Injectable holothurin mesoporous silica nano-composite as well as preparation method and application thereof

A technology of mesoporous silica and nanocomposites, which can be used in medical preparations of non-active ingredients, drug combinations, drug delivery, etc., and can solve problems such as limiting the clinical application of sea cucumber saponins and red blood cell perforation

Pending Publication Date: 2021-04-27
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, after oral administration, sea cucumber saponins are easily degraded by enzymes in the digestive system, and sea cucumber saponins can combine with sterol molecules on the biofilm to form molecular complexes, thereby producing ion channels and large water-based channels, causing red blood cells to perforate and cause hemolysis
The severe hemolysis of sea cucumber saponins makes it difficult to administer intravenously, which limits the clinical application of sea cucumber saponins

Method used

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  • Injectable holothurin mesoporous silica nano-composite as well as preparation method and application thereof
  • Injectable holothurin mesoporous silica nano-composite as well as preparation method and application thereof
  • Injectable holothurin mesoporous silica nano-composite as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] A preparation method for injectable sea cucumber saponin mesoporous silicon dioxide nanocomposite, comprising the following steps:

[0039] (1) Preparation of mesoporous silica nanoparticles: Weigh 6g of cetyltrimethylammonium chloride (CTAC) and 0.1g of triethanolamine (TEA) into 60mL of deionized water, heat and stir at 60°C 2h, add 20mL of 3% tetraethylorthosilicate (TEOS) cyclohexane solution, heat and stir at 40°C for 8h, centrifuge to collect the reaction product, wash with ethanol three times, and disperse the reaction product in 100mL of 1% ammonium chloride solution, Heat and stir at 40°C for 8 hours to remove the template agent, repeat the operation twice, collect the reaction product by centrifugation, wash three times with ethanol and deionized water, and freeze-dry to obtain mesoporous silica nanoparticles.

[0040] (2) Preparation of sea cucumber saponin-encapsulated mesoporous silica nanoparticles: Weigh 10 mg of mesoporous silica nanoparticles, add it to...

Embodiment 2

[0043] A preparation method for injectable sea cucumber saponin mesoporous silicon dioxide nanocomposite, comprising the following steps:

[0044] (1) Preparation of mesoporous silica nanoparticles: Weigh 6g of cetyltrimethylammonium chloride (CTAC) and 0.2g of triethanolamine (TEA) into 60mL of deionized water, heat and stir at 70°C 2h, add 25mL of 4% tetraethylorthosilicate (TEOS) in cyclohexane, heat and stir at 70°C for 12h, collect the reaction product by centrifugation, wash with ethanol three times, and disperse the reaction product in 100mL of 1% ammonium chloride solution. Heat and stir at 70°C for 8 hours to remove the template agent, repeat the operation twice, collect the reaction product by centrifugation, wash three times with ethanol and deionized water, and freeze-dry to obtain mesoporous silica nanoparticles.

[0045] (2) Preparation of sea cucumber saponin-encapsulated mesoporous silica nanoparticles: Weigh 20 mg of mesoporous silica nanoparticles, add it to ...

Embodiment 3

[0048] A preparation method for injectable sea cucumber saponin mesoporous silicon dioxide nanocomposite, comprising the following steps:

[0049] (1) Preparation of mesoporous silica nanoparticles: Weigh 6g of cetyltrimethylammonium chloride (CTAC) and 0.5g of triethanolamine (TEA) into 60mL of deionized water, heat and stir at 80°C 2h, add 30mL of 4% tetraethylorthosilicate (TEOS) cyclohexane solution, heat and stir at 80°C for 16h, collect the reaction product by centrifugation, wash with ethanol three times, and disperse the reaction product in 100mL of 1% ammonium chloride solution, Heat and stir at 80°C for 16 hours to remove the template agent, repeat the operation twice, collect the reaction product by centrifugation, wash three times with ethanol and deionized water, and freeze-dry to obtain mesoporous silica nanoparticles.

[0050] (2) Preparation of sea cucumber saponin-encapsulated mesoporous silica nanoparticles: Weigh 24 mg of mesoporous silica nanoparticles, add...

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Abstract

The invention discloses an injectable holothurin mesoporous silica nano-composite as well as a preparation method and application thereof. The holothurin mesoporous silica nano-composite comprises mesoporous silica nanoparticles, holothurin entrapped in the mesoporous silica nanoparticles and chitosan for modifying the surfaces of the mesoporous silica nanoparticles. Specifically, macroporous mesoporous silica nanoparticles are synthesized firstly, the holothurin is entrapped in mesopores of mesoporous silica, then the chitosan is used for modifying the surface of the mesoporous silica, and the injectable chitosan modified holothurin mesoporous silica nano-composite is constructed. The holothurin mesoporous silica nano-composite prepared by the preparation method provided by the invention has the particle size of about 100 nm, the encapsulation rate of 60% or above and the hemolysis rate of less than 5%, meets clinical requirements on hemolysis of drugs, and is expected to be developed into antitumor drugs or antitumor auxiliary drugs for in-vivo injection administration.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a preparation method and application of an injectable sea cucumber saponin mesoporous silica nanocomposite. Background technique [0002] Sea cucumber saponins are important secondary metabolites in sea cucumbers. They have various pharmacological activities such as antitumor, antifungal, and hemolytic, and have low toxic and side effects. However, after oral administration, sea cucumber saponins are easily degraded by enzymes in the digestive system, and sea cucumber saponins can combine with sterol molecules on biofilms to form molecular complexes, thereby producing ion channels and large water-based channels, causing red blood cells to perforate and cause hemolysis. The severe hemolysis of sea cucumber saponins makes it difficult to administer intravenously, which limits the clinical application of sea cucumber saponins. Therefore, reducing the hemolytic toxicity of sea...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K35/616A61K47/61A61K9/00A61P31/04A61P35/00
CPCA61K35/616A61K47/6949A61K47/61A61K9/0019A61P35/00A61P31/04
Inventor 李红燕解万翠杨锡洪董秀芳宋琳车红霞
Owner QINGDAO UNIV OF SCI & TECH
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