Production method of tobacco liposome modified by polyethylene glycol-poly(beta-amino ester)

A polyethylene glycol modification and polyethylene glycol technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve liposome loading capacity, stability, and embedding rate And the degradability rate needs to be improved to achieve good biocompatibility, improve stability, and increase the effect of grafting rate

Inactive Publication Date: 2019-03-01
嘉兴市秀洲区洪合镇中学
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The liposome prepared by this method is prepared by click chemical coupling method, the synthesis method is simple and efficient, the main fragment of the molecular structure is derived from the natural product cholesterol, and the rest of the molecular structure is derived from the natural product and organic synthesis raw materials that can be prepared in large quantities at an industrial level , the synthetic method is easy to promote to achieve low-cost large-scale preparation, and has good industrial productivity, but the loading capacity, stability, entrapment rate and degradability rate of the prepared liposomes need to be improved

Method used

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  • Production method of tobacco liposome modified by polyethylene glycol-poly(beta-amino ester)

Examples

Experimental program
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Effect test

Embodiment 1

[0024] (1) Add methoxypolyethylene glycol with a molecular weight of 1500 into tetrahydrofuran, stir at 0°C until dissolved, and add propylene dropwise according to the molar ratio of methoxypolyethylene glycol and acryloyl chloride to 1:2 Acryloyl chloride, heated and reacted at 25°C for 12h, filtered, and freeze-dried to obtain acryloyl chloride-modified polyethylene glycol.

[0025] (2) Add tobacco volatile oil, phospholipid and cholesterol with a molar ratio of 2.5:1 to ethanol, mix evenly, transfer to a supercritical carbon dioxide fluid reactor, and replace ethanol with carbon dioxide. The molar ratio to cholesterol is 0.4:1, add acryloyl chloride modified polyethylene glycol, add phosphoric acid to adjust the pH value of the system to 7.2, stir and disperse evenly, heat up to 40°C at a rate of 5°C / min, and under 15MPa, Stir at a rate of 100r / min for 15min, then raise the temperature to 58°C at a rate of 1°C / min, and stir at a rate of 500r / min for 30min at 28MPa until su...

Embodiment 2

[0028] (1) Add methoxypolyethylene glycol with a molecular weight of 2500 into tetrahydrofuran, stir at 4°C until dissolved, and add propylene dropwise according to the molar ratio of methoxypolyethylene glycol and acryloyl chloride to 1:4 Acryloyl chloride, heated and reacted at 30°C for 24h, filtered, and freeze-dried to obtain acryloyl chloride-modified polyethylene glycol.

[0029] (2) Add tobacco volatile oil, phospholipid and cholesterol with a molar ratio of 5:3:1 to ethanol, mix evenly, transfer to a supercritical carbon dioxide fluid reactor, and replace ethanol with carbon dioxide. The molar ratio of diol to cholesterol is 0.7:1, add polyethylene glycol modified by acryloyl chloride, add phosphoric acid to adjust the pH value of the system to 7.4, stir and disperse evenly, and heat up to 45°C at a rate of 10°C / min. Stir at a rate of 200r / min for 20min, then raise the temperature to 65°C at a rate of 3°C / min, and stir at a rate of 800r / min for 90min at 35MPa until sup...

Embodiment 3

[0032](1) Add methoxypolyethylene glycol with a molecular weight of 2000 into tetrahydrofuran, stir at 2°C until dissolved, and add propylene dropwise according to the molar ratio of methoxypolyethylene glycol and acryloyl chloride to 1:2.5 Acyl chloride, heated at 29°C for 16h, filtered, and freeze-dried to obtain acryloyl chloride-modified polyethylene glycol.

[0033] (2) Add tobacco volatile oil, phospholipid, and cholesterol with a molar ratio of 3.5:3:1 to ethanol, mix evenly, transfer to a supercritical carbon dioxide fluid reaction kettle, and replace ethanol with carbon dioxide. The molar ratio of diol to cholesterol is 0.6:1, add polyethylene glycol modified by acryloyl chloride, add phosphoric acid to adjust the pH value of the system to 7.3, stir and disperse evenly, and heat up to 42°C at a rate of 7°C / min. Stir at a rate of 130r / min for 19min, then raise the temperature to 62°C at a rate of 1.5°C / min, and stir at a rate of 600r / min for 45min at 32MPa until superc...

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Abstract

The invention provides a production method of tobacco liposome modified by polyethylene glycol-poly(beta-amino ester). The production method of the tobacco liposome modified by polyethylene glycol-poly(beta-amino ester) comprises the following steps that methoxy polyethylene glycol is added into tetrahydrofuran, stirring to dissolve at low temperature is carried out, acrylamide chloride is added,and heating reaction is carried out to obtain polyethylene glycol modified by the acrylamide chloride; tobacco volatile oil, phospholipid and cholesterol are added to the ethanol and transferred to asupercritical carbon dioxide fluid reactor, carbon dioxide is added to replace the ethanol, polyethylene glycol modified by the acrylamide chloride is added, phosphoric acid regulating system PH valueis added, stirring is carried out, supercritical carbon dioxide is pressed and heated to precipitated, pressure is released quickly, the tobacco liposome modified by polyethylene glycol which is modified by the acrylamide chloride is obtained; the tobacco liposome modified by polyethylene glycol which is modified by the acrylamide chloride, 1,4-butanediol diacrylate and 1-amino-3-propanol is added to trichloromethane, ultrasonic dispersion, microwave reaction, precipitation filtration and drying are carried out, and the tobacco liposome modified by polyethylene glycol-poly(beta-amino ester) is obtained.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to a production method of polyethylene glycol-poly(β-amino ester) modified tobacco liposome. Background technique [0002] Cationic liposomes are a special kind of cationic surfactant, usually including a cationic head, two hydrophobic saturated or unsaturated alkyl chain ethyl linkages, cationic liposomes can spontaneously form lipid bilayers The structure of liposome, which has the characteristics of similar cell structure and biomembrane, has become an important pharmaceutical intermediate in the field of biomedical technology. [0003] The preparation techniques of cationic liposomes include film dispersion method, film-ultrasonic dispersion method, melting method, freeze-thaw method, injection method, reverse evaporation method and double emulsion method. Chinese patent CN102161688B discloses a biocompatible synthetic liposome containing cholesterol structural fragments, a p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/81A61K47/59A61K47/60A61K47/69
CPCA61K36/81A61K47/59A61K47/60A61K47/6911
Inventor 朱胜祥
Owner 嘉兴市秀洲区洪合镇中学
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