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A kind of △5-cholesteryl sulfate compound liposome and its preparation method

A technology of cholesteryl sulfate and compound, which is applied in the field of △5-cholesteryl sulfate compound liposome and its preparation, to achieve the effect of overcoming adverse effects, good dispersion and stable properties

Active Publication Date: 2021-05-14
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The technical problem to be solved by the present invention is that no matter which method is used today, cholesterol needs to be added to liposomes to improve its stability, and excessive serum cholesterol is the main risk factor for coronary heart disease

Method used

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  • A kind of △5-cholesteryl sulfate compound liposome and its preparation method
  • A kind of △5-cholesteryl sulfate compound liposome and its preparation method
  • A kind of △5-cholesteryl sulfate compound liposome and its preparation method

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Effect test

Embodiment 1

[0029] The representative components of △5-cholesteryl sulfate group are 24-methylene-cholest-5-ene-3β-ol-3-sulfate group and cholest-5-ene-3β-sulfate group. The structural formula is shown in figure 1 , the preparation method is as follows: take the body wall of the aquatic product, grind and sieve after vacuum freeze-drying, add a certain volume of chloroform:methanol solution (2:1, v / v), and keep the total solid-liquid ratio as 1:15 (m / v), continuous stirring and leaching for 24h. After filtering the extract, add 1 / 4 volume of water, fully oscillate and mix, and then let stand to separate layers. After the layers were separated, the lower chloroform layer was removed, concentrated under reduced pressure in vacuo, and dried to obtain the total fat. Take 200-300 mesh silica gel and activate it at 105°C for 10-12 hours, then cool it at room temperature for use, dissolve the total fat in chloroform, mix it with silica gel, pour it into a silica gel column quickly and evenly, ...

Embodiment 2

[0032] Wherein the membrane material components are: 1.0g lecithin and 0.2g Δ5-cholesteryl sulfate compound. All the other are identical with embodiment 1.

[0033] The prepared blank nanoliposomes of △5-cholesteric sulfate group compound is a relatively transparent light yellow solution with an average particle diameter of 107.3nm and a dispersion coefficient of 0.193. It has good stability and can be stored for more than 10 days at 4°C. Equal stability to cholesterol blank liposomes.

Embodiment 3

[0035] Application of a kind of embodiment 1 liposome in drug delivery system:

[0036] Accurately weigh 0.6g of lecithin, 0.2g of △5-cholesteric sulfate group compound and 20mg of astaxanthin, completely dissolve in 12mL of dichloromethane, and remove the dichloromethane by vacuum rotation in a water bath at 40°C. A uniform lipid film was formed on the Add 20 mL of normal saline solution, place it in an ultrasonic cell disruptor and sonicate to obtain a deep red suspension, namely the crude liposome suspension of △5-cholesteryl sulfate compound encapsulating astaxanthin. The crude liposome suspension was centrifuged at 10000 g for 10 min to remove impurities that did not form liposomes in the system. The supernatant is the prepared astaxanthin-encapsulating △5-cholesteric sulfate compound nanoliposome. The prepared △5-cholesteric sulfate nanoliposomes encapsulating astaxanthin is a deep red solution, with an average particle diameter of 110.3nm, a dispersion coefficient of ...

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Abstract

The invention relates to the technical field of food nutrition, in particular to a Δ5-cholesteryl sulfate compound liposome and a preparation method thereof. The △5-cholesteric sulfate-based compound liposome refers to a liposome membrane material that does not encapsulate the drug to be encapsulated but contains a △5-cholesteric sulfate-based compound, wherein the membrane material of the liposome consists of The composition and its weight percentage are: 66.7%-83.3% of phospholipids, 16.7%-33.3% of △5-cholesteric sulfate-based compounds, no cholesterol; the average particle size is 100-200nm, narrow distribution, good stability and dispersion Good performance, encapsulation rate of more than 90% when encapsulating drugs.

Description

technical field [0001] The invention relates to the technical field of food nutrition, in particular to a Δ5-cholesteryl sulfate compound liposome and a preparation method thereof. Background technique [0002] Liposome is an excellent carrier with cell membrane-like structure formed by amphiphilic molecules such as phospholipids in aqueous solution. It can wrap hydrophilic, lipophilic and amphiphilic drugs and nutritional factors, which can protect drugs and nutritional factors. Reduce its toxic and side effects, achieve the purpose of sustained release, and improve the targeting and bioavailability of the drug. Liposome preparation methods mainly include thin film dispersion method, ultrasonic dispersion method, ethanol injection method, supercritical method and so on. Currently widely used methods are thin film dispersion and ultrasonic dispersion. The film dispersion method is to dissolve lipids such as phospholipids and cholesterol in an organic solvent, then place th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/28
CPCA61K9/1271A61K9/1277A61K47/28
Inventor 张恬恬王玉明薛长湖薛勇李兆杰王静凤常耀光唐庆娟徐杰姜晓明
Owner OCEAN UNIV OF CHINA
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