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A dual drug-loading system based on targeting nucleolin and its preparation method and application

A dual drug-loading and nucleolin technology is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, and medical preparations containing active ingredients. Selectivity is not high, to achieve the effect of precise targeting, high therapeutic effect, and high-efficiency targeting effect

Active Publication Date: 2020-07-10
QINGDAO UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, clinically used anti-tumor drugs usually have defects such as low selectivity, that is, while killing tumor cells, they can damage normal cells in the body, especially cells that proliferate vigorously.
These defects have become the main problems that limit the amount of anti-tumor drugs and hinder the efficacy of anti-tumor drugs.

Method used

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  • A dual drug-loading system based on targeting nucleolin and its preparation method and application
  • A dual drug-loading system based on targeting nucleolin and its preparation method and application
  • A dual drug-loading system based on targeting nucleolin and its preparation method and application

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Embodiment 1

[0052] Suspend 1.0000 g of mesoporous silica nanoparticles (MSN) in 100 mL of absolute ethanol and add excess aminopropyltriethoxysilane (APTES 1 mL). The mixture was continuously stirred at 36°C for 6 hours, filtered, washed with ethanol and dried at 60°C to afford APTES-MSN. Disperse 1.0000 g of APTES-MSN powder into 1 mL of ultrapure water to obtain a suspension. Then add PMA (0.05mL, 5μg mL -1 ) and DOX (0.05mL, 0.25mg mL -1 ) and stirred overnight at room temperature, centrifuged with ultrapure water, and dried in vacuum to obtain a white powder. Disperse 1mg of white powder in 1mL PBS (1mg mL -1 ) and mixed with AS1411 aptamer (50 μL, 10 μM), and reacted at 37° C. for 1 hour. Then, the mixture was centrifuged to obtain the AS1411 aptamer-coated MSN@PMA@DOX dual drug-loading system, which was centrifuged twice with ultrapure water and resuspended in PBS. Finally, the obtained MSN@PMA@DOX dual drug-loading system was stored at 4°C in the dark.

[0053] The MSN@PMA an...

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Abstract

Disclosed are a dual drug delivery system based on targeting nucleolin, a preparation method therefor and the use thereof. The system has a nanoparticle structure, and comprises a mesoporous silica nanoparticle, an anti-tumor drug and an AS1411 aptamer, wherein the anti-tumor drug is loaded in the mesopores of the mesoporous silica nanoparticle, and the AS1411 aptamer is encapsulated on the surface of the mesoporous silica nanoparticle. In the system, the mesoporous silica nanoparticle is used as a drug carrier, and the AS1411 aptamer can target a marker, i.e. nucleolin, of tumor cells, and in combination with a combined therapy of PMA and DOX, an MSN@PMA@DOX dual drug delivery system for tumor targeted therapy is constructed. Experimental results show that the dual drug delivery system has a high-efficiency targeting effect on nucleolin in HeLa tumor cells, and has advantages such as precise targeting and high-efficiency therapeutic effects.

Description

technical field [0001] The disclosure belongs to the technical field of biomedicine, and relates to a dual drug-loading system based on targeting nucleolin, a preparation method and an application. Background technique [0002] The statements herein merely provide background information related to the present disclosure and may not necessarily constitute prior art. [0003] Tumor refers to the new organism formed by the proliferation of local tissue cells under the action of various tumorigenic factors. According to the cell characteristics of new organisms and the degree of harm to the body, tumors are divided into two categories: benign tumors and malignant tumors. Malignant tumors can be divided into carcinoma and sarcoma. Carcinoma refers to malignant tumors derived from epithelial tissue. Sarcomas refer to malignant tumors of mesenchymal tissues, including fibrous connective tissue, fat, muscle, blood vessels, bone and cartilage tissues. Antineoplastic drugs are a cl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/52A61K47/54A61K31/704A61K31/23A61P35/00
CPCA61K31/23A61K31/704A61K47/52A61K47/549A61K47/6929A61P35/00A61K2300/00
Inventor 王宗花高晚霞张怀荣
Owner QINGDAO UNIV
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