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A taurine-modified graphene oxide drug-loaded 5-fluorouracil and its preparation method and application

A technology of fluorouracil and taurine, which is applied in the field of preparation of taurine-modified graphene oxide-loaded drug-loaded 5-fluorouracil, can solve the problems of poor water solubility of 5-fluorouracil and drug application restrictions, and achieve enhanced anti-tumor efficacy, Enhanced curative effect, high drug loading effect

Active Publication Date: 2020-08-25
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, 5-fluorouracil (5-FU) itself has poor water solubility, and taking it alone has strong irritation to normal organs of the body, especially the gastrointestinal tract, which greatly limits the application of the drug

Method used

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  • A taurine-modified graphene oxide drug-loaded 5-fluorouracil and its preparation method and application
  • A taurine-modified graphene oxide drug-loaded 5-fluorouracil and its preparation method and application
  • A taurine-modified graphene oxide drug-loaded 5-fluorouracil and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] (1) The effect of ultrasonic stripping time on the Zeta potential of TCA-GO particle size

[0031] 1) Preparation of TCA-GO: Take 100ml of 1mg / ml GO aqueous solution, ultrasonically strip it at room temperature for 20min, then put it into an ice-water bath, add 200mg of NHS and 300mg of EDC, slowly add 100ml of 10mg of GO under stirring at 50rpm / ml TCA aqueous solution, stirred and reacted at 50rpm for 24h, and adjusted the pH to 6. After the reaction was completed, centrifuged at 10,000rpm for 5min, washed with pure water, centrifuged and dried to obtain the target product TCA-GO, and dissolved TCA-GO in water. Prepared into 1mg / ml aqueous solution.

[0032] 2) Take 3 parts of 1mg / ml TCA-GO solution of the same volume, ultrasonically peel them for 5min, 10min, and 20min respectively, and measure the particle size and zeta potential. The results are shown in Table 1.

[0033] Table 1 Effect of ultrasonic stripping time on the preparation of TCA-GO

[0034]

[003...

Embodiment 2

[0055] Example 2 Taurine-modified graphene oxide loaded with 5-fluorouracil

[0056] (1) Preparation method

[0057] 1. Preparation of TCA-GO: Take 100ml of 1mg / ml GO aqueous solution, ultrasonically strip it at room temperature for 20min, then put it into an ice-water bath, add 200mg of NHS and 300mg of EDC respectively, slowly add 100ml of 10mg of GO under stirring at 50rpm / ml TCA aqueous solution, stirred and reacted at 50rpm for 24h, adjusted the pH to 6, after the reaction was completed, centrifuged at 10000rpm for 5min, washed with pure water, centrifuged and dried to obtain the target product TCA-GO.

[0058] 2. Preparation of TCA-GO / 5-FU: Dissolve 25 mg of TCA-GO material in 50 ml of pure water, ultrasonically peel for 10 min, add 5 ml of 1 mg / ml 5-FU aqueous solution dropwise, and adjust the pH to 7 with 1 mol / ml NaOH solution. Shade, 50rpm, stir for 24h, centrifuge at 10000rpm for 5min, remove unloaded 5-FU, freeze-dry to form TCA-GO / 5-FU complex.

[0059] (2) Cha...

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Abstract

The invention relates to taurine modified graphene oxide loaded 5-fluorouracil (5-FU), a preparation method and application thereof. The preparation method includes: subjecting a graphene oxide solution to ultrasonic activation, then slowly adding a taurine solution dropwise, adjusting the pH, and conducting centrifugation, washing and drying to obtain TCA-GO, dissolving TCA-GO in water, performing ultrasonic peeling, adding a 5-fluorouracil aqueous solution, adjusting the PH, carrying out shading stirring reaction, then performing centrifugation to remove unloaded 5-FU, and conducting freeze-drying to obtain a TCA-GO / 5-FU compound. The carrier material provided by the invention has excellent solubility in water and strong stability, and the particle size meets the standard of a nano-drugloading system. At the same time, the system has the function of sustained or controlled release, prolongs the detention time of 5-FU in vivo, and enhances the curative effect. The taurine modified graphene oxide loaded 5-fluorouracil provided by the invention can be applied to anti-tumor study, and has very good clinical research application value.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a preparation method and application of taurine-modified graphene oxide loaded with 5-fluorouracil. Background technique [0002] Graphene oxide (GO) is a multifunctional material composed of sp3 carbon atoms with a two-dimensional planar structure. The abundant oxygen-containing groups on its surface and its unique two-dimensional structure make it amphiphilic and functionally modifiable. At the same time, the rich oxygen-rich groups on its surface make it have good water solubility and biocompatibility. However, pure GO is unstable and easily aggregated due to the change of sheet structure in saline solution and physiological solution. [0003] Taurine (TCA) was first isolated from bezoar, hence the name. It is widely distributed in animal tissue cells, especially in nerves, muscles and glands, and is the most abundant free amino acid in the body. And studies have...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/20A61K47/04A61K31/513A61P35/00
CPCA61K9/5115A61K9/5123A61K31/513A61P35/00
Inventor 刘宇韩佳婧
Owner LIAONING UNIVERSITY
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