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A kind of pyrromidazole polyamide liposome and its preparation method and application

A technology for pyrrolimidazole polyamide ester and pyrrolimidazole polyamide, which is applied in the field of pyrrolimidazole polyamide liposome and its preparation, can solve the problems of limited water solubility, low entrapment rate of pyrrolimidazole polyamide, etc. volume, improve blood circulation time, and increase the effect of accumulation

Active Publication Date: 2020-06-05
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, hydroxypropyl β-cyclodextrin has a cylindrical hydrophobic inner cavity and a hydrophilic outer edge, resulting in very low entrapment efficiency of pyrrolidazole polyamides
However, hydroxypropyl β-cyclodextrin itself has limited water solubility and is prone to hemolysis and irritation.

Method used

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  • A kind of pyrromidazole polyamide liposome and its preparation method and application
  • A kind of pyrromidazole polyamide liposome and its preparation method and application
  • A kind of pyrromidazole polyamide liposome and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: the preparation method of pyrrolidazole polyamide liposome

[0037] (1) 24 μL of distearoylphosphatidylcholine (DSPC) with a concentration of 0.1M and 15 μL of cholesterol with a concentration of 50 mM were dissolved in a mixed solution of 2 mL of chloroform and 1 mL of methanol;

[0038] (2) Under reduced pressure, the mixed solvent is removed by rotary evaporation, and a uniform film is obtained at the bottom of the bottle;

[0039] (3) Dissolve 0.1 μmol of pyrrolimidazole polyamide (compound of formula I) in 2 mL of ultrapure water, add it to the above-mentioned glass bottle covered with phospholipid film, and sonicate for 10 to 20 minutes until the solution changes from turbid to clear;

[0040] (4) Pass the solution obtained above through a 0.22 μm water filter membrane, repeating 3 times;

[0041] (5) Transfer the above mixed aqueous solution of pyrromidazole and polyamide to an ultrafiltration centrifuge tube with a molecular cut-off of 50,000, and w...

Embodiment 2

[0042] Embodiment 2: the preparation method of pyrrolidazole polyamide liposome

[0043] (1) 240 μL of distearoylphosphatidylcholine (DSPC) with a concentration of 0.1M and 150 μL of cholesterol with a concentration of 50 mM were dissolved in a mixed solution of 20 mL of chloroform and 10 mL of methanol;

[0044] (2) Under reduced pressure, the mixed solvent is removed by rotary evaporation, and a uniform film is obtained at the bottom of the bottle;

[0045] (3) Dissolve 1 μmol of pyrrolimidazole polyamide (compound of formula I) in 20 mL of ultrapure water, add it to the glass bottle covered with phospholipid film, and sonicate for 10 to 20 minutes until the solution changes from turbid to clear;

[0046] (4) Pass the solution obtained above through a 0.22 μm water filter membrane, repeating 3 times;

[0047] (5) Transfer the above mixed aqueous solution of pyrromidazole and polyamide to an ultrafiltration centrifuge tube with a molecular cut-off of 50,000, and wash with ul...

Embodiment 3

[0048] Embodiment 3: the preparation method of pyrrolidazole polyamide liposome

[0049] (1) 24 μL of carboxylated polyethylene glycol-distearoylphosphatidylethanolamine (DSPC-PEG-COOH) with a concentration of 0.1M and 15 μL of cholesterol with a concentration of 50 mM were dissolved in a mixed solution of 2 mL of chloroform and 1 mL of methanol;

[0050] (2) Under reduced pressure, the mixed solvent is removed by rotary evaporation, and a uniform film is obtained at the bottom of the bottle;

[0051] (3) Dissolve 0.1 μmol of pyrrolimidazole polyamide (compound of formula I) in 2 mL of ultrapure water, add it to the above-mentioned glass bottle covered with phospholipid film, and sonicate for 10 to 20 minutes until the solution changes from turbid to clear;

[0052] (4) Pass the solution obtained above through a 0.22 μm water filter membrane, repeating 3 times;

[0053] (5) Transfer the above mixed aqueous solution of pyrromidazole and polyamide to an ultrafiltration centrifu...

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Abstract

The invention provides a pyrrole-imidazole polyamide lipidosome as well as a preparation method and use thereof and particularly discloses the pyrrole-imidazole polyamide lipidosome. The pyrrole-imidazole polyamide lipidosome is formed by a lipid bilayer and pyrrole-imidazole polyamide entrapped in the lipid bilayer, wherein the lipid bilayer contains phospholipid molecules and cholesterol, the molar ratio of the phospholipid molecules to cholesterol is (3-4) to 1, and the molar ratio of the phospholipid molecules to pyrrole-imidazole polyamide is (20-30) to 1. According to the pyrrole-imidazole polyamide lipidosome, pyrrole-imidazole polyamide is entrapped in an inner cavity of the lipidosome, so that compared with entrapping manners of other carriers, the pyrrole-imidazole polyamide lipidosome has the advantages that the entrapment amount can be effectively increased, and the bioavailability of pyrrole-imidazole polyamide drugs is remarkably improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pyrromidazole polyamide liposome and a preparation method thereof. Background technique [0002] Gene-targeted cancer therapy is an emerging and efficient treatment method, and it is particularly critical to develop small molecule compound inhibitory drugs for tumor treatment. Pyrrolimidazole polyamide is a class of artificially synthesized five-membered heterocyclic compounds mainly composed of N-methylpyrrole (Py), N-methylimidazole (Im) and N-methyl-3-hydroxypyrrole (Hp) aromatic amino acids. , artificial small molecule ligands linked via amide bonds. Pyrrole-imidazole polyamides recognize DNA sequences by forming the most possible hydrogen bonds with DNA base pairs: antiparallel paired Py / Py recognizes T·A or A·T base pairs; Im / Py is specific Py / Im specifically recognizes C·G base pairs, Hp / Py specifically recognizes T·A base pairs, and Py / Hp specifically recogn...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/10A61K47/28A61K31/787A61P35/00A61P35/02
CPCA61K9/127A61K31/787A61K47/10A61K47/24A61K47/28
Inventor 粟武敖丽娇武春雷黄亮
Owner SHENZHEN INST OF ADVANCED TECH
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