of cancer has become an urgent task in scientific research. Chemotherapy, the treatment of cancer with drugs that kill cancer cells, is by far the most common cancer treatment. The tumor cell killing mechanisms of commonly used chemotherapeutic drugs are different. Usually, in order to improve the curative effect and reduce drug resistance, doctors will choose different chemotherapeutic drugs to be used in combination in the treatment plan. Two or more drugs will produce synergistic effects, which can Get better treatment results. Therefore, multi-drug combination therapy is the most effective way to treat cancer. [0003] Since most chemotherapeutic drugs cur...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K9/16B82Y5/00B82Y40/00A61P35/00
Inventor 梁兴杰陈飞赵元元
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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