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A kind of baicalin liposome and its application

A technology of baicalin and baicalin, which is applied in baicalin liposomes and its application fields, can solve the problems of accelerated liposome degradation, easy precipitation, liposome instability, etc., and achieve increased plasma membrane elasticity and uniform particle size , the effect of improving stability

Active Publication Date: 2021-12-10
BEIJING UNDERPROVED MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since baicalin is almost insoluble in water, during the preparation of baicalin liposomes, baicalin is mainly added as a lipid material in the form of powder and wrapped into a phospholipid bilayer. This liposome is unstable and easy to separate out , to accelerate liposome degradation, and the uniformity and particle size of liposomes are greatly challenged

Method used

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  • A kind of baicalin liposome and its application
  • A kind of baicalin liposome and its application
  • A kind of baicalin liposome and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The preparation of embodiment 1 baicalin liposome I of the present invention

[0049] Accurately weigh 200 mg of phospholipids, 20 mg of cholesterol and 20 mg of ceramide, respectively, and place them in a 500 mL round bottom flask at the same time, add an appropriate amount of ethanol and ultrasonically assist to dissolve them completely. The ethanol was removed by rotary evaporation in a water bath at 50°C, and a light yellow film was formed on the inner wall of the flask. Add 250ml-1000ml of 250mM ammonium sulfate buffer solution, hydrate at 40°C for 20 minutes, and dissolve with the aid of ultrasound; then filter, homogenize the filtrate through a high-pressure homogenizer for 5-15 times, and then use HBS for 24h dialysis, baicalin aqueous solution (5mg / ml, pH6.5-7.5) 1ml, stirred in a 40-degree water bath for 20 minutes to obtain baicalin liposome I.

Embodiment 2

[0050] The preparation of embodiment 2 baicalin liposome II of the present invention

[0051] Precisely weigh 200 mg of phospholipids, 16 mg of cholesterol, 2 mg of triolein, 2 mg of cholesterol oleate, and 20 mg of ceramide into a 500 mL round bottom flask at the same time, and add an appropriate amount of ethanol to assist in ultrasonication to dissolve them completely. The ethanol was removed by rotary evaporation in a water bath at 50°C, and a yellow film was formed on the inner wall of the flask. Add 250ml-1000ml of 250mM ammonium sulfate buffer solution, hydrate in a water bath at 40°C for 20 minutes, and dissolve with the aid of ultrasound; then filter, homogenize the filtrate through a high-pressure homogenizer for 5-15 times, and then use HBS for dialysis for 24 hours, baicalin Take 1ml of aqueous solution (10mg / ml, pH6.5-7.5), stir in a 40-degree water bath for 20 minutes to obtain baicalin liposome II.

Embodiment 3

[0052] Embodiment 3 The preparation of baicalin liposome III of the present invention

[0053] Accurately weigh 200 mg of phospholipids, 14 mg of cholesterol, 2 mg of glyceryl trioleate, 2 mg of medium chain triglycerides, 2 mg of macrogol glycerol oleate and 20 mg of ceramide in a 500 mL round-bottomed flask at the same time. Aids in complete dissolution. The ethanol was removed by rotary evaporation in a water bath at 50°C, and a yellow film was formed on the inner wall of the flask. Add 250ml-1000ml of 250mM ammonium sulfate buffer solution, hydrate in a water bath at 40°C for 20 minutes, and dissolve with the aid of ultrasound; then filter, homogenize the filtrate through a high-pressure homogenizer for 5-15 times, and then use HBS for dialysis for 24 hours, baicalin Aqueous solution (20mg / ml, pH6.5-7.5) 1ml, stirred in 40 degree water bath for 20 minutes to obtain baicalin liposome III.

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Abstract

The invention discloses a baicalin liposome, which comprises baicalin, ceramide and a lipid material. Baicalin is used as a drug component, and ceramide is simultaneously used as a drug component and one of the lipid material components. It is prepared by an active drug loading method. to make. The present invention catalyzes the active encapsulation and formation of baicalin liposomes by pH difference, solves the problems of poor stability and poor solubility of baicalin, and is difficult to exert curative effect when used alone, and overcomes the low encapsulation rate of baicalin liposomes and the The problem of poor amide stability has expanded the application range and usage of baicalin. The baicalin liposome of the invention has the functions of moisturizing and anti-oxidation, and can be used as an active part in cosmetics.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a baicalin liposome and its application. Background technique [0002] Baicalin (Baicalin, BCL) is a flavonoid isolated from the dry root of the dicotyledonous plant Scutellaria baicalensis Georgi, which has significant biological activities, including anti-inflammatory, immune regulation, anti-allergic , anti-tumor, antibacterial, anti-viral, antihypertensive, etc., among which the anti-inflammatory and immune regulation functions are particularly prominent. Baicalin has shown clear anti-inflammatory and immunomodulatory effects on a variety of inflammatory and autoimmune animal models, including: asthma, acute pancreatitis, acute lung injury, liver fibrosis, sun-induced dermatitis, etc. [0003] [0004] Baicalin contains phenolic hydroxyl groups in its structure, which is unstable and susceptible to air oxidation and discoloration. Moreover, baicalin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/7048A61K31/164A61K47/18A61K47/24A61K47/28A61P17/00A61P17/10A61P37/08A61P17/16A61P17/06A61K8/14A61K8/60A61K8/68A61K8/55A61K8/63A61Q19/08A61Q19/00A61Q19/02
CPCA61K9/1277A61K31/7048A61K31/164A61K47/18A61K47/24A61K47/28A61P17/00A61P17/10A61P37/08A61P17/16A61P17/06A61K8/14A61K8/602A61K8/68A61K8/553A61K8/63A61Q19/08A61Q19/00A61Q19/02A61K2800/56A61K2300/00
Inventor 陈勇
Owner BEIJING UNDERPROVED MEDICAL TECH CO LTD
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