Preparation method of long-circulation lipidosome of olive polyphenol extract rich in hydroxytyrosol and verbascoside

Verbacosin oil, a technology rich in hydroxyphenol, is applied in the chemical, pharmaceutical and biological fields, and can solve the problems of limiting olive polyphenols, etc., and achieve the effects of reducing the number of medications, good stability, and uniform particle size distribution

Inactive Publication Date: 2017-08-08
INST OF CHEM IND OF FOREST PROD CHINESE ACAD OF FORESTRY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Literature at home and abroad have reported the extraction and separation of polyphenolic compounds such as oleuropein, hydroxytyrosol, verbascoside and tyrosol from olive leaves or olive fruits, but most of

Method used

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  • Preparation method of long-circulation lipidosome of olive polyphenol extract rich in hydroxytyrosol and verbascoside
  • Preparation method of long-circulation lipidosome of olive polyphenol extract rich in hydroxytyrosol and verbascoside
  • Preparation method of long-circulation lipidosome of olive polyphenol extract rich in hydroxytyrosol and verbascoside

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Preparation of olive polyphenol extract

[0053] Get 1kg of olive leaves, add 30% ethanol 8L to extract, temperature 85 ℃, extraction time 2 hours, extract twice, combine extracts, adopt ceramic membrane (aperture 50nm) and molecular weight 3000Da ultrafiltration membrane to filter respectively, then use nanofiltration membrane Concentrate the filtrate to 1.5L, vacuum-dry the concentrate, and break it into powder to make olive polyphenol extract. HPLC analysis shows that oleuropein is 36.8%, verbascoside is 5.6%, and hydroxytyrosol is 3.4%. The water solubility is dissolved in 100ml water 5.2g.

Embodiment 2

[0055] Preparation of olive polyphenol extract rich in hydroxytyrosol and verbascoside

[0056] Compounding 90% hydroxytyrosol with 36.8% oleuropein extract and 90% verbascoside, the mass ratio is 4-8:2-5:1-3, preferably 4-5:2-3:1-2 , add 4 times of absolute ethanol, heat and reflux at 60°C for 20min, filter the sample after fully dissolving, and concentrate under reduced pressure to prepare olive polyphenol extract rich in hydroxytyrosol and verbascoside, HPLC analysis, wherein hydroxytyrosol is 56%, olive 18% picroside and 7% verbascoside;

[0057] In order to achieve the effect of the long-circulation liposome of the olive polyphenol extract, the present invention adopts a film dispersion-mechanical oscillation method. Rotary evaporation and decompression film forming pressure -0.05~-0.1Mpa, temperature 50~70℃, vacuum freeze drying film forming pressure 2~10Mpa, temperature -10~-50℃, ultrasonic mechanical oscillation power 100~200W, time 20~40min , high-speed shear power ...

Embodiment 3

[0060] Preparation of long-circulating liposomes from olive polyphenol extract rich in hydroxytyrosol and verbascoside

[0061] The encapsulation target is the olive polyphenol extract rich in hydroxytyrosol and verbascoside, the design temperature is 40-70°C, preferably 55°C, the mass ratio of lecithin and cholesterol is 3:1, and the mass of lecithin and cholesterol is 4g, and the surfactant Tween-80 volume 5mL, PEG 200 3.5g, put into a round bottom flask, add acetone, ultrasonic vibration for 10min, dissolve and remove the solvent by vacuum thin film evaporation, rotary evaporation and vacuum film forming pressure -0.05~-0.1Mpa, temperature 50-70°C, vacuum freeze-drying film-forming pressure 2-10Mpa, temperature -10-50°C, ultrasonic mechanical oscillation power 100-200W, time 20-40min, high-speed shear power 500-1000W, time 5-10min. Then add 6 mL of 3 mg / mL hydroxytyrosol (HT) aqueous solution and 2 mL of olive polyphenol extract aqueous solution, rotate the membrane for 15 ...

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Abstract

The invention discloses a preparation method of long-circulation lipidosome of an olive polyphenol extract rich in hydroxytyrosol and verbascoside. Olive leaf is taken as a raw material, and is prepared into an olive polyphenol extract by extracting with 30 to 50 percent of ethanol, separating with a ceramic membrane and an ultrafiltration membrane and concentrating with a nanofiltration membrane; 90 percent of the hydroxytyrosol, 10 to 40 percent of an oleuropein extract and 90 percent of the verbascoside are compounded to prepare the olive polyphenol extract rich in the hydroxytyrosol and the verbascoside; the hydroxytyrosol and verbascoside polyphenol as model materials, lecithin, cholesterol, a Tween-80 surfactant and the like are prepared into the corresponding lipidosome. The lipidosome has the advantages that the bioavailability of the olive polyphenol extract is remarkably increased, and high encapsulation efficiency, uniform particle size distribution, good stability, slow release property, oxidation resistance and an antibacterial effect are achieved. The preparation method is simple and feasible, equipment is simple, and the application of the lipidosome in the medicine field can be widened.

Description

[0001] 1. Technical field [0002] The invention relates to the fields of biology, chemistry and medicine, in particular to a preparation method of hydroxytyrosol liposome. [0003] 2. Background technology [0004] Liposomes are mainly bilayer hollow spheres composed of lipid materials, which have both hydrophilic and hydrophobic properties, so they can encapsulate both fat-soluble substances and water-soluble substances. When the lipid material is dispersed in water, the water-soluble substances will be spontaneously distributed inside the liposome, while the fat-soluble substances will be distributed at the lipophilic end of the liposome. Liposome preparation methods mainly include: film dispersion method, ultrasonic dispersion method, freeze-thaw method, ethanol injection method, reverse phase evaporation method, etc. The evaluation indexes of its physical and chemical properties mainly include: liposome average particle size and particle size distribution, encapsulation e...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K36/63A61K31/7048A61K47/24A61K47/26G01N21/31G01N1/38A61P39/06A61P31/04A61K31/05A61K31/7032
CPCA61K9/0002A61K9/1277A61K31/05A61K31/7032A61K31/7048A61K36/63A61K47/24A61K47/26G01N1/38G01N21/314A61K2300/00Y02A50/30
Inventor 王成章原姣姣李文君刘玉红
Owner INST OF CHEM IND OF FOREST PROD CHINESE ACAD OF FORESTRY
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