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Galactosylated chitosan coated mesoporous silica carrier and application thereof

A technology of mesoporous silica and chitosan, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, and the digestive system, can solve problems such as unstable oral bioavailability, and achieve The effect of increasing the intake rate

Inactive Publication Date: 2020-06-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its unstable oral bioavailability and rapid metabolism by dihydropyrimidine dehydrogenase after oral administration, intravenous administration of 5-FU is commonly used clinically, but continuous intravenous injection of 5-FU will produce serious systemic adverse reactions

Method used

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  • Galactosylated chitosan coated mesoporous silica carrier and application thereof
  • Galactosylated chitosan coated mesoporous silica carrier and application thereof
  • Galactosylated chitosan coated mesoporous silica carrier and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] 1. Synthesis of MSN

[0061] Weigh 1.0g CTAB, add 480mL ultrapure water, stir gently to dissolve CTAB, adjust the oil bath temperature to 80°C, add 3.5mL 2M NaOH solution, stir for 20min, then add 5.0mLTEOS solution dropwise to the mixture, continue After two hours of reaction, stop the reaction and let it cool down, centrifuge (12000rpm, 5min), wash with ultrapure water and absolute ethanol three times, and dry in a vacuum oven at 50°C for 12h to obtain crude MSN. Add 50mL of absolute ethanol and 0.5mL of HCl (37.2%) for every 0.5g of crude MSN, the oil bath temperature is 79°C, reflux for 6h, centrifuge (12000rpm, 5min), discard the supernatant, wash with ultrapure water and absolute ethanol Three times, placed in a drying oven to dry for 12 hours, to obtain MSN without template.

[0062] 2. MSN-NH 2 Synthesis

[0063] The prepared MSNs were dried at 140 °C for 1 h. Add 1.0g of MSN to 7mL of APTES, stir, mix evenly, add to a round bottom flask filled with 50mL of ...

Embodiment 2

[0072] 1. Synthesis of MSN-COOH

[0073] Weigh 1.2g CTAB and add it to a 500mL round bottom flask containing a mixture of 180mL and 5.5mL ammonia (25%), then vigorously stir in a water bath at 60°C for 30min, then quickly add 2.0mL TEOS and 0.4mL 2- Cyanoethyltriethoxysilane, stirred for another 2h; stood still at the same temperature for 24h, and centrifuged (20000rpm, 20min). Then re-disperse twice with deionized water and ethanol respectively, and dry at 50°C. Add the product to 30mL of 9mol / L sulfuric acid after drying, and react in an oil bath at 100°C for 18h. After the reaction, centrifuge (20000rpm, 20min), and continue to treat the product with 9% hydrochloric acid ethanol solution at 65°C for 24h, and centrifuge (20000rpm, 20min), dry overnight, which is MSN-COOH.

[0074] 2. Synthesis of MSN-COOH / GC

[0075] Measure 5mL of PBS buffered saline solution with pH 7.4 into a 25mL round bottom flask, then add 5mL of GC solution (5mg / mL), and stir well. Then 30 mg of d...

Embodiment 3

[0082] Take SW620 in the logarithmic phase, trypsinize and collect, inoculate in a 12-well plate (3×104 cells / well) and incubate for 24 hours, discard the original culture medium, add fluorescein isothiocyanate (FITC), FITC@ MSN-NH 2 , FITC@MSN-NH 2 / GC culture solution, the concentration is 50μg / mL. After incubation for 4 hours, the culture medium was discarded, washed three times with PBS, and the uptake of samples by SW620 cells was analyzed with a fluorescence microscope. To assess the competitive effect of galactose on cellular uptake, set FITC@MSN-NH 2 A group of / GC+galactose, that is, in FITC@MSN-NH 2 Add galactose solution with a concentration of 2mg / ml 30min before GC application; suck out the galactose-containing medium after incubation for 30min, and add FITC@MSN-NH 2 / GC (50μg / ml) was added to the wells, and the results of fluorescence microscope analysis were compared with those of MSN-NH without galactose 2 / GC for comparative analysis.

[0083] From Fig...

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Abstract

The invention belongs to the field of medicines, and relates to a galactosylated chitosan coated mesoporous silica carrier and application thereof. On the basis of a mesoporous silica carrier, combined colon cancer targeted therapy of 5-fluorouracil (5-FU) and formyl calcium tetrahydrofolate (LV) is realized in combination with galactosylated chitosan (GC). The preparation method comprises the following steps: constructing GC-coated mesoporous silica nanoparticles (5-FU@MSN-NH2 / GC) loading 5-FU, synthesizing MSN-COOH by virtue of a two-step synthesis method, and constructing GC-coated mesoporous silica nanoparticles (LV@MSN-COOH / GC) loading LV. Research results show that the GC-coated mesoporous silica nano drug delivery system can utilize GC to be combined with a galectin receptor on thesurface of a colon cancer cell so as to increase the concentration of LV and 5-FU in tumor cells, and can remarkably reduce the expression level of thymidylate synthase (TS) in SW620 cells by combining the two medicines, so that the anti-colon cancer effect is improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, specifically, it provides a mesoporous silica carrier coated with galactosylated chitosan and its application, more specifically, it is based on a mesoporous silica carrier, combined with galactose Chitosan was used to realize the combined targeted therapy of 5-FU and LV for colon cancer. Background technique [0002] Colon cancer is a common malignant tumor of the digestive tract. In recent years, with the improvement of people's living standards, changes in eating habits and structure, and the impact of population aging, the incidence and mortality of colon cancer in my country have increased rapidly, especially in large and medium-sized cities such as Shanghai, Beijing and Guangzhou. Has become the first malignant tumor of the digestive tract. Therefore, the diagnosis and treatment of colon cancer have attracted more and more attention of researchers. The clinical treatment of colo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/04A61K47/61A61K47/52A61K31/513A61K31/519A61P35/00A61P1/00
CPCA61K47/36A61K47/02A61K47/61A61K47/52A61K31/513A61K31/519A61P35/00A61P1/00
Inventor 潘卫三刘伟田蕾陈奋叶田田朱勇超刘晓静
Owner SHENYANG PHARMA UNIVERSITY
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