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Baicalin lipidosome and application thereof

A technology of baicalin and baicalin, which is applied in the field of pharmaceutical preparations, can solve the problems of accelerated liposome degradation, easy precipitation, liposome instability, etc., and achieve the effects of increasing elasticity, uniform particle size, and improving stability

Active Publication Date: 2020-04-24
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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  • Baicalin lipidosome and application thereof
  • Baicalin lipidosome and application thereof
  • Baicalin lipidosome and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation of embodiment 1 baicalin liposome I of the present invention

[0048] Precisely weigh 200mg of phospholipids, 20mg of cholesterol and 20mg of ceramides and place them in a 500mL round bottom flask at the same time, add 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

[0049] The preparation of embodiment 2 baicalin liposome II of the present invention

[0050] 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

[0051] Embodiment 3 The preparation of baicalin liposome III of the present invention

[0052] 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 Take 1ml of aqueous solution (20mg / ml, pH6.5-7.5), and stir in a water bath at 40°C for 20 minutes to obtain baicalin liposome III.

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Abstract

The invention discloses baicalin lipidosome which comprises baicalin, ceramide and a lipid material. The baicalin serves as a medicine component, ceramide serves as one of the medicine component and the lipid material component at the same time, and the baicalin lipidosome is prepared through an active drug loading method. Active encapsulation formation of baicalin lipidosome is catalyzed throughpH difference, and the problem that baicalin has poor stability and poor solubility and is difficult to use independently to achieve the curative effect is solved; meanwhile, the problem that baicalinlipidosome has low encapsulation efficiency and ceramide has poor stability is solved, and the application range of baicalin is widened and the use mode of baicalin is expanded. The baicalin lipidosome disclosed by the invention has the effects of moisturizing and resisting oxidation, and can be used as an active part to be applied to 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 Applications(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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