Drug containing arsenic nanoparticles and preparation method thereof

A nanoparticle and drug technology, applied in the field of biomedicine, can solve the problems of not being able to achieve a good therapeutic effect, difficult to degrade and excrete, poor biocompatibility, etc., to achieve clinical transformation potential, and the reaction raw materials are cheap and easy to obtain , the effect of little environmental pollution

Inactive Publication Date: 2020-03-06
THE FIFTH AFFILIATED HOSPITAL SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the incomplete release of insoluble arsenic compounds, compared with free ATO, entrapped ATO exhibited weaker cytotoxicity and could not achieve a good therapeutic effect.
At the s

Method used

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  • Drug containing arsenic nanoparticles and preparation method thereof
  • Drug containing arsenic nanoparticles and preparation method thereof
  • Drug containing arsenic nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Synthesis of FeAs / HSA

[0042] Dissolve 10 mg of human serum albumin in 20 mL of PBS solution at pH = 3, stir at 37°C and add 40 μL (0.1M) of anhydrous ferric chloride (0.1M) and 40 μL (0.1M) of sodium arsenite dropwise at the same time, add dropwise after 1 hour Ammonia and hydrochloric acid (0.1M) adjust the reaction pH to 5.5-7.4. Continue to react under these conditions for 8 hours and then end the reaction. Centrifuge for 10 minutes to remove the supernatant at a speed of 10,000 r / min. Resuspend the precipitate in pure water and use a 50KD ultrafiltration centrifuge tube to remove unreacted ions and HSA. After washing three times in this way, freeze-dry to obtain FeAs / HSA.

Embodiment 2

[0044] Synthesis of MnAs / HSA

[0045] 10 mg of human serum albumin was dissolved in 20 mL of pure water, 80 μL (0.1 M) of manganese acetate and 40 μL (0.1 M) of sodium arsenite were added dropwise thereto, and the reaction was stirred at 37° C. for 1 hour. After 1 hour, ammonia water or NaOH (1M) was added dropwise to the reaction system to adjust the pH of the reaction solution to 8.0-9.5. After continuing to stir and react at 37°C for 8 hours, centrifuge for 12 minutes to remove the supernatant at a speed of 12000r / min, resuspend the precipitate with pure water and use a 50KD ultrafiltration centrifuge tube to remove unreacted ions and HSA by ultrafiltration. After washing three times in this way, freeze-dry to obtain MnAs / HSA.

Embodiment 3

[0047] Synthesis of NiAs / HSA

[0048] 10 mg of human serum albumin was dissolved in 20 mL of pure water, 80 μL (0.1 M) of nickel acetate and 40 μL (0.1 M) of sodium arsenite were added dropwise thereto, and the reaction was stirred at 37° C. for 1 hour. After 1 hour, aqueous ammonia or NaOH (1M) was added dropwise to the reaction system to adjust the pH of the reaction solution to 7.5-9.5. After continuing to stir and react at 37°C for 8 hours, centrifuge for 10 minutes to remove the supernatant at a speed of 10,000r / min, resuspend the precipitate with pure water and use a 50KD ultrafiltration centrifuge tube to remove unreacted ions and HSA. After washing three times in this way, freeze-dry to obtain NiAs / HSA.

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Abstract

The invention belongs to the field of biological medicines, and discloses a drug containing arsenic nanoparticles, which comprises transition metal, arsenic and protein, and the protein is a carrier and is loaded with the transition metal and the arsenic. According to the synthesized drug containing arsenic nanoparticles, single protein serves as a template, the particle size of the synthesized drug is smaller than 15 nm, the in-vivo circulation time can be prolonged due to the small particle size, and uptake of tumor to the drug is increased. The drug containing the arsenic nanoparticles hasan acid-responsive release characteristic, and can release the drug for a tumor microenvironment and tumor cells in a targeting manner, so that the side effect caused by non-specific release of the drug is reduced, the local drug concentration of the tumor can be improved, and the tumor killing effect is enhanced. Meanwhile, the drug containing the arsenic nanoparticles is simple in synthesis mode, mild in reaction condition, cheap and easily available in reaction raw materials, low in purification cost and small in environmental pollution, does not need to use an organic solvent, has clinicalconversion potential, and can be produced in a large-scale expanded manner.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a drug containing arsenic nano particles and a preparation method thereof. Background technique [0002] Arsenic is a common naturally occurring substance that exists in both organic and inorganic forms. There are three inorganic forms of arsenic: red arsenic (As 4 S 4 , also known as realgar), yellow arsenic (As 2 S 3 ) and arsenic (As 2 o 3 ). Arsenic is a well-known poison and the oldest therapeutic drug used in Chinese and Western medicine. [0003] Arsenic trioxide (ATO, As 2 o 3 ) is a first-line antitumor drug for the treatment of acute promyelocytic leukemia (APL), and the complete remission rate of clinical treatment is 83-95%. ATO can affect many intracellular signal transduction pathways, alter cell function, lead to apoptosis, inhibit angiogenesis, and promote cell differentiation. Therefore, along with the success of ATO in the treatment of APL, the application ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/42A61K47/02A61K33/36A61P35/00A61P35/02
CPCA61K9/5115A61K9/5169A61K33/36A61P35/00A61P35/02
Inventor 张可李丹单鸿
Owner THE FIFTH AFFILIATED HOSPITAL SUN YAT SEN UNIV
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