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Liposome complex not penetrating blood-brain barrier and preparation method thereof

A liposome complex, blood-brain barrier technology, applied in the field of medicine, can solve the problems of lack of good treatment measures and side effects, and achieve the effects of improving binding efficiency, prolonging shelf life and improving stability

Active Publication Date: 2019-10-01
邢瑞
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The FDA approved temozolomide (TMZ) for the first-line treatment of glioblastoma, but the main obstacle in the treatment of glioblastoma is that TMZ will produce serious side effects, so the dose is limited clinically
Currently, there is no good treatment for the side effects of TMZ on the market

Method used

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  • Liposome complex not penetrating blood-brain barrier and preparation method thereof
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  • Liposome complex not penetrating blood-brain barrier and preparation method thereof

Examples

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Effect test

Embodiment 1

[0030] The invention provides a liposome complex impermeable to the blood-brain barrier, comprising: 4 parts of D-methionine, 8 parts of soybean lecithin, 4 parts of egg yolk phosphatidylinositol, 0.8 parts of cholesterol, chlorinated 2 parts of sodium, 6 parts of glucose, 0.5 parts of sodium bisulfite;

[0031] The present invention also provides a preparation method of a liposome complex impermeable to the blood-brain barrier, comprising the following steps:

[0032] S1. After uniformly mixing soybean lecithin, egg yolk phosphatidylinositol and cholesterol, dissolve it in 60 parts by weight of an organic solvent to obtain the first mixed solution, and heat the first mixed solution under 25 kHz ultrasonic waves to obtain the second mixed solution. The heat treatment of the mixed liquid is as follows: heat the mixed liquid for 3 minutes to 60°C and keep it for 5 minutes, then raise the temperature from 60°C for 5 minutes to 70°C and keep it for 10 minutes, then cool it down fr...

Embodiment 2

[0036] The liposome complex that does not pass through the blood-brain barrier includes by weight: 6 parts of D-methionine, 20 parts of soybean lecithin, 15 parts of egg yolk phosphatidylinositol, 2 parts of cholesterol, 4 parts of sodium chloride, glucose 8 parts, 1 part of sodium bisulfite;

[0037] The present invention also provides a preparation method of a liposome complex impermeable to the blood-brain barrier, comprising the following steps:

[0038] S1. After uniformly mixing soybean lecithin, egg yolk phosphatidylinositol and cholesterol, dissolve it in 120 parts by weight of an organic solvent to obtain the first mixed solution, and heat the first mixed solution under 31 kHz ultrasonic waves to obtain the second mixed solution. The heat treatment of the mixed liquid is as follows: heat the mixed liquid for 3 minutes to 60°C and keep it for 5 minutes, then raise the temperature from 60°C for 5 minutes to 70°C and keep it for 10 minutes, then cool it down from 70°C fo...

Embodiment 3

[0042] The liposome complex that does not pass through the blood-brain barrier includes by weight: 5 parts of D-methionine, 14 parts of soybean lecithin, 10 parts of egg yolk phosphatidylinositol, 1.4 parts of cholesterol, 3 parts of sodium chloride, glucose 7 parts, 0.8 parts of sodium bisulfite;

[0043] The present invention also provides a preparation method of a liposome complex impermeable to the blood-brain barrier, comprising the following steps:

[0044] S1. After uniformly mixing soybean lecithin, egg yolk phosphatidylinositol and cholesterol, they are dissolved in 90 parts by weight of an organic solvent to obtain the first mixed solution, and the first mixed solution is heated under 28 kHz ultrasonic waves to obtain the second mixed solution. The heat treatment of the mixed liquid is as follows: heat the mixed liquid for 3 minutes to 60°C and keep it for 5 minutes, then raise the temperature from 60°C for 5 minutes to 70°C and keep it for 10 minutes, then cool it d...

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Abstract

The invention discloses a liposome complex which does not penetrate the blood-brain barrier and a preparation method thereof. The liposome complex comprises, by weight, 4-6 parts of D-methionine, 8-20parts of soybean lecithin, 4-15 parts of yolk phosphatidylinositol, 0.8-2 parts of cholesterol, 2-4 parts of sodium chloride, 6-8 parts of glucose and 0.5-1 part of sodium hydrogen sulfite. The preparation method of the liposome complex includes the steps that the soybean lecithin, the yolk phosphatidylinositol and the cholesterol are uniformly mixed, the obtained mixture is dissolved in an organic solvent to prepare a blank liposome suspension, the blank liposome suspension is mixed with D-methionine, and cooling and drying are conducted to obtain the liposome complex. The liposome complex can effectively alleviate the damage of temozolomide (TMZ) to normal tissues, thereby maintaining the health of the human body.

Description

technical field [0001] The invention relates to the technical field of medicine. More specifically, the present invention relates to a liposome complex impermeable to the blood-brain barrier and a preparation method thereof. Background technique [0002] Liposomes are ultrafine particles with a diameter of several nanometers to several micrometers formed by directional arrangement of phospholipid bimolecules, and fat-soluble and water-soluble drugs are respectively encapsulated inside and outside the bilayer. Liposomes can enable drugs to be targeted, improve and prolong curative effect, alleviate toxicity, avoid drug resistance and change the route of administration. Since the first application of liposomes as drug carriers by Rahman et al. in the 1960s, the research on the preparation process, mechanism of action, distribution in vivo, pharmacology and toxicology of liposomes has continued to deepen. [0003] More than 14 million cancer cases are newly discovered in the ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4188A61K47/02A61K47/26A61K47/34A61K47/54A61K47/69A61P35/00
CPCA61K9/127A61K31/4188A61K47/02A61K47/26A61K47/34A61K47/542A61K47/6911A61P35/00
Inventor 邢瑞王明勇田晶晶
Owner 邢瑞
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