Sulforaphane preparation and its preparation method and use

A technology for sulforaphane and preparations, applied in the field of medicine, can solve the problems of poor stability and short half-life in vivo of sulforaphane, and achieve the effects of overcoming the shortcomings of non-selective distribution and serious toxicity, reducing toxic effects and solving instability

Inactive Publication Date: 2014-08-20
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The present invention aims to solve the technical problems of poor stability of sulforaphane and short half-life in the body, and provides a sulforaphane preparation, which uses mesoporous silica nanoparticles as the carrier material of sulforaphane. The surface of mesoporous silica nanoparticles is coated with a lipid film. This preparation can not only significantly improve the stability of sulforaphane, but also has a good slow-release effect of sulforaphane

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  • Sulforaphane preparation and its preparation method and use
  • Sulforaphane preparation and its preparation method and use
  • Sulforaphane preparation and its preparation method and use

Examples

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preparation example Construction

[0029] The preparation method of sulforaphane preparation of the present invention comprises the following steps:

[0030] 1. Preparation of Mesoporous Silica Nanoparticles Loaded with Sulforaphane

[0031] 1) Preparation of blank mesoporous silica nanoparticles

[0032] Dissolve a certain amount of cetyltrimethylamine bromide (CTAB) in deionized water, add sodium hydroxide solution, and mix well. The mixed solution was heated to obtain a clear liquid. A certain amount of tetraethyl orthosilicate (TEOS) was injected into the above clear liquid, stirred, and a white precipitate was obtained.

[0033] The white precipitated solid is calcined in a muffle furnace to fully remove the surfactant and other organic residues in the mesopores, and ground in a mortar to disperse the particles evenly. The ratio of the materials used is:

[0034] CTAB 0.25-0.75g

[0035] Deionized water 120-360ml

[0036] NaOH 0.875-2.625ml

[0037] TEOS 1.25-3.75ml

[0038] Add the liposome suspen...

Embodiment 1

[0071] Example 1 Preparation of lipid membrane-coated mesoporous silica-loaded sulforaphane nanoparticles

[0072] 1. Preparation of Mesoporous Silica Nanoparticles Loaded with Sulforaphane

[0073] 1) Preparation of blank mesoporous silica nanoparticles

[0074] References Organic Functionalization and Morphology Control of Mesoporous Silica Materials via a Co-condensation Synthesis Method. Seong Huh, Jerzy W. Wiench, Ji-Chul Yoo, Marek Pruski and Victor S.-Y. Lin. Chem. Mater., 2003, 15(22), 4247-4256. In a 500ml round bottom flask, dissolve 0.5g cetyltrimethylamine bromide (CTAB) in 240ml deionized water, add 1.75ml 2.0mol / l sodium hydroxide aqueous solution, and mix well. The mixed solution was heated to 80°C and maintained for 30 min to obtain a clear liquid. Inject 2.5ml tetraethyl orthosilicate (TEOS) into the above clear liquid, stir at 550rpm, white precipitate can be seen after 3min, keep the reaction temperature at 80°C for 2h.

[0075] The mixed solution was co...

Embodiment 2

[0083] Example 2 Preparation of lipid membrane-coated mesoporous silica-loaded sulforaphane nanoparticles

[0084] 1. Preparation of Mesoporous Silica Nanoparticles Loaded with Sulforaphane

[0085] 1) Preparation of blank mesoporous silica nanoparticles

[0086] In a 500ml round bottom flask, dissolve 0.25g of cetyltrimethylamine bromide (CTAB) in 120ml of deionized water, add 0.875ml of 2.0mol / l sodium hydroxide aqueous solution, and mix well. The mixed solution was heated to 80°C and maintained for 30 min to obtain a clear liquid. Inject 1.25ml tetraethyl orthosilicate (TEOS) into the above clear liquid, stir at 550rpm, white precipitate can be seen after 3min, keep the reaction temperature at 80°C for 2h.

[0087] The mixed solution was cooled to room temperature, distributed into 50ml centrifuge tubes, centrifuged at 3000rpm for 20min, and the supernatant was discarded to obtain a solid product, which was washed with an appropriate amount of deionized water and ethanol,...

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Abstract

The invention discloses a sulforaphane preparation. The sulforaphane preparation comprises sulforaphane, mesoporous silica and a lipid membrane. The surface of the mesoporous silica is provided with nanoscale apertures. The nanoscale apertures are filled with sulforaphane. The surfaces of the mesoporous silica nano-particles carrying sulforaphane are coated with the lipid membrane. The invention also discloses a preparation method and a use of the sulforaphane preparation. The sulforaphane preparation has positive effects of cancer treatment, can substantially improve sulforaphane stability, has slow release and targeting dual-effects, can keep long blood circulation time and necessary plasma concentration, can recognize cancer tissue or cells, can realize intracellular administration by cell endocytosis and has a very wide application prospect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a new preparation of sulforaphane, namely lipid film-coated mesoporous silica-loaded sulforaphane nanoparticles, and a preparation method and application of the sulforaphane nano-preparation. Background technique [0002] Malignant tumors are the number one killer of human health. In recent years, the incidence of malignant tumors has been increasing year by year, and the age of onset is getting younger and younger. Medical research has always been committed to the treatment and prevention of cancer, but the mortality of cancer patients has not been effectively suppressed. At present, seeking high-efficiency and low-toxic antitumor drugs from natural plants has become one of the important directions for tumor prevention and treatment. Sulforaphane, also known as "sulforaphane", is an isothiocyanate substance extracted from cruciferous vegetables. It is the active ingredient wit...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/26A61K47/04A61P35/00
Inventor 张国庆钟延强周闺臣王新霞王东孙治国鲁莹张翮邹豪俞媛陈琰刘俊杰
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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