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Preparation method of pH-sensitive drug-self-gating mesoporous nano antitumor carrier

A nano-carrier and anti-tumor technology, applied in the field of medicine, can solve the problems of non-response and inability to achieve sensitive and intelligent release of drugs, and achieve the effects of sensitive pH responsiveness, simple and efficient drug release performance, and reduction of toxic and side effects

Active Publication Date: 2017-01-04
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Second: the sensitive and intelligent release of drugs cannot be achieved for the microenvironment of the tumor site
For example, most of the acid-responsive systems developed so far can only achieve response at lower (pH 11.0) pH values, and have little response under near-physiological conditions.

Method used

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  • Preparation method of pH-sensitive drug-self-gating mesoporous nano antitumor carrier
  • Preparation method of pH-sensitive drug-self-gating mesoporous nano antitumor carrier
  • Preparation method of pH-sensitive drug-self-gating mesoporous nano antitumor carrier

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Embodiment Construction

[0026] The present invention will be further described below by embodiment.

[0027] (1) DOX molecular self-gated, mesoporous drug delivery system loaded with DOX drug molecules

[0028] Weigh 1 g of dry mesoporous silica and disperse it in 20 ml of anhydrous toluene, add 500 μL of (3-aminopropyl)triethoxysilane (APTES), reflux at 120 °C for 16 hours under an argon atmosphere, and react After completion, filter, wash twice with a mixed solution of ether and dichloromethane (1:1), and dry in vacuum to obtain silicon amide spheres on the surface. Add 20 ml water, 5ml DMF, 45 mg p-carboxybenzaldehyde, 77 mg EDC, 46 mg NHS to a 100 ml flask, adjust the pH value to 5~6 with dilute hydrochloric acid, activate the carboxyl group of p-carboxybenzaldehyde, and then add 0.85 g amide silicon spheres, reacted overnight, filtered, washed with water three times, then washed with DMF, soaked overnight, resuspended in alcohol, and dried in vacuum to obtain benzaldehyde-modified mesoporous si...

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to a preparation method of a pH-sensitive drug-self-gating mesoporous nano antitumor carrier. The preparation method includes: reacting orderedmesoporous silicon dioxide with amino-containing trimethoxy silane to obtain mesoporous silicon dioxide with the surface aminated; subjecting para-carboxyl benzaldehyde and aminated mesoporous silicon dioxide to amidation to obtain mesoporous silicon dioxide with the surface amidated; loading doxorubicin which is a wide-spectrum antitumor drug amidated mesoporous silicon dioxide in a weak acidic condition, restoring to a neutral condition to obtain the pH-sensitive DOX-self-gating mesoporous nano carrier loaded with the antitumor drug DOX, and complex assistant chemical molecules do not need to be used as gating materials, so that reducing of toxic and side effect of foreign components in the actual tumor treatment process is facilitated, and the carrier has high efficacy and drug release performance sensitive to tumor acidic microenvironment.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pH-sensitive, drug self-gated, and mesoporous nanometer anti-tumor carrier. Background technique [0002] Mesoporous silica nanoparticles (MSNs) are a new class of inorganic nanomaterials with high specific surface area, large pore volume, controllable structure size, high drug loading capacity and good biocompatibility. In recent years, the application of MSNs materials in drug delivery systems has attracted extensive research and is expected to become a new generation of drug carriers. How to control the release of drugs from mesoporous channels more reasonably, efficiently and sensitively is a hot and difficult point in current research. An effective drug intelligent controlled release system must be able to ensure that the delivered drug molecules reach the target and be released in a controlled manner. Therefore, the drug carrier is often required to achieve ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61K45/06A61K47/26A61P35/00
CPCA61K31/704A61K45/06A61K47/26A61K2300/00
Inventor 潘国庆曾小伟张文崔文国过倩萍
Owner SUZHOU UNIV
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