Folic acid-berberine nano-drug and preparation method and application thereof

A nano-drug, berberine technology, applied in the direction of drug combination, pharmaceutical formula, anti-tumor drugs, etc., can solve the problems that have not been seen before, achieve the effect of confirming the result, reducing the risk of drug resistance, and enhancing the efficacy of the drug

Active Publication Date: 2020-06-19
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] There is no related report

Method used

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  • Folic acid-berberine nano-drug and preparation method and application thereof
  • Folic acid-berberine nano-drug and preparation method and application thereof
  • Folic acid-berberine nano-drug and preparation method and application thereof

Examples

Experimental program
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Embodiment 1

[0040] The preparation of embodiment 1 solution

[0041] 23.39 mg (0.06953 mmol) of berberine was dissolved in 3.48 mL of DMSO to prepare a 0.02 mmol / mL solution of berberine in DMSO. Dissolve 30.00 mg (0.06797 mmol) of folic acid in 3.40 mL of DMSO to prepare a DMSO solution with a folic acid concentration of 0.02 mmol / mL.

[0042] 22.46 mg (0.06677 mmol) of berberine was dissolved in 1.67 mL of DMSO to prepare a DMSO solution with a berberine concentration of 0.04 mmol / mL. Dissolve 26.06 mg (0.05904 mmol) of folic acid in 1.48 mL of DMSO to prepare a DMSO solution with a folic acid concentration of 0.04 mmol / mL.

[0043] Dissolve 0.67 g (0.01675 mol) of NaOH in 13.40 mL of ultrapure water to prepare a 0.00125 mmol / μL NaOH aqueous solution.

[0044] The application process for preparing folic acid (FA)-berberine (BBR) self-assembled nanomedicine is as follows figure 1 shown.

Embodiment 2

[0045] Example 2 Folic acid: berberine molar ratio is 1:1 system

[0046]In a 50 mL round bottom flask, first add 0.50 mL of berberine in DMSO solution with a concentration of 0.02 mmol / mL. Then add 0.50mL of DMSO solution with a folic acid concentration of 0.02mmol / mL, and then add 16μL of 0.00125mmol / μL NaOH aqueous solution, heat in a water bath at 80°C, stir with a magnetic stirrer for 30min at a speed of 200r / min, and then mix the solution Ultrasound for 1min. Use a 1mL pipette gun to drop the mixed solution into 10mL of ultrapure water at a rate of 15μL / s, stir at a stirring rate of 300r, stir for 0.5h, then transfer the solution to a 1000D dialysis bag, and dialyze in ultrapure water for 6h , the stirring speed is 300r.

[0047] figure 2 It is a transmission electron microscope topography diagram of the folic acid-berberine self-assembled nanomedicine synthesized in Example 2, which intuitively shows a spherical shape, uniform particle size and good dispersibility. ...

Embodiment 3

[0052] Example 3 Folic acid: berberine molar ratio is 2:1 system

[0053] In a 50 mL round bottom flask, first add 0.33 mL of a DMSO solution with a berberine concentration of 0.02 mmol / mL. Then add 0.66mL of DMSO solution with a folic acid concentration of 0.02mmol / mL, and then add 21μL of 0.00125mmol / μL NaOH aqueous solution, heat in a water bath at 80°C, stir with a magnetic stirrer for 30min at a speed of 200r / min, and then ultrasonicate the mixed solution for 1min . Use a 1mL pipette gun to drop the mixed solution into 10mL of ultrapure water at a rate of 15μL / s, stir at a stirring rate of 300r, stir for 0.5h, then transfer the solution to a 1000D dialysis bag, and dialyze in ultrapure water for 6h , the stirring speed is 300r.

[0054] image 3 Left 2 is a photograph of the folic acid-berberine self-assembled nanomedicine solution synthesized in Example 3 after being placed for a week after preparation, and it can be seen intuitively that there is precipitation.

[0...

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Abstract

The invention discloses a folic acid-berberine self-assembled targeting nano-drug and a preparation method thereof. Folic acid-berberine nano-drug molecules are prepared by designing the preparation method, self-assembly of indissolvable drugs is realized, and the water-soluble targeting nano-drug is obtained. The invention provides the preparation method of the folic acid-berberine nano-drug andapplication of the nano-drug in cancer treatment. The folic acid-berberine nano-drug provided by the invention has specific antibody response, can realize targeted drug release of the drug at a tumorsite, and has the advantages of being low in cost, high in stability, free of immunogenicity, capable of reducing toxicity accumulation and drug resistance, capable of exerting a good treatment effectdue to the low drug loading capacity and capable of being selectively delivered to tumor tissues.

Description

technical field [0001] The invention belongs to drug nanotechnology, and in particular relates to a folic acid-berberine nano drug with high dispersibility, stability, controllable particle size and no need for additional carrier, its preparation method and application. Background technique [0002] Cancer is an important health problem worldwide, with an increasing mortality rate. Antibiotics, which were once effective in curing bacterial infections, are now a cause of death worldwide and may cause more morbidity than cancer due to antibiotic resistance, surveys show. While antibiotics are used to treat bacterial infections, certain bacteria can escape treatment and develop resistance to specific antibiotics, causing bacteria to multiply unaffected by the action of antibiotics and produce a wider variety of bacteria. [0003] Berberine, an isoquinoline alkaloid, can be isolated from Chinese herbal medicines such as Coptis chinensis, Cortex Phellodendron, and Perilla, and h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/22A61K31/4375A61P35/00
CPCA61K47/22A61K31/4375A61P35/00
Inventor 吉远辉吴东旭程宇
Owner SOUTHEAST UNIV
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