Preparation method of fluorocarbon compound liposome

Abstract

The invention relates to a preparation method of fluorocarbon compound liposome. The method comprises the following steps of a. dissolving 1-50 parts by weight of phospholipid and 0-50 parts by weight of cholesterol in 200 parts by weight of an organic solvent, and mixing uniformly under the assistance of ultrasonic; b. adding 10-50 parts by weight of fluorocarbon in the organic solvent with the phospholipid dissolved therein, and continuously mixing uniformly under the assistance of the ultrasonic; and c. dropwise-adding the solution obtained from the step b in 100-500 parts by weight of a salt solution, stirring the solution with a stirring rate of 500-2,500 revolutions per minute until the organic solvent is volatilized completely, the stirring time being 2 hours, and thus the fluorocarbon compound liposome is obtained. The prepared fluorocarbon compound liposome has good stability and small particle size. The method is simple, and is convenient for large-scale production. The prepared fluorocarbon compound liposome can have good applications in the aspects such as emergency oxygen supply drugs, acute blood supply, contrast agents, etc.

Description

technical field

[0001] The invention relates to a preparation method of liposome, in particular to a preparation method of fluorocarbon liposome liposome. Background technique

[0002] Fluorochemicals are molecules that contain fluorine atoms. Fluorinated compounds or fluorocarbons are contrasted with perfluorocarbons (“PFCs”), which are chemically inert synthetic molecules composed primarily of carbon and fluorine atoms. Liquid PFCs and fluorocarbons are usually clear, colorless, odorless, high density, low surface tension, and not easy to decompose in the body. PFC has a strong ability to carry gases, and the gases referred to here include oxygen, carbon dioxide and nitrogen. The principle of oxygen in PFC solution is different from that of hemoglobin. Hemoglobin is combined through the chemical force between iron and oxygen, and the combination is strong; while both PFC and gas have low cohesive energy density, and the combination of the two is carried out through weak...

Examples

Embodiment 1

[0021] In parts by weight, the formula is as follows:

[0022] Phosphate buffer solution (0.01 M) 200 parts

[0023] Soy lecithin 20 parts

[0024] FC-77 20 copies

[0025] 200 parts of ether

[0026] Preparation Process:

[0027] In parts by weight, 20 parts of soybean lecithin are dissolved in 200 parts of ether, and ultrasonically mixed;

[0028] Add 20 parts of FC-77 (a mixture of perfluorooctane and perfluorocyclohexyl ether) to the ether solution of phospholipids, and continue to mix evenly by ultrasonic;

[0029] will step The obtained solution was slowly added dropwise to 200 parts of phosphate buffer solution, and the solution was stirred (the stirring speed was 1000 rpm), and stirred until the ether was completely volatilized, and the time was about 2.5 hours. That is, FC-77 liposomes can be obtained.

[0030] Appearance of the preparation: milky white solution; dilute 10 times to get a light white transparent solution with bluish opalescence.

[00...

Embodiment 2

[0034] In parts by weight, the formula is as follows:

[0035] Phosphate buffer solution (0.01 M) 200 parts

[0036] Egg yolk lecithin 19 parts

[0037] Cholesterol 1 part

[0038] Perfluorooctyl bromide 10 parts

[0039] Chloroform 200 parts

[0040] Preparation Process:

[0041] In parts by weight, 19 parts of egg yolk lecithin and 1 part of cholesterol were dissolved in 200 parts of chloroform, and ultrasonically mixed evenly;

[0042] Add 25 parts of perfluorooctyl bromide to the chloroform solution of phospholipids, and continue ultrasonic mixing;

[0043] will step The obtained solution was slowly added dropwise to 200 parts of phosphate buffer solution, and the solution was stirred (the stirring speed was 2000 rpm), and stirred until the chloroform was completely volatilized for about 1.5 hours. That is, perfluorooctyl bromide liposomes can be obtained.

[0044] Appearance of the preparation: milky white solution, diluted 10 times to get a light white ...

Embodiment 3

[0048] In parts by weight, the formula is as follows:

[0049] Sodium chloride solution (0.9%) 200 parts

[0050] Hydrogenated soybean lecithin 20 parts

[0051] Cholesterol 10 servings

[0052] 1-Bromotridefluorohexane 25 parts

[0053] 200 parts of ether

[0054] Preparation Process:

[0055] In parts by weight, 20 parts of hydrogenated soybean lecithin and 10 parts of cholesterol are dissolved in 200 parts of ether, and ultrasonically mixed;

[0056] Add 25 parts of 1-bromotridefluorohexane to the ether solution of phospholipids, and continue to ultrasonically mix evenly;

[0057] will step The resulting solution was slowly added dropwise to 200 parts of sodium chloride solution (0.9%), the solution was stirred (stirring speed was 1500 rpm), and stirred until the ether was completely volatilized for about 2 hours. That is, 1-bromotridefluorohexane liposomes can be obtained.

[0058] Appearance of the preparation: milky white solution, dilute 10 times to get...

technical field

[0001] The invention relates to a preparation method of liposome, in particular to a preparation method of fluorocarbon liposome liposome. Background technique

[0002] Fluorochemicals are molecules that contain fluorine atoms. Fluorinated compounds or fluorocarbons are contrasted with perfluorocarbons (“PFCs”), which are chemically inert synthetic molecules composed primarily of carbon and fluorine atoms. Liquid PFCs and fluorocarbons are usually clear, colorless, odorless, high density, low surface tension, and not easy to decompose in the body. PFC has a strong ability to carry gases, and the gases referred to here include oxygen, carbon dioxide and nitrogen. The principle of oxygen in PFC solution is different from that of hemoglobin. Hemoglobin is combined through the chemical force between iron and oxygen, and the combination is strong; while both PFC and gas have low cohesive energy density, and the combination of the two is carried out through weak...

Examples

Embodiment 1

[0021] In parts by weight, the formula is as follows:

[0022] Phosphate buffer solution (0.01 M) 200 parts

[0023] Soy lecithin 20 parts

[0024] FC-77 20 copies

[0025] 200 parts of ether

[0026] Preparation Process:

[0027] In parts by weight, 20 parts of soybean lecithin are dissolved in 200 parts of ether, and ultrasonically mixed;

[0028] Add 20 parts of FC-77 (a mixture of perfluorooctane and perfluorocyclohexyl ether) to the ether solution of phospholipids, and continue to mix evenly by ultrasonic;

[0029] will step The obtained solution was slowly added dropwise to 200 parts of phosphate buffer solution, and the solution was stirred (the stirring speed was 1000 rpm), and stirred until the ether was completely volatilized, and the time was about 2.5 hours. That is, FC-77 liposomes can be obtained.

[0030] Appearance of the preparation: milky white solution; dilute 10 times to get a light white transparent solution with bluish opalescence.

[00...

Embodiment 2

[0034] In parts by weight, the formula is as follows:

[0035] Phosphate buffer solution (0.01 M) 200 parts

[0036] Egg yolk lecithin 19 parts

[0037] Cholesterol 1 part

[0038] Perfluorooctyl bromide 10 parts

[0039] Chloroform 200 parts

[0040] Preparation Process:

[0041] In parts by weight, 19 parts of egg yolk lecithin and 1 part of cholesterol were dissolved in 200 parts of chloroform, and ultrasonically mixed evenly;

[0042] Add 25 parts of perfluorooctyl bromide to the chloroform solution of phospholipids, and continue ultrasonic mixing;

[0043] will step The obtained solution was slowly added dropwise to 200 parts of phosphate buffer solution, and the solution was stirred (the stirring speed was 2000 rpm), and stirred until the chloroform was completely volatilized for about 1.5 hours. That is, perfluorooctyl bromide liposomes can be obtained.

[0044] Appearance of the preparation: milky white solution, diluted 10 times to get a light white ...

Embodiment 3

[0048] In parts by weight, the formula is as follows:

[0049] Sodium chloride solution (0.9%) 200 parts

[0050] Hydrogenated soybean lecithin 20 parts

[0051] Cholesterol 10 servings

[0052] 1-Bromotridefluorohexane 25 parts

[0053] 200 parts of ether

[0054] Preparation Process:

[0055] In parts by weight, 20 parts of hydrogenated soybean lecithin and 10 parts of cholesterol are dissolved in 200 parts of ether, and ultrasonically mixed;

[0056] Add 25 parts of 1-bromotridefluorohexane to the ether solution of phospholipids, and continue to ultrasonically mix evenly;

[0057] will step The resulting solution was slowly added dropwise to 200 parts of sodium chloride solution (0.9%), the solution was stirred (stirring speed was 1500 rpm), and stirred until the ether was completely volatilized for about 2 hours. That is, 1-bromotridefluorohexane liposomes can be obtained.

[0058] Appearance of the preparation: milky white solution, dilute 10 times to get...

Images