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A drug-loaded micelle combined with a polypeptide and a chemotherapeutic drug, its preparation method and application

A chemotherapeutic drug and drug-loaded micelle technology, applied in the field of medicine and biology, can solve the problems of low drug loading and the like

Active Publication Date: 2019-01-04
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of polymer nanomicelle carriers to deliver chemotherapy drugs is a hot spot in the research of drug delivery systems in recent years, but there is still a defect of low drug loading. Combined drug loading can make up for this defect, and at the same time exert the respective efficacy and synergistic effects of drugs

Method used

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  • A drug-loaded micelle combined with a polypeptide and a chemotherapeutic drug, its preparation method and application
  • A drug-loaded micelle combined with a polypeptide and a chemotherapeutic drug, its preparation method and application
  • A drug-loaded micelle combined with a polypeptide and a chemotherapeutic drug, its preparation method and application

Examples

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Effect test

Embodiment 1

[0112] A polypeptide nanomicelle formed by self-assembly of polyethylene glycolated phospholipid (PEG-PE) and E5 polypeptide, wherein the polyethylene glycol hydrophilic block in the polyethylene glycolated phospholipid (PEG-PE) molecule The molecular weight of the polypeptide is 2000, the molar ratio of PEGylated phospholipid (PEG-PE) and E5 polypeptide is 20:1, and the particle size of the polypeptide nanomicelle is 10-30nm.

Embodiment 2

[0114] A polypeptide nanomicelle formed by self-assembly of polyethylene glycolated phospholipid (PEG-PE) and E5 polypeptide, wherein the polyethylene glycol hydrophilic block in the polyethylene glycolated phospholipid (PEG-PE) molecule The molecular weight is 2000, the molar ratio of pegylated phospholipid (PEG-PE) and E5 polypeptide is 10:1, and the particle size of the polypeptide nanomicelle is 10-30nm.

Embodiment 3

[0116] A polypeptide nanomicelle formed by self-assembly of polyethylene glycolated phospholipid (PEG-PE) and E5 polypeptide, wherein the polyethylene glycol hydrophilic block in the polyethylene glycolated phospholipid (PEG-PE) molecule The molecular weight of the polypeptide is 2000, the molar ratio of PEGylated phospholipid (PEG-PE) and E5 polypeptide is 5:1, and the particle size of the polypeptide nanomicelle is 10-30nm.

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Abstract

The invention relates to a polypeptide and chemotherapy drug combined drug-loaded micelle and a preparation method and an application thereof. Polypeptide with a tumor targeting therapeutical effect and a chemotherapy drug are combined to prepare the tumor-targeting polypeptide-PEGylated phospholipid complex-chemotherapy drug drug-loaded micelle; the polypeptide with the tumor targeting therapeutical effect is specifically combined with a chemotactic factor receptor CXCR4, the CXCR4 polypeptide antagonist is used for increasing a targeting penetration ability of the drug to tumor tissues, the PEGylated phospholipid micelle is used for increasing the drug biological stability and the drug loading amount, and compared with a single chemotherapy drug doxorubicin, the combined drug-loaded micelle shows a stronger characteristic of inhibiting tumor cell vitality. The polypeptide and chemotherapy drug combined drug-loaded micelle provides a feasible method and technique for improving the tumor therapeutic effect.

Description

technical field [0001] The invention belongs to the field of medicine and biology, and specifically relates to a drug-loaded micelle that uses pegylated phospholipids as a carrier to carry CXCR4-targeting polypeptides and chemotherapy drugs, and its preparation method and application. Background technique [0002] Malignant cancer is currently the main cause of global morbidity and death, and about 90% of cancer patients die from cancer metastasis and recurrence. Blocking a certain link of cancer metastasis to curb the spread of cancer is very important for the treatment of cancer. Chemokines and chemokine receptors not only participate in normal physiological activities, but also participate in pathological processes such as cancer occurrence, invasion and metastasis, among which CXCR4 / SDF-1 (or CXCL12) plays an important role in the process of cancer migration and invasion. Antagonists of CXCR4 receptors are critical for controlling cancer metastasis and improving cancer c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/19A61K47/10A61K47/24A61K47/42A61K31/704A61K31/337A61P35/00A61P35/04A61P35/02
Inventor 王琛方小翠杨延莲段鸿洋许海燕李潇瑾孟洁
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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