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Oral colon-targeted lycopene nano-liposome and preparation method thereof

A technology of nano-liposome and lycopene, which is applied in the field of pharmacy, can solve the problems of unsatisfactory colon-targeted drug release, poor mechanical properties, and structural damage, and achieve obvious colon-targeted release effect and stability Improve and reduce the damage effect

Inactive Publication Date: 2020-06-23
JIANGXI SCI & TECH NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Currently common OCDDS formulations include pellets, microspheres, hydrogels, etc., but these carriers have the following disadvantages: 1) The particle size is large, the contact area with the digestive juice is small, the degradation rate in the colon is slow, and the embedding low bioavailability; 2) Lack of a solid core, mostly in a loose state, poor mechanical properties, susceptible to structural damage caused by gastrointestinal peristalsis, early release of embeddings, and unsatisfactory colon-localized drug release effect
However, lycopene is extremely sensitive to the external environment, prone to degradation and isomerization, and loses physiological activity; poor water solubility, direct oral administration, low bioavailability
In order to solve the above problems, some researchers have used some traditional dosage forms (ordinary liposomes, microcapsules, microspheres, emulsions) to embed and protect them, but these dosage forms have poor gastrointestinal tract stability and unsatisfactory targeting. and other defects

Method used

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  • Oral colon-targeted lycopene nano-liposome and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 0.5g egg yolk lecithin, 0.1g cholesterol and completely dissolve in 50mL of anhydrous ether, another 20mg of lycopene is completely dissolved in 10mL of dichloromethane, mix the above two solutions, slowly inject into 200mL, pH7 .0, in a phosphate buffer solution with a concentration of 0.02M / L, magnetically stirred at 45°C for 20min, then transferred to a round-bottomed flask, removed anhydrous ether and dichloromethane by vacuum rotary evaporation, and heated at 150MPa Circulate the homogeneous treatment twice under pressure to obtain lycopene conventional liposomes; inject the lycopene conventional liposome solution into 200mL, 0.25% chitosan acetic acid solution (0.2% concentration of acetic acid solution), and stir to react After 20 minutes, continuous ultrasonic treatment was performed for 20 minutes to obtain chitosan-modified liposomes. Then add chitosan-modified nano-liposomes into 600mL, 0.35% pectin phosphate solution drop by drop while stirring, after ...

Embodiment 2

[0030] Weigh 0.31g of lecithin, 0.03g of cholesterol and completely dissolve in 40mL of anhydrous ether, another 10mg of lycopene is completely dissolved in 5mL of dichloromethane, mix the above two solutions, slowly inject into 300ml of pH6.8 , concentration of 0.02M phosphate buffer solution, magnetically stirred at 45°C for 20min, then transferred to a round-bottom flask, vacuum rotary evaporation to remove anhydrous ether and dichloromethane, and intermittent ultrasonication at 250w for 5min to obtain Lycopene conventional liposomes; the lycopene conventional liposome solution was added dropwise to 300mL, 0.3% chitosan acetic acid solution (0.1% concentration of acetic acid solution), stirred and reacted for 20min, and then ultrasonically treated continuously for 20min, Chitosan-modified liposomes were obtained. Add the chitosan-modified liposome dropwise to 400mL, 0.4% pectin phosphate solution (phosphate solution pH 6.8, concentration 0.02M) while stirring, stir for 20mi...

Embodiment 3

[0032] Weigh 10g of lecithin, 4.16g of cholesterol and completely dissolve in 300mL of anhydrous ether, another 100mg of lycopene is completely dissolved in 50mL of dichloromethane, mix the above two solutions, slowly inject into 350mL of pH6.8, concentration In a 0.2M phosphate buffer solution, stir magnetically at 45°C for 20min, then transfer it to a round-bottom flask, remove anhydrous ether and dichloromethane by vacuum rotary evaporation, and then circulate and homogenize at 150MPa for 3 The conventional liposome of lycopene was obtained; the conventional liposome solution of lycopene was added dropwise to 300mL, 4% chitosan acetic acid solution (0.1% concentration of acetic acid solution), and after stirring for 20min, continuous ultrasonic Treated for 20 minutes to obtain chitosan-modified liposomes. Add the chitosan-modified liposome dropwise to 350mL, 2.2% pectin phosphate solution (phosphate solution pH 6.8, concentration 0.2M) while stirring, stir for 20min, and ci...

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Abstract

The invention relates to the technical field of pharmaceutics, and specifically relates to an oral colon-targeted lycopene nano-liposome and a preparation method thereof. The nano-liposome consists ofa liposome core and a modified layer shell; the liposome core is the lycopene-loaded liposome with negative charge prepared by adopting an ether injection method; and the modified layer shell is formed by a colon-specific degradation material. Compared with conventional lipids, the stability of the obtained nano-liposome in gastrointestinal tracts can be greatly enhanced; and the nano-liposome has obvious colon-targeted release effects and can obviously enhance the repair efficiency of colon parts, and the average particle size is about 560 nm.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to an oral colon-targeting lycopene nanoliposome and a preparation method thereof. Background technique [0002] The colon is an important digestive part of the human body and has functions such as absorbing water and electrolytes. In recent years, due to the improvement of people's living standards and changes in lifestyle and eating habits, the incidence of colon diseases (colon cancer, colitis, etc.) has gradually increased. With the continuous improvement and development of pharmacy, the research and development of oral colon-specific drug delivery system (OCDDS) has become a research hotspot. OCDDS is a kind of drug designed according to the special digestive environment (pH, metabolic enzymes, peristaltic speed) of the colon through certain pharmaceutical methods, so that the drug will not be released in the upper gastrointestinal tract after oral administration, but will st...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/01A61K47/61A61P39/06A61P37/04A61P29/00A61P35/00B82Y5/00B82Y40/00
CPCA61K31/01A61K47/61A61K47/6911A61K9/0056A61P39/06A61P37/04A61P29/00A61P35/00B82Y5/00B82Y40/00
Inventor 白春清赵利郑景霞袁美兰陈丽丽江勇刘华
Owner JIANGXI SCI & TECH NORMAL UNIV
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