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Acidity and lipase double-sensitive nano-container and preparation method thereof

A dual-sensitivity, nano-container technology, applied in the field of materials, can solve the problems of limiting the application of nano-containers, low sensitivity, long response time of stimulus sources, etc., and achieve the effect of improving sensitivity and application range

Inactive Publication Date: 2017-12-12
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, nanocontainers such as pH-stimuli-responsive smart nanocontainers (Wang, T., et al. (2014). Chemical Communications, 50(83), 12469-12472.) and enzyme-stimuli-responsive smart nanocontainers are single Heavy response, long response time to stimuli, cumbersome and complicated process, low sensitivity, and limited application range limit the application of nanocontainers in the biomedical field

Method used

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  • Acidity and lipase double-sensitive nano-container and preparation method thereof
  • Acidity and lipase double-sensitive nano-container and preparation method thereof
  • Acidity and lipase double-sensitive nano-container and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0028] The preparation method of acid and lipase double sensitive nano container, the steps are as follows:

[0029] 1. Preparation of Mesoporous Silica Microspheres MCM-41

[0030] Cetyltrimethylammonium bromide (CTAB, 0.5g), NaOH solution (2mol / L, 1.75mL) and H 2 O (240 mL) was mixed and stirred at 80 °C for 30 min. Ethyl orthosilicate (TEOS, 2.5 mL) was added dropwise, and a white precipitate was formed after thorough stirring for 10 min. Stir at 80°C for 2h, filter while hot, wash the product thoroughly with water and methanol, and dry it in vacuum at 90°C.

[0031] Weigh 0.3g of dry solid, ultrasonically disperse in a mixed solution of isopropanol (60mL) and concentrated hydrochloric acid (3mL), heat to reflux for 6h, centrifuge, wash thoroughly with water and methanol, and dry under vacuum at 90°C to obtain mesoporous silica Microspheres (MCM-41).

[0032] 2. Surface modification of mesoporous silica

[0033] The dried MCM-41 (200mg) was ultrasonically dispersed in ...

Embodiment 2

[0046] The preparation method of acid and lipase double sensitive nano container, the steps are as follows:

[0047] 1. Preparation of Mesoporous Silica Microspheres MCM-41

[0048] Cetyltrimethylammonium bromide (CTAB, 0.5g), NaOH solution (2mol / L, 1.75mL) and H 2 O (240 mL) was mixed and stirred at 80 °C for 30 min. Ethyl orthosilicate (TEOS, 2.5 mL) was added dropwise, and a white precipitate was formed after thorough stirring for 10 min. Stir at 80°C for 2h, filter while hot, wash the product thoroughly with water and methanol, and dry it in vacuum at 90°C.

[0049] Weigh 0.3g of dry solid, ultrasonically disperse in a mixed solution of isopropanol (60mL) and concentrated hydrochloric acid (3mL), heat to reflux for 6h, centrifuge, wash thoroughly with water and methanol, and dry under vacuum at 90°C to obtain mesoporous silica Microspheres (MCM-41).

[0050] 2. Surface modification of mesoporous silica

[0051] The dried MCM-41 (200mg) was ultrasonically dispersed in ...

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Abstract

The invention discloses an acidity and lipase double-sensitive nano-container and a preparation method thereof. The double-sensitive nano-container is prepared by connecting a mesoporous silica microsphere to a benzimidazole-modified cyclodextrin molecule through an ester chain, and storing rhodamine or gemcitabine in the mesoporous silica microsphere through adsorption. The method comprises the following steps: executing the modification of an organic functional group on the surface of the mesoporous silica microsphere and the cyclodextrin, and finally connecting the modified macrocyclic molecular cyclodextrin to the silica microsphere through a carbon chain containing an ester bond. The ester bond of the nano-container is broken by the hydrolysis under the environment of over-expression of the lipase, the cyclodextrin is stripped, and drug molecules are released. Under the acidic condition, the inclusion and release of a guest by a host can be realized by the pH regulation of an imidazole group, and the molecule adsorbing-releasing of the nano-container is realized. The nano-container can be applied for the targeted therapy in the chemotherapy, and the purposes of specific killing effect, curative effect improvement and toxicity reduction can be realized.

Description

technical field [0001] The invention belongs to the technical field of materials, and relates to an acid and lipase double-sensitive nano container and a preparation method thereof. Background technique [0002] With the change of human work and lifestyle, environmental deterioration and food safety problems have emerged, and the number of people suffering from cancer worldwide has exceeded 14 million. The current methods of treating cancer mainly include surgery, radiotherapy, biological therapy, chemotherapy and so on. Each method has its own advantages and disadvantages, and clinical treatment is generally coordinated with each other. Wherein surgical operation method can recover from illness theoretically, but it is extremely traumatic to human body. Radiation therapy is the use of radiation to kill cancer cells and shrink tumors, but radiation can also damage normal cells, reducing the number and activity of human lymphocytes. Biological therapy has relatively few si...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K47/04A61K31/7068A61K31/352A61P35/00
CPCA61K47/40A61K9/0002A61K31/352A61K31/7068A61K47/02
Inventor 孙艳辉魏萌萌王婷傅佳骏
Owner NANJING UNIV OF SCI & TECH
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