Nucleotide phospholipid molecule and lipidosome and preparation method and application thereof

Abstract

The invention discloses a nucleotide phospholipid compound and a preparation method thereof, wherein the nucleotide phospholipid compound has a structure with a general expression (VIII) or (IX), and a large amount of nucleotide phospholipid compounds can be conveniently prepared on the basis of a one-pot method strategy. The invention further provides a novel lipidosome and a preparation method thereof, and the phospholipids lipidosome has the characteristics of simple preparation, good utility, wide application range and the like. The lipidosome can be used as a molecular biology tool for researching antisense oligonucleotide and short interfering RNA (siRNA) mechanisms and also has potential medicament development prospects.

Description

technical field The invention belongs to the technical field of drug transport carriers, and relates to a novel nucleotide phospholipid molecule used for transmembrane nucleic acid transport and a preparation method thereof, and also relates to a liposome formed by the nucleotide phospholipid molecule, a preparation method and application thereof . Background technique Some drugs and biologically active molecules based on nucleic acid, such as isonucleosides, oligonucleotides, small interfering RNA (siRNA), and various RNAs, DNA single- and double-strands must be able to effectively solve their permeability if they want to exert their biological activity. ability to cross the cell membrane. Many techniques have been used to improve the cellular uptake of these compounds, such as high-pressure intravenous injection, liposomes, and nanopolymers, but these methods have their own shortcomings that limit their development. At present, liposome carrier is the most widely used i...

AI Technical Summary

Problems solved by technology

Natural phospholipids contain negative charges and have poor carrying capacity for nucleic acid molecules. Liposomes need cumbersome processing and preparation equipment and processes to make liposomes. Although they have cost advantages, they are poor in ease of use and cannot be used as transfection reagents.

Although cationic liposomes can efficiently carry and transport nucleic acid molecules, they can also cause serious damage to cell membranes. Although they are easy to use, their cytotoxicity determines that they can only be used in transfection experiments at low concentrations and cannot be used on a large scale. in pharmaceutical preparations

Moreover, the cationic liposome process as a high-efficiency transfection reagent is controlled by foreign countries, and the price is high

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