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Anti-inflammatory liposome having targeting effect and preparation method and application thereof

A liposome-acting technology, applied in the field of medicine, can solve the problems of low encapsulation rate, inability to target inflammatory sites, low drug utilization rate, etc. Effect

Active Publication Date: 2019-09-06
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The invention solves the technical problems in the prior art that the anti-inflammatory drugs entrapped in liposomes cannot target the inflammatory site, the encapsulation rate is low, and the drug utilization rate is low

Method used

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  • Anti-inflammatory liposome having targeting effect and preparation method and application thereof
  • Anti-inflammatory liposome having targeting effect and preparation method and application thereof
  • Anti-inflammatory liposome having targeting effect and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: Preparation of oxymatrine-NO liposome

[0051] Comparing different liposome preparation methods, it is determined by the drug entrapment rate that the best entrapment method for oxymatrine is the pH gradient method, and the best drug-to-lipid ratio is 1:10 (anti-inflammatory drugs and phospholipids, cholesterol, negative The ratio of the sum of charged amphiphilic molecules and nitric oxide donor molecules), the optimal formula ratio is soybean lecithin, cholesterol, DSPE-PEG and nitric oxide donor molecules (TNO 3 ) The mass ratio is 4:1:1:0.5.

[0052] 1) Preparation of oxymatrine-NO liposomes

[0053] Weigh soybean lecithin 33.2mg, cholesterol 8.3mg, distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) 8.3mg and TNO 3 4.1 mg, TNO 3 The molecular formula is as follows:

[0054]

[0055] Dissolve the above materials together in 4 mL of dichloromethane, place in a round-bottomed flask, spin dry the solvent under reduced pressur...

Embodiment 2

[0056] Embodiment 2: the preparation of oxymatrine-NO liposome

[0057] Weigh respectively soybean lecithin 66.4mg, cholesterol 8.3mg, distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) 8.3mg and TNO 3 4.1mg, dissolve the above materials together in 4mL of dichloromethane, place in a round-bottomed flask, spin dry the solvent under reduced pressure at 25°C, and then place it in a vacuum drying oven for 30 minutes; pour into the dried film Add 3 mL of sodium citrate buffer solution with pH 5.0, sonicate at 110W for 30 minutes until fully hydrated, then disperse three times with an aqueous filter membrane with a pore size of 0.35um to obtain blank liposomes; adjust the blank with saturated dipotassium hydrogen phosphate solution The pH of the liposome solution was 7.2, and 5 mg of oxymatrine drug was added to the blank liposome; the above solution was incubated in a shaker at 55°C for 1.5 h; The oxymatrine drug was changed every half an hour for a total ...

Embodiment 3

[0058] Embodiment 3: the preparation of oxymatrine-NO liposome

[0059] Weigh soybean lecithin 33.2mg, cholesterol 16.6mg, distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) 16.6mg and TNO 3 4.1mg, dissolve the above materials together in 4mL of dichloromethane, place in a round-bottomed flask, spin dry the solvent under reduced pressure at 25°C, and then place it in a vacuum drying oven for 30 minutes; pour into the dried film Add 3 mL of sodium citrate buffer solution with a pH of 5.0, sonicate at 120W for 30 minutes until fully hydrated, and then disperse three times with an aqueous filter membrane with a pore size of 0.45um to obtain blank liposomes; adjust the blank with saturated dipotassium hydrogen phosphate solution The pH value of the liposome solution was 7.4, and 5 mg of oxymatrine drug was added to the blank liposome; the above solution was incubated in a shaker at 60°C for 2 hours; after the incubation was completed, the free phase was dia...

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Abstract

The invention discloses anti-inflammatory liposome having targeting effect and a preparation method and application thereof and belongs to the technical field of medicine. The liposome is of a phospholipid bimolecular layer structure, cholesterol, amphipathic molecules with negative charge and nitric oxide donor molecules are embedded in the phospholipid bimolecular layer structure, cholesterol isused for enhancing stability of the phospholipid bimolecular layer structure, the amphipathic molecules are used for enabling the liposome to have targeting effect, the nitric oxide donor molecules are used for releasing nitric oxide, and an anti-inflammatory active ingredient is embedded in a hydrophilic cavity of the phospholipid bimolecular layer structure. The preparation method includes: adopting a hydration method to obtain blank liposome, and adopting a pH gradient method to entrap the anti-inflammatory active ingredient. The liposome prepared by the method can give synergistic effectof the anti-inflammatory active ingredient and NO into play, improve drug distribution, target colon parts and improve treatment effect of ulcerative colitis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an anti-inflammatory liposome with targeting effect and its preparation and application, in particular to an anti-inflammatory liposome with NO release function, which can passively target the inflammatory colon and exert anti-inflammatory effect. Liposomes. Background technique [0002] Alkaloids are a type of nitrogen-containing basic organic compounds that exist in nature (mainly plants, but some also exist in animals), and have alkali-like properties. Most of them have a complex ring structure, and nitrogen is mostly contained in the ring, which has significant biological activity and is one of the important active ingredients in Chinese herbal medicine. Among them, the representative oxymatrine (Oxymatrine) is a quinolizidine alkaloid isolated from the traditional Chinese medicine Sophora flavescens Ait, which has a wide range of biological activities, such as anti-inflammat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K33/00A61K31/4375A61K31/235A61P29/00A61P1/00
CPCA61K9/1271A61K9/1277A61K31/235A61K31/4375A61K33/00A61K47/24A61K47/28A61P1/00A61P29/00A61K2300/00
Inventor 谭松巍张伟唐庆谭晨张冲
Owner HUAZHONG UNIV OF SCI & TECH
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