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A miR-375 and PTX loaded four-way adapter RNA nano-drug and a preparation method and application thereof

A mir-375, nano-drug technology, applied in the field of tumor targeted therapy, can solve the problem of low drug targeted delivery efficiency, and achieve good esophageal squamous cell carcinoma inhibitory effect, effective treatment effect, and low off-target effect.

Pending Publication Date: 2021-10-15
王其龙
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

At present, albumin and liposome nano-drugs commonly used in clinical practice can only play a role through the passive targeting effect mediated by it. Although the anti-tumor effect of conventional chemotherapy drugs has been improved, there are significant non-target Organ distribution effect, drug targeted delivery efficiency is still low

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  • A miR-375 and PTX loaded four-way adapter RNA nano-drug and a preparation method and application thereof
  • A miR-375 and PTX loaded four-way adapter RNA nano-drug and a preparation method and application thereof
  • A miR-375 and PTX loaded four-way adapter RNA nano-drug and a preparation method and application thereof

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Embodiment Construction

[0026] The technical solution of the present invention will be further described below in conjunction with the examples, but it should not be understood as a limitation to the technical solution, and the adaptive improvements on this basis all belong to the protection scope of the present invention.

[0027] 1. Construction of 4WJ-miR-375-PTX:

[0028] (1) RNA oligonucleotide synthesis: synthesize oligonucleotides rG, rG, rC, rU, 2'F rC2'F rU phosphoramide monomer, 2'O-propargyl rC and rU phosphoramide monomer, and Analysis and purification by gel electrophoresis after desalting treatment by desalting column;

[0029] (2) Synthesis of PTX-azide compounds: PTX, 6-azidocaproic acid, N, N'-dicyclohexylcarbodiimide and 4-(dimethylamino)pyridine in a molar ratio of 1:2:2:1 The concentration was added to 10L of dichloromethane; the mixed solution was stirred overnight at room temperature for 16h, and the crude product was obtained by filtration and rotary evaporation; the crude pro...

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Abstract

The invention discloses a miR-375 and PTX loaded four-way adapter RNA nano-drug and a preparation method and application thereof; the nano-drug takes a four-way adapter RNA nano 4WJ as a core, is loaded with miR-375 and PTX with a remarkable esophageal squamous carcinoma cell inhibition effect, and has relatively strong esophageal squamous carcinoma targeting and permeation effects. An in-vitro cell experiment proves that the nano-drug has relatively good esophageal squamous carcinoma cell inhibition capability.

Description

technical field [0001] The invention belongs to the field of targeted tumor therapy, and relates to an RNA nano-medicine for targeted tumor therapy, in particular to a four-way linker RNA nano-drug 4WJ-miR-375-PTX loaded with miR-375 and PTX and its preparation method and application. Background technique [0002] The incidence and mortality rate of esophageal cancer in my country rank first in the world, and the treatment is still dominated by surgery and traditional radiotherapy and chemotherapy. Among them, the application of chemotherapy drugs is still one of the most important treatment methods in the treatment of advanced esophageal cancer, but the target of chemotherapy drugs is The lack of tropism and its severe side effects greatly limit its therapeutic effect. Seeking new targeted therapy strategies to improve efficacy is the focus and difficulty of current esophageal cancer research. With the development of nanotechnology, the development of nanomedicine has beco...

Claims

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Application Information

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IPC IPC(8): A61K47/26A61K48/00A61K31/7088A61K31/337A61P35/00
CPCA61K47/26A61K31/7088A61K31/337A61P35/00A61K2300/00Y02A50/30
Inventor 高勇王其龙张莉罗超李想
Owner 王其龙