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Self-assembled spherical drug nano-preparation and its preparation method and application

A nano-preparation and drug technology, which is applied in the field of self-assembled spherical drug nano-preparation and its preparation, can solve the problems of poor stability and short half-life, and achieve the effect of mild preparation process conditions, simple and easy process, and cheap and easy-to-obtain raw materials

Active Publication Date: 2021-06-29
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As the main components of tissue cells, liposomes and other molecules have good biocompatibility and wide drug-loading adaptability, but their stability is poor, and they are easily phagocytized and eliminated by the reticuloendothelial system when they enter the body. short

Method used

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  • Self-assembled spherical drug nano-preparation and its preparation method and application
  • Self-assembled spherical drug nano-preparation and its preparation method and application
  • Self-assembled spherical drug nano-preparation and its preparation method and application

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preparation example Construction

[0044] The present invention also provides a preparation method of a spherical drug nano-preparation, comprising the steps of:

[0045] S1: Mix hydrophobic molecules and cross-linking agents, stir and react at room temperature for 4-8 hours, then dialyze and freeze-dry. The hydrophobic molecules are oil-soluble molecules such as glycerides or phospholipid molecules, and the molecular moles of hydrophobic molecules and cross-linking agents The ratio is 1:(1~10), the glyceride is 1,3-dilinolenic acid glyceride and other molecules, the phospholipid molecule is 1,2-dioleoyl-SN-glycero-3-phosphoethanolamine and other molecules; cross-linking agent N-hydroxysuccinimide 3-(2-pyridyldimercapto) propionate or sodium azide; dialysis bags are used for dialysis, and substances with a molecular weight greater than 500KD are collected after dialysis;

[0046] S2: Carry out group modification on the hydrophilic drug molecule, stir and react at room temperature for 4-8 hours, then dialyze and...

Embodiment 1

[0051] This embodiment provides a self-assembled spherical pharmaceutical nano-preparation, the monomer molecule of which is formula (I):

[0052]

[0053] R1 and R2 in the formula (I) are any fatty chain, and the hydrophilic drug is any hydrophilic drug molecule.

Embodiment 2

[0055] This embodiment provides a self-assembled spherical pharmaceutical nano-preparation, the monomer molecule of which is formula (II):

[0056]

[0057] R1 and R2 in the formula (II) are any fatty chain, and the hydrophilic drug is any hydrophilic drug molecule.

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Abstract

The invention relates to a self-assembled spherical pharmaceutical nano-preparation and its preparation method and application. It is a nano-preparation prepared by self-assembly using amphiphilic monomer molecules as base units; the amphiphilic monomer molecules are composed of hydrophobic Sexual molecules and hydrophilic drug molecules. The nano-preparation can reduce the degradation rate of the drug itself, increase the utilization rate of the drug, and realize the controlled release of the drug; the molecules of the hydrophobic layer and the hydrophilic layer can be loaded with drugs or other functional components with different characteristics, and can be used as a carrier for drugs or vaccines, genes and Molecular probes and other fields; monomer molecules connected by disulfide bonds, after entering the cells, will undergo a bond-breaking reaction due to the glutathione that exists in large quantities in the cells, and realize the rapid responsive release of drugs to play a role, and nanoparticles can It ensures that the functional components such as the drugs contained in them can function in a free form; the preparation conditions of the system are mild, which can ensure the integrity and functional effectiveness of the drugs, genes or molecular probes contained in the nanoparticles.

Description

technical field [0001] The invention relates to drug delivery, drug carrier, gene carrier, vaccine adjuvant, molecular probe and other biotechnology fields, in particular to a self-assembled spherical drug nano-preparation and its preparation method and application. Background technique [0002] Traditional drug molecules are easily degraded and removed after entering the body. By imitating the structure and function of biological systems, the biomimetic nano-delivery system can effectively reduce the immunogenicity and side effects of traditional nanoparticles and improve the utilization of drugs, making it an ideal candidate for delivery. system. As the main components of tissue cells, liposomes and other molecules have good biocompatibility and wide drug-loading adaptability, but their stability is poor, and they are easily phagocytized and eliminated by the reticuloendothelial system when they enter the body. short. With the help of biomimetic molecules such as liposom...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/69A61K31/704A61K31/7068A61P35/00
CPCA61K31/704A61K31/7068A61K47/543A61K47/544A61K47/6929A61P35/00
Inventor 刘兰霞刘丹冷希岗孔德领
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI