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Nano-drug carrier and preparation method and application thereof

A nano drug and drug activity technology, applied in the field of biochemistry, can solve the problems of difficult drug release function, poor cell selectivity, affecting transfection efficiency, etc., and achieve the effects of reducing drug toxicity, high delivery efficiency, and improving release efficiency

Active Publication Date: 2019-08-09
BEIJING CARRIUS BIO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the degree of polymerization of organic polymer materials will significantly affect the transfection efficiency, and the reproducibility is poorer than that of liposomes.
At present, the main problem of liposome delivery of gene drugs is that the cell selectivity is poor, and it is difficult to efficiently and specifically realize the drug release function in the target cells

Method used

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  • Nano-drug carrier and preparation method and application thereof
  • Nano-drug carrier and preparation method and application thereof
  • Nano-drug carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Embodiment 1 prepares compound b

[0061]

[0062] Dissolve 1 mM compound a in 3 ml of 1,4-dioxane solvent, add 1 mM potassium hydroxide powder, then add 1 mM n-dodecyl bromide, raise the temperature to 105° C., and react overnight. TLC monitoring, after the reaction was completed, it was extracted with dichloromethane and water, dried, rotary evaporated, and passed through the column with petroleum ether and ethyl acetate 5:1 to obtain the product, namely compound b.

Embodiment 2

[0063] Embodiment 2 prepares formula I-1 compound

[0064]

[0065] Dissolve compound b in anhydrous dichloromethane and add 1.2 equivalents of triethylamine, add acryloyl chloride dropwise under ice bath conditions, remove the ice bath, react at room temperature for 5 hours, add water to quench after the reaction is completed, extract, dry, rotary evaporate, and use Petroleum ether and ethyl acetate 10:1 through the column. A light yellow liquid is obtained, namely the compound of formula I-1.

Embodiment 3

[0066] Embodiment 3 preparation formula II-1 liposome: ROS-TK-1

[0067]

[0068] Mix the compound of formula I-1 with the fatty amine shown in compound 1 at a molar ratio of 2.4:1, heat to 80°C, react for 36 hours, and pass through the column with dichloromethane and methanol at 20:1 to prepare liposomes of formula II-1 : ROS-TK-1, its nuclear magnetic spectrum is as follows figure 2 shown.

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Abstract

The invention relates to a nano-drug carrier and a preparation method and application thereof. The nano-drug carrier is cationic liposome based on an oxidative stress (ROS) response, the liposome is prepared from an organic amine compound and a compound in the formula I through an addition reaction; organic amine is aliphatic amine or aromatic amine; the compound in the formula I is as shown in the description, wherein m is an integer from 7 to 20, R1 is -O- or -S- or -NH-, and R2 is -S- or -O-. The liposome has cellular selectivity in the drug delivery process, not only is the release efficiency of drugs in disease cells improved, but also the drug toxicity on normal cells is lowered.

Description

technical field [0001] The invention relates to the field of biochemical technology, in particular to a nano drug carrier and its preparation method and application. Background technique [0002] Compared with traditional chemically synthesized drugs, gene drugs have the advantages of high curative effect, less side effects, and strong specificity, and for some diseases where traditional drugs are not effective, such as various tumors, genetic diseases and immune-related diseases, gene drugs can also be obtained Better curative effect. At present, hundreds of gene drugs have entered clinical trials, and finding a carrier that can efficiently transfect gene drugs into disease tissues and is non-toxic is one of the main tasks in the development of gene drugs. [0003] In order to transfect gene drugs into cells more efficiently, a variety of gene drug carriers have been developed and applied, such as inorganic materials, polymer materials, liposomes, viruses, etc. Although v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/18A61K47/22A61K47/20A61K48/00A61K31/713A61P35/00A61P9/00A61P25/28A61P27/02
CPCA61K9/127A61K31/713A61K47/18A61K47/20A61K47/22A61K48/0033A61K48/005A61P9/00A61P25/28A61P27/02A61P35/00
Inventor 汪铭梁春菁
Owner BEIJING CARRIUS BIO LTD
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