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Preparation method of magnetic nanometer drug-loading sustained-release microspheres encapsulating 5-fluorouracil

A fluorouracil, magnetic nanotechnology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., to achieve the effects of high drug loading, promoting growth and metabolism, and increasing stability

Inactive Publication Date: 2018-04-10
THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Polylactic acid (PLA) is widely used as a drug carrier due to its good biocompatibility and biodegradability, and it can also improve the biological activity of the overall biological sustained-release material. 3 o 4 As a carrier, there are few reports, while PLA / Fe 3 o 4 As a 5-Fu carrier and made into composite microspheres, it has not been reported at home and abroad

Method used

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  • Preparation method of magnetic nanometer drug-loading sustained-release microspheres encapsulating 5-fluorouracil
  • Preparation method of magnetic nanometer drug-loading sustained-release microspheres encapsulating 5-fluorouracil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Step 1: Take 100g of magnetic nano-particle ferric oxide and 10g of 5-fluorouracil and add it to the sodium hydroxide solution, first perform ultrasonic mixing at 60kHz, then magnetically stir at 500rpm for 36h, and freeze-dry to obtain a black freeze-dried powder ;

[0033] Step 2, get 0.2g chitosan and dissolve in 2ml methylene chloride containing 10% g / mL polylactic acid to obtain an organic solution of chitosan and polylactic acid;

[0034] Step 3, add the black freeze-dried powder obtained in step 1 to the organic solution of chitosan and polylactic acid obtained in step 2, stir at 5000 rpm for 5 minutes, and ultrasonically mix and disperse at 70 kHz to obtain the first mixed emulsion ;

[0035] Step 4, adding the first mixed emulsion obtained in step 3 to a deionized aqueous solution containing 0.1 g / ml methylcellulose to obtain a second mixed emulsion; wherein, the first mixed emulsion and the deionized aqueous solution of methylcellulose The volume ratio is 1:...

Embodiment 2

[0038] Step 1: Add 10g of magnetic nano-particle ferric oxide and 10g of 5-fluorouracil into the sodium hydroxide solution, first perform ultrasonic mixing at 40kHz, then magnetically stir at 200rpm for 12h, and freeze-dry to obtain a black freeze-dried powder ;

[0039] Step 2, get 0.2g chitosan and dissolve in 2ml methylene chloride containing 1% g / mL polylactic acid to obtain an organic solution of chitosan and polylactic acid;

[0040] Step 3, add the black freeze-dried powder obtained in step 1 to the organic solution of chitosan and polylactic acid obtained in step 2, stir at 1000 rpm for 1 min, and ultrasonically mix and disperse at 40 kHz to obtain the first mixed emulsion ;

[0041] Step 4, adding the first mixed emulsion obtained in step 3 into a deionized aqueous solution containing 2% g / ml methylcellulose to obtain a second mixed emulsion; wherein, the first mixed emulsion and the deionized aqueous solution of methylcellulose The volume ratio is 1:10.

[0042] S...

Embodiment 3

[0044] Step 1: Take 500g of magnetic nanoparticles ferric oxide and 10g of 5-fluorouracil into the sodium hydroxide solution, perform ultrasonic mixing at 100kHz, then magnetically stir at 1000rpm for 48 hours, freeze-dry to obtain black freeze-dried powder ;

[0045] Step 2, get 0.2g chitosan and dissolve in 2ml methylene chloride containing 20% ​​g / mL polylactic acid to obtain an organic solution of chitosan and polylactic acid;

[0046] Step 3: Add the black freeze-dried powder obtained in step 1 to the organic solution of chitosan and polylactic acid obtained in step 2, stir at 10,000 rpm for 10 minutes, and ultrasonically mix and disperse at 4,100 kHz to obtain the first mixed emulsion ;

[0047] Step 4, adding the first mixed emulsion obtained in step 3 into a deionized aqueous solution containing 4% g / ml methylcellulose to obtain a second mixed emulsion; wherein, the first mixed emulsion and the deionized aqueous solution of methylcellulose The volume ratio is 1:1000....

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Abstract

The invention discloses a preparation method of magnetic nanometer drug-loading sustained-release microspheres encapsulating 5-fluorouracil. The specific steps comprises: 1) adding the mixture of magnetic nanoparticles ferroferric oxide and 5-fluorouracil into an alkaline solution, carrying out ultrasound and stirring, and carrying out freeze drying to obtain black freeze drying powder; 2) dissolving chitosan in an organic solvent containing polylactic acid to obtain an organic mixed solution; 3) adding the black freeze drying powder to the organic mixed solution, and carrying out ultrasound and stirring to obtain a first mixed emulsion; 4) adding the first mixed emulsion to a deionized water solution containing methyl cellulose to obtain a second mixed emulsion; and 5) stirring the secondmixed emulsion, centrifuging, and washing to obtain the target product. According to the present invention, the defect of the short sustained release time of the 5-fluorouracil preparation is overcome by using the high magnetic adsorption performance and the chemical bond effect of the magnetic nanoparticles ferroferric oxide on the 5-fluorouracil, and the obtained product can effectively treat large-area bone defect diseases caused by bone tumors.

Description

technical field [0001] The invention belongs to the technical field of preparing drug sustained-release nano-microspheres, and in particular relates to a preparation method of magnetic nanometer drug-loaded sustained-release microspheres wrapped with 5-fluorouracil. Background technique [0002] 5-Fluorouracil (5-Fu) can inhibit thymidine nucleotide synthase, block the conversion of deoxypyrimidine nucleotide into thymidine nucleus, interfere with DNA synthesis, and play an anti-cancer role; and it can also be mixed with pseudo metabolites into RNA to inhibit the proliferation of tumor cells. It is the most commonly used anticancer drug in clinical practice for more than 30 years. Cancer, liver cancer, bladder cancer, etc. have good curative effect, even so far, it is still one of the most effective anti-tumor drugs that cannot be replaced. Generally, it is administered by intravenous injection or infusion, but the selectivity to tumor cells is poor, the toxic and side eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/513A61K47/36A61K47/34A61K47/02A61P35/00
CPCA61K9/5115A61K9/5146A61K9/5161A61K31/513
Inventor 黄江鸿王大平熊建义刘威陈洁琳段莉朱伟民尤微朱飞燕贾兆锋
Owner THE SECOND PEOPLES HOSPITAL OF SHENZHEN