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Preparation method of pulsed electric field sensitive liposome for targeted release of drug carrier

A pulsed electric field, liposome technology, applied in the directions of liposome delivery, drug delivery, drug combination, etc., can solve the problems of connective tissue damage during heating time, reduce the heat sensitivity of liposomes, and low drug release efficiency, and improve the effect. effect, poison reduction, high release rate effect

Active Publication Date: 2016-10-05
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] (1) pH-sensitive immunoliposomes can easily cause immune reactions;
[0008] (2) The aggregation of heat-sensitive liposomes in the lesion is a passive targeting distribution, with limited specificity, and excessive heating time can cause damage to normal connective tissue;
[0009] (3) Due to the embedding of hydrophilic macromolecules in heat-sensitive long-circulation liposomes, the heat sensitivity of liposomes is reduced to a certain extent, and the drug release efficiency is low during electrotherapy

Method used

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  • Preparation method of pulsed electric field sensitive liposome for targeted release of drug carrier
  • Preparation method of pulsed electric field sensitive liposome for targeted release of drug carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Take by weighing 250mg soybean lecithin, 50mg cholesterol, 25mg vitamin E and 50ml rotary evaporation flask, and use the mixed solution of 10ml chloroform and ethanol (V 氯仿 :V 乙醇 =9:1) was fully dissolved, and the mixture of chloroform and ethanol was evaporated under reduced pressure in a rotary evaporator (RE-2000B, Shanghai Yarong Biochemical Instrument Factory) at a temperature of 30°C until a uniform lipid film was formed. Then, at a temperature of 25° C., vacuum-dry in a vacuum oven (DZF-6050, Shanghai Qixin Scientific Instrument Co., Ltd.) for 15 hours to remove residual chloroform and ethanol. The lipid film was fully dissolved with 9ml of ether to obtain a mixture of ether and phospholipid; 3ml of 0.05M carboxyfluorescein aqueous solution was added to the mixture of ether and phospholipid. At a temperature of 5°C, the power was 600 W in a water bath for 3 minutes so that the two phases were fully mixed. Under the condition that the temperature was lower than ...

Embodiment 2

[0037] Take by weighing 150mg egg yolk lecithin, 75mg cholesterol, 15mg vitamin E in the rotary evaporating flask of 50ml, and with the mixed solution of the chloroform of 10ml and ethanol (V 氯仿 :V 乙醇 =9:1) was fully dissolved, and the mixture of chloroform and ethanol was evaporated under reduced pressure in a rotary evaporator (RE-2000B, Shanghai Yarong Biochemical Instrument Factory) at a temperature of 35°C until a uniform lipid film was formed. Then, at a temperature of 30° C., vacuum-dry in a vacuum oven (DZF-6050, Shanghai Qixin Scientific Instrument Co., Ltd.) for 10 h to remove residual chloroform and ethanol. Fully dissolve the lipid film with 9 ml of ether to obtain a mixture of ether and phospholipid; add 3 ml of 0.05 M carboxyfluorescein aqueous solution to the mixture of ether and phospholipid. At a temperature of 8°C, the power was 600W and the water bath was ultrasonically charged for 5 minutes to fully mix the two phases. Under the condition that the tempera...

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Abstract

The invention discloses a preparation method of a pulsed electric field-sensitive liposome for targeted release of a drug carrier, comprising the following steps: (1) preparing a lipid film by using phospholipids, cholesterol and vitamin E as raw materials; (2) preparing the lipid film Dissolving with ether, loading the drug to be encapsulated to obtain the liposome; (3) centrifuging to remove the unencapsulated drug outside the liposome; (4) adding magnesium salt to modify the liposome to obtain pulsed electric field sensitive liposome. The preparation process of the invention is simple, the encapsulation rate of the liposome to the water-soluble drug is high, the performance is stable, and the release rate is high under the action of a pulsed electric field.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of pulse electric field sensitive liposomes for targeted release of drug carriers. Background technique [0002] Liposomes are monolayer or multilayer lipid bimolecular membranes encapsulated in the form of concentric circles, similar to cell membrane microspheres, and their main components are phospholipids and cholesterol. In the early 1970s, liposomes were used as drug carriers to embed amyloglucosidase for the first time in the treatment of glycogenosis. Since then, as a drug carrier, liposomes have the advantages of targeting the drug to the reticuloendothelial system, prolonging drug efficacy, reducing drug toxicity, improving efficacy, avoiding tolerance, and changing the route of administration, etc., and thus have attracted extensive attention from the medical community. However, as a drug carrier, liposomes still have disadvantages such a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/08A61K47/02A61K47/24A61P35/00
Inventor 曾新安刘志伟孙大文韩忠王满生
Owner SOUTH CHINA UNIV OF TECH