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Preparation method of dihydromyricetin-carried ternary complex liposome

A technology of dihydromyricetin and ternary compounding, which is applied in liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of macrocytic toxicity and maintain biological activity , Improve transfection efficiency, reduce toxicity

Active Publication Date: 2015-08-05
INST OF APPLIED CHEM JIANGXI ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cationic liposome is the most widely used non-viral carrier, which has high gene carrying capacity and cell uptake rate, but with a large number of positive charges on the surface, it is easy to react with polyanions in the body environment in blood circulation, thereby causing greater cytotoxicity

Method used

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  • Preparation method of dihydromyricetin-carried ternary complex liposome
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  • Preparation method of dihydromyricetin-carried ternary complex liposome

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Embodiment 1

[0022] A preparation method of dihydromyricetin-loaded ternary composite liposomes, comprising the following steps:

[0023] (1) Dissolve dihydromyricetin, phosphatidylglycerol (PG) and dioleoylphosphatidylethanolamine (DOPE) in chloroform at a molar ratio of 2:3:3, evaporate under reduced pressure to remove chloroform, and obtain dry lipid Membrane, add HEPES buffer (pH7.4), shake slowly to suspend the lipid film in HEPES buffer to obtain anionic liposome suspension, put the anionic liposome suspension in an ultrasonic cleaner for Ultrasound in a water bath, fully hydrated, and squeezed through the membrane to obtain anionic liposomes;

[0024] (2) Dissolve trimethyl-2,3-dioleoyloxypropylammonium bromide (DOTAP) and phosphatidylcholine (PC) in chloroform at a molar ratio of 1:1, and evaporate under reduced pressure to remove chloroform , to obtain a uniform film, add HEPES buffer (pH7.4), slow shaking makes the lipid film suspended in HEPES buffer, to obtain cationic liposom...

Embodiment 2

[0027] A preparation method of dihydromyricetin-loaded ternary composite liposome, said method comprising the following steps:

[0028] (1) Dissolve dihydromyricetin, phosphatidylinositol (PI) and cholesterol (CHOL) in chloroform at a molar ratio of 2.5:3.5:3.5, evaporate under reduced pressure to remove chloroform, obtain a dry lipid film, and add HEPES Buffer solution (pH7.4), shake slowly to suspend the lipid film in the HEPES buffer solution to obtain anionic liposome suspension, place the anionic liposome suspension in an ultrasonic cleaner for ultrasonic cleaning in a water bath, fully After hydration, squeeze through the membrane to obtain anionic liposomes;

[0029] (2) Dissolve 1,2-dioleoyl-3-succinyl-sn-glycerol choline ester (DOSC) and dioleoylphosphatidylethanolamine (DOPE) in chloroform at a molar ratio of 1:0.8, and decompress Evaporate and remove chloroform to obtain a uniform film, add HEPES buffer (pH7.4), slowly shake to suspend the lipid film in HEPES buffe...

Embodiment 3

[0032] A preparation method of dihydromyricetin-loaded ternary composite liposome, said method comprising the following steps:

[0033](1) Dissolve dihydromyricetin, phosphatidylserine (PS) and dioleoylphosphatidylethanolamine (DOPE) in chloroform at a molar ratio of 2.8:4:3, evaporate under reduced pressure to remove chloroform, and obtain dry lipid Membrane, add a certain volume of HEPES buffer (pH7.4), shake slowly to suspend the lipid film in HEPES buffer to obtain anionic liposome suspension, put the anionic liposome suspension in ultrasonic cleaning Ultrasound in a water bath in the instrument, after fully hydrating, squeeze through the membrane to obtain anionic liposomes;

[0034] (2) Dissolve trimethyl-2,3-dioleyloxypropyl ammonium chloride (DOTMA) and phosphatidylcholine (PC) in chloroform at a molar ratio of 1.2:1, and evaporate under reduced pressure to remove chloroform , to obtain a uniform film, add HEPES buffer (pH7.4), slow shaking makes the lipid film suspen...

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Abstract

The invention provides a preparation method of dihydromyricetin-carried ternary complex liposome. The preparation method comprises the following steps: (1) preparing an anion liposome ; (2) preparing an anion-cation binary complex liposome suspension; (3) preparing dihydromyricetin ternary complex liposome. According to the dihydromyricetin-carried ternary complex liposome prepared by a layer-by-layer self-assembly technology provided by the invention, an ultrathin membrane is formed by the alternating deposition of substances with opposite charges on a liquid solid interface through an electrostatic interaction, and a brand new multi-layer self-assmebling system: 'anion lipid-cation lipid-carboxymethyl chitosan' is put forward. The ternary complex liposome, of which the particle diameter of is 204.8+ / -6.2nm and the potential is -8.1+ / -2.5mV after the completion of the assembly, has a significant laminated structure and good stability in a plasma; furthermore, the cytotoxicity is less than cationic liposome; meanwhile, the ternary complex liposome has a pH sensitivity, and is capable of selectively releasing dihydromyricetin in different mediums.

Description

technical field [0001] The invention relates to the technical field of dihydromyricetin, in particular to a method for preparing a dihydromyricetin-loaded ternary composite liposome. Background technique [0002] Ampelopsis grossedentata, commonly known as vine tea, is a new food raw material announced by the National Health and Family Planning Commission. Dihydromyricetin, a polyphenolic hydroxyflavonol, is the main active ingredient in S. dentatus grapes. Medical research shows that dihydromyricetin has a wide range of pharmacological effects, such as anti-tumor, anti-thrombotic, anti-bacterial, lowering blood sugar, lowering blood pressure, protecting liver and liver, and alleviating ethanol poisoning. However, due to the disadvantages of dihydromyricetin itself such as poor fat solubility, easy oxidation and degradation, this greatly limits its application in industries such as medicine and food. If the dihydromyricetin is loaded with a safe and efficient drug carrier ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/352A61K47/36A61K47/24A61K47/18A61P35/00A61P7/02A61P31/04A61P3/10A61P9/12A61P1/16A61P39/02
Inventor 熊伟李雄辉王慧宾付建平胡居吾朱仁果韩晓丹
Owner INST OF APPLIED CHEM JIANGXI ACAD OF SCI
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