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Polypeptide nano-micelle, and preparation method and application thereof

A technology of nano-micelle and nano-micelle solution, which is applied in the field of medicine and biology, can solve the problems of difficult to reach the expected value of drug bioavailability, high blood drug concentration, peptide degradation, etc., achieve strong cancer cell migration and infiltration, improve solubility, The effect of inhibiting cancer cell metastasis

Active Publication Date: 2016-03-30
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

However, most microsphere preparations have drug burst release and subsequent low release phenomenon, which will cause blood drug concentration to be too high or too low. In addition, microsphere preparations are also prone to peptide degradation during the production process
Although the use of liposomes to entrap hydrophilic or lipophilic polypeptides can improve the stability of polypeptides, the amount of polypeptides that can be entrapped in liposomes per unit mass is usually low, and the bioavailability of drugs is difficult to achieve the desired value

Method used

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  • Polypeptide nano-micelle, and preparation method and application thereof
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  • Polypeptide nano-micelle, and preparation method and application thereof

Examples

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Embodiment 1

[0069] 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

[0071] 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

[0073] 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 nano-micelle for treatment of cancers. The polypeptide in the invention can inhibit cancer metastasis; the polypeptide nano-micelle is formed by self-assembling of pegylated phosphatide (PEG-PE) and the polypeptide; and the pegylated phosphatide is a compound formed by combination of polyethylene glycol with nitrogenous bases on phosphatide molecules through covalent bonds. Specifically, the invention relates to a method for improving biostability of the polypeptide through PEG-PE micelles and provides a preparation method for the polypeptide-PEG-PE nano-micelle and application of the polypeptide-PEG-PE nano-micelle in inhibition of cancer metastasis. The nano-micelle formed by PEG-PE and the polypeptide has good stability in a salt solution, and presents the stronger characteristic of inhibiting migration and infiltration of cancer cells. The polypeptide-PEG-PE nano-micelle provided by the invention provides a feasible method and technology for cancer metastasis inhibition and cancer treatment.

Description

technical field [0001] The invention belongs to the technical field of medicine and biology, and in particular relates to a polypeptide nanomicelle with pegylated phospholipid as a carrier, 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 cure rates. [0003] Since the polypeptide is easy to de...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K38/16A61K47/34A61P35/02
CPCA61K9/1075A61K38/16A61K47/24
Inventor 王琛方小翠杨延莲段鸿洋许海燕
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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