Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Acid-responsive mesoporous silica nano-based drug as well as preparation method and applications thereof

A technology of mesoporous silicon nanoparticles and nano-drugs, which is applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of good biocompatibility, low toxicity and side effects, and high bioavailability, and achieve simple and efficient operation. Ease of application and reduced toxic and side effects

Active Publication Date: 2019-03-15
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In the prior art, there are many studies on the environment-responsive mesoporous silicon nano-drug delivery system, but there is a lack of a drug with good biocompatibility, low toxicity and side effects, high bioavailability, acidic pH responsiveness, and treatment for vascular normalization. Mesoporous silicon nanomedicine

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Acid-responsive mesoporous silica nano-based drug as well as preparation method and applications thereof
  • Acid-responsive mesoporous silica nano-based drug as well as preparation method and applications thereof
  • Acid-responsive mesoporous silica nano-based drug as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] In this embodiment, the following method is used to verify whether the ester bond of carboxyphenylboronic acid and dopamine has acid responsiveness, the specific method is:

[0083] Dissolve 1.896 mg of dopamine in 1 mL of heavy water (10 mM), and dissolve 1.659 mg of 4-carboxyphenylboronic acid in 1 mL of heavy water (10 mM), then mix and react for 1 h. The mixed solution was divided into three parts, and the pH was adjusted to pH=5.5, pH=6.5, and pH=7.4 respectively. With the increase of pH, the solution gradually changed from milky white to colorless.

[0084] use 1 The H-NMR method was used to characterize the three mixtures respectively, and the experimental results are as follows: figure 1 As shown, in the conjugate of dopamine and 4-carboxyphenylboronic acid, the peak at 7.5ppm represents the H atom on the benzene ring of 4-carboxyphenylboronic acid, and the peak at 6.45-6.65ppm represents the H atom on the benzene ring of dopamine. H atom, when the pH decreas...

Embodiment 2

[0086] This embodiment provides an acid-responsive mesoporous silicon nano-medicine. The nano-medicine uses mesoporous silicon nanoparticles as a carrier, 4-carboxyphenylboronic acid is coupled to the mesoporous silicon nanoparticles, and the drug dopamine is coupled to the mesoporous silicon nanoparticles. On the 4-carboxyphenylboronic acid. Its preparation method is as follows:

[0087](1) Cetyltrimethylammonium bromide is dissolved in deionized water, ammoniacal liquor is added thereto, then tetraethoxysilane is added dropwise in cetyltrimethylammonium bromide aqueous solution at 25 React for 5 hours under stirring at ℃, collect the precipitate, resuspend the precipitate in ethanol and sonicate for 5 minutes, centrifuge at 12000 rpm for 10 minutes, and then collect the precipitate. This process is repeated 3 times to obtain the mesoporous silicon nanoparticles;

[0088] (2) Dissolve the mesoporous silicon nanoparticles obtained in step (1) in toluene washed with acetone or...

Embodiment 3

[0096] This embodiment provides an acid-responsive mesoporous silicon nano-medicine. The nano-medicine uses mesoporous silicon nanoparticles as a carrier, 4-carboxyphenylboronic acid is coupled to the mesoporous silicon nanoparticles, and the drug dopamine is coupled to the mesoporous silicon nanoparticles. On the 4-carboxyphenylboronic acid. Its preparation method is as follows:

[0097] (1) cetyltrimethylammonium bromide is dissolved in deionized water, ammoniacal liquor is added wherein, then tetraethoxysilane is added dropwise in cetyltrimethylammonium bromide aqueous solution at 20 The reaction was carried out under stirring at ℃ for 8 hours, the precipitate was collected, the precipitate was resuspended in ethanol and sonicated for 5 minutes, centrifuged at 12000 rpm for 10 minutes, and the precipitate was collected again. This process was repeated 5 times to obtain the mesoporous silicon nanoparticles;

[0098] (2) Dissolve the mesoporous silicon nanoparticles obtained...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention relates to an acid-responsive mesoporous silica nano-based drug as well as a preparation method and application thereof. The nano-based drug takes mesoporous silica nanoparticles as carriers, acid-responsive functional molecules are coupled on the mesoporous silica nanoparticles, a drug is coupled on the acid-responsive functional molecules, and a drug made from dopamine and used forvascular normalization is used. The acid-responsive mesoporous silica nano-based drug can stably exist during in vivo transportation, pH response can be realized when the drug reaches weakly acidic tumor sites, and the drug made from the dopamine and used for prompting the vascular normalization is released, thereby achieving the effects of reducing in vivo toxicity, improving biological safety and obviously prompting the normalization of in situ tumor vessels. Furthermore, the preparation method of the acid-responsive mesoporous silica nano-based drug is simple and easy to operate, high in stability and high in repetition rate.

Description

technical field [0001] The invention belongs to the field of nano-medicine, relates to a mesoporous silicon nano-medicine and its preparation method and application, in particular to an acid-responsive mesoporous silicon nano-medicine and its preparation method and application. Background technique [0002] In 1907, Goldman discovered that blood vessels grow around tumors, suggesting that tumor growth depends on adjacent capillaries. In 1968, some scholars proposed that tumors can produce diffuse angiogenic substances to promote the formation of new blood vessels. The system structure of tumor blood vessels is disordered, and the abnormality of this blood vessel structure leads to the disorder of blood flow, thereby changing the metabolic microenvironment of the tumor, such as acidosis and hypoxia. Abnormal tumor blood vessels and microenvironment are the main reasons for tumor chemotherapy and radiotherapy resistance. In 1971, Folkman first proposed that tumor growth and m...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/54A61K47/24A61K31/137A61P35/00
CPCA61K47/24A61K47/542A61P35/00A61K31/137
Inventor 聂广军莫海祁迎秋韩雪祥
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com