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A kind of anthracycline antitumor antibiotic compound micelle and its preparation method and application

An anti-tumor and anthracycline technology, applied in the field of biomedicine, can solve problems such as differences in physical and chemical properties, blanks, etc., and achieve the effects of uniform particle size, high encapsulation efficiency, and sustained drug release.

Active Publication Date: 2020-03-24
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the significant differences in physicochemical properties between anthracycline antitumor antibiotics and SAA, how to realize the simultaneous delivery of the two has become the biggest difficulty and challenge, and is also the key to realize their clinical combination
At present, there is no report on the compound preparation of SAA and anthracycline antitumor antibiotics, and the compound micelle drug-loading system loaded with anthracycline antitumor antibiotics and SAA is still blank.

Method used

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  • A kind of anthracycline antitumor antibiotic compound micelle and its preparation method and application
  • A kind of anthracycline antitumor antibiotic compound micelle and its preparation method and application
  • A kind of anthracycline antitumor antibiotic compound micelle and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation and characterization of compound nanomicelles loaded with doxorubicin and salvianolic acid A

[0041] Preparation of compound nanomicelles: 20 mg of salvianolic acid A and 100 mg of block copolymer mPEG-PCL were dissolved in 5 mL of acetone, and the organic solvent was removed by rotary evaporation at 55 °C to obtain the polymerization of salvianolic acid A Add 5 mL of ultrapure water to hydrate for 30-60 min, continue to add 0.5 mL of PBS buffer solution (10×) with pH 7.4 and 2 mL of doxorubicin aqueous solution (concentration 3 mg / mL), and stir electromagnetically at room temperature (350 rpm ×20 min) until the solution was completely clarified, and then filtered through a 0.22 μm sterile membrane to obtain compound nanomicelles co-loaded with doxorubicin and salvianolic acid A. At the same time, doxorubicin single-drug micelles without salvianolic acid A were prepared under the same conditions; 3 mg doxorubicin was dissolved in 1 mL ultrapure wa...

Embodiment 2

[0046] Example 2 Preparation of compound nanomicelle freeze-dried powder loaded with doxorubicin and salvianolic acid A

[0047] Dissolve 20 mg salvianolic acid A and 100 mg block copolymer mPEG-PCL in 5 mL acetone, remove the organic solvent by rotary evaporation at 55 °C, add 5 mL ultrapure water, and hydrate for 30-45 min to dissolve the drug film . At the same time, doxorubicin single-drug micelles without salvianolic acid A were prepared under the same conditions. 1–10 mg of doxorubicin was dissolved in 1 mL of ultrapure water to obtain a concentration of doxorubicin of (1–10) mg / mL of doxorubicin in water. Then, continue to add 0.5 mL of PBS buffer solution (10×) at pH 7.4 and 2 mL of doxorubicin aqueous solution (concentration 3 mg / mL), and stir electromagnetically at room temperature (300 rpm×30 min) until the solution is completely clear, and then, Filtration with a 0.22 μm bacteria-removing membrane to obtain compound nanomicelles co-loaded with doxorubicin and sal...

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Abstract

The invention discloses compound nano micelles simultaneously loaded with anthracycline antitumor antibiotics and salvianolic acid A, and a preparation method and an application thereof. The compoundmicelles contain a therapeutically effective amount of anthracycline antitumor antibiotics, salvianolic acid A and an amphiphilic high-molecular polymer; through combined action of electrostatic attraction between an alkaline group of the anthracycline antitumor antibiotics and an acidic group of salvianolic acid A and self-assembly of the amphiphilic high-molecular polymer in an aqueous medium, the two drugs are jointly stably wrapped in nano micelles by a simple physical encapsulation mode; the obtained compound micelles have uniform particle size, have the encapsulation rate of 95% or more,and has both the drug loading amount and the stability obviously better than those of single-drug micelles.

Description

technical field [0001] The invention relates to a compound nano-micelle based on an amphiphilic high molecular polymer material simultaneously carrying anthracycline anti-tumor antibiotics and salvianolic acid A, and provides a method for preparing the nano-micelle and its use, belonging to biological field of medical technology. Background technique [0002] Cancer is a kind of disease that seriously threatens human life and health. Traditional chemotherapy drugs are the mainstay of cancer clinical treatment. Among them, anthracycline anti-tumor antibiotics are a class of anti-tumor drugs whose main mechanism of action is to cause DNA chain breaks and structural damage. They have the characteristics of broad anti-tumor spectrum and are effective for hypoxic cells. , occupies an important position in the treatment of tumors, and is the core drug for the first-line treatment of acute leukemia, lymphoma, breast cancer, lung cancer, liver cancer and many other solid tumors, ma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K45/00A61K31/216A61K31/704A61K47/34A61P35/00
CPCA61K9/1075A61K31/216A61K31/704A61K45/00A61K47/34A61K2300/00
Inventor 许卉杨昕张迪许茜杨倩文张杰郝盛源
Owner YANTAI UNIV
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