A kind of preparation method and application of pentafluorouracil nano drug preparation

A technology of pentafluorouracil and nano-drug, applied in the directions of drug combination, pharmaceutical formulation, anti-tumor drug, etc., can solve the problems of poor tumor cell selectivity, unfavorable cell endocytosis, strong toxic and side effects, etc., to improve bioavailability and effective Dosage, the effect of improving stability

Active Publication Date: 2021-08-03
HUNAN UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

5Fu is generally administered by injection, but this method of administration has poor selectivity to tumor cells, strong toxic and side effects, fast metabolism, and short half-life
However, the above-mentioned studies are mainly for the slow release of drugs, and have not been coordinated with the means of tumor treatment; moreover, the sustained-release microspheres finally prepared in the above-mentioned studies are relatively large in size, which is not conducive to endocytosis, and is generally released in the In the body fluid, the cells achieve the therapeutic effect by absorbing the body fluid

Method used

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  • A kind of preparation method and application of pentafluorouracil nano drug preparation
  • A kind of preparation method and application of pentafluorouracil nano drug preparation
  • A kind of preparation method and application of pentafluorouracil nano drug preparation

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Experimental program
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Embodiment 1

[0022] 1. Synthesis of Mn-pentafluorouracil nanoparticles (Mn-5Fu nanoparticles)

[0023] 0.2g (1mmol) of MnCl 2 4H 2 O and 0.13g (1mmol) of 5-Fu were placed in 25mL of DMF solvent, and the solution was ultrasonicated until the solution was clear; then, 0.25mL triethylamine was added to the above solution, and ultrasonication was continued for 1h; after the ultrasonication was completed, the entire solution was placed at 100°C Heat in an oven for 1 hour, then continue ultrasonication for 20 minutes, then filter, wash the filter cake three times with DMF and water respectively, finally obtain Mn-5Fu, disperse it in water, and store it at room temperature.

[0024] 2. Preparation of pentafluorouracil nanomedicine preparations (Mn-5Fu@PDA@PEG)

[0025] Take 8 mL of Mn-5Fu dispersed in Tris buffer (the concentration of Mn-5Fu is 10 mM, the pH of Tris buffer is 8.5), add 0.2 mL of freshly prepared dopamine aqueous solution (2 mg / mL), and stir at room temperature for 1 h, the solu...

Embodiment 2

[0028] Embodiment 2Mn-5Fu drug release

[0029]Disperse the 10mM (according to 5Fu calculation) aqueous solution of Mn-5Fu nanoparticles into the PBS buffer solution of pH 5.5or 7.4, after a period of time (0, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6 , 8, 10 and 12h) Take out 0.2mL of the solution and centrifuge to leave the supernatant. The supernatant was used to measure the concentration of pentafluorouracil quantitatively by ultraviolet absorption spectrometry, and to measure the concentration of manganese ions by inductively coupled plasma mass spectrometry (ICP-MS). Calculate the amount of drug and manganese ion released at different times. The result is as image 3 As shown, in the environment of pH 7.4, the amount of manganese ions or drugs released by Mn-5Fu does not exceed 10%; while in the environment of pH 5.5, the release of manganese ions and drugs is about 86% and 81%; it shows that Mn-5Fu Manganese ions and drugs can be released under acidic conditions, indicating ...

Embodiment 3

[0030] Example 3 Cytotoxicity Test

[0031] Mouse breast cancer cells (4T1) were inoculated into a 96-well plate, cultured in a cell incubator for 24 hours, and then washed twice with DPBS. Cells were incubated with different concentrations of Mn-5Fu (concentrations were calculated based on 5Fu, respectively 1, 10, 50, 100, and 200uM) for 24h or 48h, discard the cell culture medium, add fresh medium and MTS staining After incubating for 30 min in a cell culture incubator, measure the UV absorbance of each well of cells at 490 nm with a microplate reader. Calculate cell viability. Take the 5Fu solution according to the above concentration as a control.

[0032] The result is as Figure 4 As shown, the survival rate of cells incubated with 5Fu was higher than that of cells treated with Mn-5Fu, especially at concentrations of 50, 100, and 200uM, the survival rate of cells incubated with 5Fu was higher than that of cells treated with Mn-5Fu double the cell viability. This sho...

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Abstract

The invention discloses a preparation method and application of a pentafluorouracil nano-pharmaceutical preparation, which comprises the following steps: dissolving metal salt and 5Fu in a solvent, adding triethylamine after complete dissolution, and performing ultrasonic reaction; The liquid is placed in an oven and heated in a sealed manner. After the heating is completed, ultrasonic treatment is performed. After the ultrasonic treatment, centrifugation is performed; the precipitate is repeatedly resuspended and washed by centrifugation to obtain X‑5Fu; X‑5Fu is dispersed in the buffer solution, and then X‑5Fu is Add a dopamine aqueous solution to the 5Fu dispersion, react, and then centrifuge, resuspend the precipitate repeatedly, centrifuge and wash, disperse in water, adjust the pH of the aqueous solution to alkaline, and then add NH 2 -PEG 5000 , After the time set by ultrasound, the reaction is stirred for the second time at room temperature. After the reaction, centrifuge, and the precipitate is repeatedly resuspended and washed by centrifugation to obtain the pentafluorouracil nano-pharmaceutical preparation. The nano drug preparation of the present invention is beneficial to cell endocytosis and tumor accumulation, and can realize pH-responsive release of drugs.

Description

technical field [0001] The invention belongs to the technical field of nanomaterials and medicines, and in particular relates to a preparation method and application of a pentafluorouracil nanomedicine preparation. Background technique [0002] Malignant tumors are diseases that seriously threaten human health and life, and cancer patients continue to increase worldwide. Conquering cancer is the common goal of all mankind. At present, the clinically applied anti-tumor treatment methods mainly include surgery, radiotherapy, chemotherapy, and immunotherapy, and these treatment methods generally require compatible drug treatment. At present, there are many kinds of drugs for cancer treatment, such as paclitaxel, cisplatin, and pentafluorouracil. These drugs not only have strong effects on cancer cells, but also have strong side effects on the body. Therefore, the drugs are coated or combined with specific targets. Combining with substances to prepare sustained-release prepara...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/10A61K47/34A61K49/12A61K31/513A61P35/00
CPCA61K9/5146A61K31/513A61K49/126A61P35/00
Inventor 张晓兵杨婵宋国胜宦双燕
Owner HUNAN UNIV
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