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Celastrol flexible liposome, gel and preparation method thereof

A technology of tripteryglide and flexible liposomes, which is applied in liposome delivery, liquid delivery, pharmaceutical formulations, etc., can solve the problem of strong irritation of excipients, complicated preparation process, and encapsulation efficiency of tripteryglide liposomes. Unsatisfactory and other problems, to achieve the ideal effect of promoting healing, good effect, particle size and encapsulation efficiency

Pending Publication Date: 2017-09-12
THE 118 CLINIC DIV OF THE NO 113 HOSPITAL OF CHINESE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Existing tripteryne liposome drugs have complex preparation process, use a wide variety of excipients, some of the excipients are highly irritating, and the prepared tripteryne liposomes have the defects that the encapsulation efficiency is not ideal.

Method used

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  • Celastrol flexible liposome, gel and preparation method thereof
  • Celastrol flexible liposome, gel and preparation method thereof
  • Celastrol flexible liposome, gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The main experimental instruments and reagents are as follows:

[0041] High performance liquid chromatography: Agilent Technologies Co., Ltd.

[0042] Ultrasonic cell disruptor: Scientz-750F, Ningbo Xinzhi Biotechnology Co., Ltd.

[0043] Laser particle size analyzer: Nano-ZS, Malvern Instruments Ltd., UK

[0044] Transdermal Absorption Apparatus: HC-188, Tianjin Zhengtong Technology Co., Ltd.

[0045] Ready-to-use dialysis bags (10K MWCO): ThermoFisher Scientific Inc.

[0046] High-purity egg yolk lecithin (PC-98T): Shanghai Evert Pharmaceutical Technology Co., Ltd.

[0047] High-purity cholesterol: Shanghai Everett Pharmaceutical Technology Co., Ltd.

[0048] Sodium cholate: Sinopharm Chemical Reagent Co., Ltd.

[0049] Chloroform, methanol, ethanol: Sinopharm Chemical Reagent Co., Ltd.

[0050] Tween 80: Sinopharm Chemical Reagent Co., Ltd.

[0051] Carbomer: The Lubrizol Corporation of America

[0052] Tripterygium: Aktin Chemicals, Inc.

[0053] Nano silv...

Embodiment 2

[0059] Precisely weigh 0.2g egg yolk lecithin, 0.05g cholesterol and 0.01g tripterine into a pear-shaped bottle, add 2ml ethanol, fully dissolve and shake well, remove the organic solvent by rotary evaporation at 40°C and 10rpm, add 5ml Sodium cholate solution (3mg / ml), fully hydrated, and ultrasonicated 10 times in an ice bath (120w, working for 2s, with an interval of 2s), to obtain 5ml of tripterine flexible liposome suspension. The average particle diameter of the obtained tripterylide flexible liposome is 110.2nm, the PDI is 0.226, the Zeta potential is -32.6mV, the encapsulation efficiency is 99.7%, and the drug loading capacity of the liposome is 4.2%. After being placed in a refrigerator at 4°C for 2 weeks, there was no significant change in the particle size and encapsulation efficiency, indicating that the liposome has good physical stability.

[0060] Accurately weigh carbomer solid 0.1g, join in 4.495ml nano-silver solution (100 μ g / ml), stir and dissolve, add 0.40...

Embodiment 3

[0062] Accurately weigh 0.2g egg yolk lecithin, 0.05g cholesterol and 0.01g tripterine into a pear-shaped bottle, add 2ml chloroform, fully dissolve and shake well, remove the organic solvent by rotary evaporation at 40°C and 10rpm, add 5ml Sodium cholate solution (2mg / ml), fully hydrated, and ultrasonicated 10 times in an ice bath (280w, working for 2s, with an interval of 2s), to obtain 5ml of tripterine flexible liposome suspension. The average particle diameter is 114.8nm, the PDI is 0.230, the Zeta potential is -33.1mV, the encapsulation efficiency is 99.8%, and the drug loading capacity of the liposome is 4.3%. After being placed in a refrigerator at 4°C for 2 weeks, there was no significant change in the particle size and encapsulation efficiency, indicating that the liposome has good physical stability.

[0063] Accurately weigh carbomer solid 0.025g, join in 4.57ml nano-silver solution (120 μ g / ml), stir and dissolve, add 0.405ml pure water, 5ml tripterine liposome su...

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses celastrol flexible liposome which is composed of 1 part of celastrol, 1-4 parts of sodium cholate, 2-10 parts of cholesterol and 15-40 parts of egg yolk lecithin. The invention further provides a preparation method of celastrol flexible liposome, compound celastrol flexible liposome gel and a preparation method thereof. The celastrol flexible liposome obtained by the preparation method is ideal in production process operation, safety, particle size and encapsulation rate and high in physical stability; an obtained celastrol flexible liposome suspension can be directly used for preparing the compound celastrol flexible liposome gel without going through steps of separation and purification. In addition, the compound celastrol flexible liposome gel obtained by the preparation method has good heal promoting effect on rat scald wounds.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to tripterine flexible liposome, gel and preparation method thereof. Background technique [0002] Celastrol is a pentacyclic triterpene quinone compound isolated and purified from Triperygium Wilfordii Hook f. Tripteryglide is insoluble in water, but easily soluble in dimethyl sulfoxide, chloroform, acetone and ether. It has strong immune response suppression, anti-inflammatory and anti-cancer effects, and can be used for a variety of autoimmune, chronic inflammatory diseases and cancer treatments, including psoriasis, atopic dermatitis, skin cancer, breast cancer, systemic lupus erythematosus and chronic rheumatoid arthritis. Although tripteryglide has good effects on inhibiting immune response, anti-inflammation and anti-cancer, tripterygne is insoluble in water, poorly absorbed from the gastrointestinal tract when taken orally, and tripterygne is highly toxic, and or...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/06A61K47/28A61K47/24A61K31/56A61P17/02
Inventor 胡永胜卓阳周雪雪黄益灯施雯宇叶胜捷
Owner THE 118 CLINIC DIV OF THE NO 113 HOSPITAL OF CHINESE PEOPLES LIBERATION ARMY
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