An acid-responsive mesoporous silicon nanomedicine and its preparation method and application

A technology of mesoporous silicon nanoparticles and nano-drugs, which can be used in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of good biocompatibility, high bioavailability, low toxicity and side effects, and achieve good stability. , reduce toxic side effects, high repetition rate

Active Publication Date: 2022-02-11
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • 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

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  • An acid-responsive mesoporous silicon nanomedicine and its preparation method and application
  • An acid-responsive mesoporous silicon nanomedicine and its preparation method and application
  • An acid-responsive mesoporous silicon nanomedicine and its preparation method and application

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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...

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Abstract

The invention relates to an acid-responsive mesoporous silicon nano-medicine and its preparation method and application. The nano-medicine uses mesoporous silicon nanoparticles as a carrier, and acid-responsive functional molecules are coupled to the mesoporous silicon nanoparticles. Coupling on the acid-responsive functional molecule; the drug is the blood vessel normalizing drug dopamine. The acid-responsive mesoporous silicon nanomedicine of the present invention can exist stably during in vivo transportation, and can realize pH response when it reaches the weakly acidic tumor site, thereby releasing the drug dopamine that promotes the normalization of blood vessels, thereby reducing the toxicity in vivo, The biological safety is improved, and the effect of significantly promoting the normalization of tumor blood vessels in situ, and the preparation method of the acid-responsive mesoporous silicon nano-medicine is simple and easy to operate, with good stability and high 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

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Application Information

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Patent Type & Authority Patents(China)
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
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