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GSH-responsive mesoporous silicon nanometer drug-loaded particles combined with drug molecule and valve molecule and preparation method thereof

A technology of drug molecules and nanoparticles, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., which can solve the problems of complex preparation and drug loading processes, and the safety of drug carriers needs to be improved. , to achieve good controlled release ability, good anti-immune response and biorecognition ability, and easy modification

Active Publication Date: 2021-09-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the deficiencies of the prior art, to provide a GSH-responsive mesoporous silicon nano drug-loaded particle and its preparation method in which the drug molecule and the valve molecule act in conjunction to solve the problem of existing mesoporous particles based on the GSH redox response. Silicon controlled release system uses high molecular weight polymer as the pore blocking molecule, which has the problems of complex preparation and drug loading process and the safety of drug carrier needs to be improved

Method used

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  • GSH-responsive mesoporous silicon nanometer drug-loaded particles combined with drug molecule and valve molecule and preparation method thereof
  • GSH-responsive mesoporous silicon nanometer drug-loaded particles combined with drug molecule and valve molecule and preparation method thereof
  • GSH-responsive mesoporous silicon nanometer drug-loaded particles combined with drug molecule and valve molecule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] In this example, the GSH-responsive mesoporous silicon nanometer drug-loaded particles that combine drug molecules and valve molecules, the steps are as follows:

[0063] (1) Preparation of mesoporous silicon nanoparticles

[0064] In this step, MCM-41 type mesoporous silicon nanoparticles are prepared by template method.

[0065] The surfactant cetyltrimethylammonium bromide (CTAB) was dissolved in deionized water to form a CTAB aqueous solution with a concentration of 2.08 mg / mL, and the pH value of the CTAB aqueous solution was adjusted to 11 with a 2mol / L NaOH solution. Heat to 80°C with an oil bath under stirring. After the temperature is reached, add tetraethyl silicate (TEOS) dropwise according to the volume ratio of TEOS and CTAB aqueous solution of 1:100, and react at 80°C for 2 hours under stirring conditions. Stop heating, cool to room temperature, centrifuge at a speed of 10000r / min for 10min, collect the particles, wash with deionized water and absolute et...

Embodiment 2

[0082] In this example, performance tests were performed on the products prepared in each step in Example 1.

[0083] 1. Morphological analysis

[0084] The morphology of the MCM-41 prepared by step (1) and the MCM41-S-S-NAC-Trp prepared by step (5) was observed with a high-magnification transmission electron microscope (TEM), and the results are as follows figure 2 as shown, figure 2 Among them, a and b are the TEM images of MCM-41 and MCM41-S-S-NAC-Trp respectively. Depend on figure 2 a It can be seen that MCM-41 is spherical, with smooth surface and obvious pores, good dispersion between particles, and the particle size is between 80 and 150nm. From figure 2 b It can be seen that MCM41-S-S-NAC-Trp is still spherical, with obvious mesoporous surfaces, and the particle size is also between 80 and 150nm, indicating that the main structure of mesoporous silicon has not been destroyed after modification. but in figure 2 In b, it can be clearly observed that the surfac...

Embodiment 3

[0104] In order to study the loading capacity of MCM41-S-S-NAC-Trp on MB and the plugging capacity of the plugging valve to the pores, an equal amount (5 mg) of drug controlled release carrier MCM41-S-S-NAC-Trp was mixed with different concentrations (1, 2,5mmol / L) of MB was loaded, and the loading operation was the same as step (6) of Example 1, and the determination of the maximum drug loading and encapsulation efficiency, drug loading (Drugloading content, DLC) and encapsulation efficiency (Entrapment efficiency, EE) calculation formula is as follows, and the results are shown in Table 5.

[0105]

[0106]

[0107] Table 5 Drug loading and encapsulation efficiency of MCM41-S-S-NAC-Trp loaded with different concentrations of MB

[0108]

[0109] When loaded with 1mmol / L MB, the drug loading capacity is 10.56%, and the encapsulation efficiency is 94.28%. It can be seen that the plugging valve has a good sealing ability for the pores; when the loaded 2mmol / L MB, the d...

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Abstract

The invention provides GSH-responsive mesoporous silicon nano-drug-loading particles with combined action of drug molecules and valve molecules. Positively charged and hydrophobic drug molecules containing benzene ring structure, the surface of which is grafted on the surface of mesoporous silicon nanoparticles with negatively charged and hydrophobic short peptides, the negatively charged and hydrophobic short peptides pass the glutathione-responsive function The groups are grafted on the surface of mesoporous silicon nanoparticles, and some drug molecules are located in the pores of the mesoporous silicon nanoparticles with negatively charged and hydrophobic short peptides grafted on the surface. The hydrophobic interaction and electrostatic interaction between the short peptides are combined to form a blocking valve, and the blocking valve blocks the pores of the pore structure of the mesoporous silicon nanoparticles with negatively charged and hydrophobic short peptides grafted on the surface.

Description

technical field [0001] The invention belongs to the field of drug carrier materials, and relates to a GSH-responsive mesoporous silicon nanometer drug-loaded particle in which drug molecules and valve molecules act in combination and a preparation method thereof. Background technique [0002] At present, there are many methods for treating tumors, such as surgery, chemotherapy, radiotherapy and targeted therapy, among which chemotherapy is the first choice for treating many tumors. However, chemotherapy itself has many defects. For example, most chemotherapy drugs will seriously damage normal human cells while killing cancer cells, and the drug utilization rate is low. In order to solve the above problems, researchers have developed a variety of drug controlled release systems. An ideal controlled drug release system requires that the drug be specifically delivered to the lesion site and then released to increase the bioavailability of the drug and reduce the systemic side e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K47/64A61K47/69A61K9/51A61K47/24A61K47/18A61K31/704A61K31/7048A61K31/407A61P35/00
CPCA61K9/5123A61K31/407A61K31/704A61K31/7048A61K47/54A61K47/64A61K47/6929A61P35/00
Inventor 阮丽萍梅显斌史争争杨春博
Owner SICHUAN UNIV