Glycyrrhetinic acid-modified multifunctional ethosome loaded with curcumin and its preparation method and application

A technology containing curcumin alcohol and glycyrrhetinic acid, applied in the field of medicine, can solve the problems of low transdermal penetration efficiency, abnormal thickening of keratin, difficult active ingredients, etc., and achieves enhanced transdermal penetration efficiency, obvious antioxidant effect, and preparation simple method effect

Active Publication Date: 2022-03-11
SHANGHAI UNIV OF T C M
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

However, psoriasis often has pathological features such as abnormally thickened keratin and scaly epidermis. The clinical application of traditional Chinese medicine external treatment is often hindered by traditional dosage forms, making it difficult for the active ingredients to exert curative effect through the skin barrier.
In addition, curcumin is insoluble in water, has poor solubility, short biological half-life, low transdermal penetration efficiency, and a large polarity difference with glycyrrhetinic acid, which makes it difficult for the combined administration of curcumin and glycyrrhetinic acid to penetrate the skin at the same time The stratum corneum plays a synergistic role

Method used

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  • Glycyrrhetinic acid-modified multifunctional ethosome loaded with curcumin and its preparation method and application
  • Glycyrrhetinic acid-modified multifunctional ethosome loaded with curcumin and its preparation method and application
  • Glycyrrhetinic acid-modified multifunctional ethosome loaded with curcumin and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation of glycyrrhetic acid-modified curcumin-loaded multifunctional alcohol plastids (Cur@GA-TPGS-ES)

[0039] 1.1. Synthesis of glycyrrhetic acid modification (GA-TPGS):

[0040] Weigh 1.51g of TPGS (vitamin E polyethylene glycol succinate) and 0.81g of CDI (carbonyldiimidazole), dissolve them in 5mL of dioxane solution by ultrasonic, activate in a water bath at 37°C for 14 hours, and the activation ends Then, the obtained activation solution was directly added to 150 mL of pre-frozen ether for cooling and crystallization, suction filtration, and the obtained crystals were washed three times with deionized water, and then vacuum-dried for 12 hours to obtain activated TPGS;

[0041] The obtained activated TPGS and ethylenediamine were dissolved in 5mL of DMSO at a molar ratio of 1:5, and at room temperature, 500rpm was magnetically stirred for 24 hours. After the reaction, the reaction solution was added to the dialysis bag (molecular weight cut-off was 1...

Embodiment 2

[0046] Example 2: Evaluation and Characterization of Cur@GA-TPGS-ES

[0047] 2.1. TEM observation of Cur@GA-TPGS-ES

[0048] Disperse Cur@GA-TPGS-ES in an appropriate amount of deionized water, add an appropriate amount dropwise to the copper mesh to dry naturally, and form a thin film after about 20 minutes, and then add 2% phosphotungstic acid for negative dyeing for 10 minutes, and put it in the air to dry. Observed under a transmission electron microscope, the results are as follows figure 2 shown.

[0049] figure 2 is the TEM image of Cur@GA-TPGS-ES, from figure 2 It can be seen that the vesicles in Cur@GA-TPGS-ES are approximately spherical or ellipsoid, and the vesicles are uniform in size and round.

[0050] 2.2. Determination of particle size and drug loading

[0051] The prepared Cur@GA-TPGS-ES was diluted with an appropriate amount of deionized water, and the particle size was measured by a Malvern nano-ZS90 particle size analyzer. The result was that the pa...

Embodiment 3

[0058] Example 3: In vitro percutaneous penetration test

[0059] Twelve male rats were randomly divided into 2 groups with 6 rats in each group. After ether inhalation anesthesia, the abdominal hair was carefully shaved with an electric shaver, and then sacrificed by cervical vertebrae. The abdominal skin was quickly peeled off and the subcutaneous fat and adhesions were removed. Rinse repeatedly with normal saline and use it immediately; use a modified vertical Franz transdermal diffusion cell (the effective administration area is about 2.0cm 2 , the volume of the receiving tank is about 12.5mL), the treated skin is fixed at the connection between the supply tank and the receiving tank, the stratum corneum faces the supply tank, and the dermis is connected to the receiving tank; 10% ethanol and 20% polyamide are injected into the receiving tank. The PBS mixed solution of ethylene glycol 400 was used as the receiving solution, the air bubbles were removed, and 1 mL of Cur@GA-...

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Abstract

The invention discloses a curcumin-loaded multifunctional ethosome modified by glycyrrhetinic acid and its preparation method and application. The inner plastid is the inner core, and the glycyrrhetinic acid modification is the outer shell. The multifunctional ethosome of the present invention can effectively deliver curcumin and glycyrrhetinic acid to the skin, can enhance the percutaneous penetration efficiency of drugs in vivo and in vitro, and fully utilize curcumin, glycyrrhetinic acid and vitamin E polyethylene glycol succinate The synergistic anti-psoriasis effect of acid esters can not only significantly improve the inflammatory symptoms of psoriasis, but also produce obvious antioxidant effects, which can effectively reduce the damage of lipid peroxidation mediated by psoriasis and increase the local application of drugs It is expected to be used in the preparation of pharmaceutical preparations for anti-inflammation, anti-oxidation and / or skin repair, especially for the preparation of pharmaceutical preparations for the treatment of psoriasis, and has a medicinal prospect.

Description

technical field [0001] The invention relates to a curcumin-loaded multifunctional alcohol plastid modified with glycyrrhetinic acid and a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Psoriasis is a multi-factor-related inflammatory skin disease. Its clinical manifestations are abnormal proliferation and inflammatory infiltration of the epidermis, resulting in damage to the skin and various organs. At present, the clinical treatment of mild to moderate psoriasis is mainly based on the topical application of corticosteroids and other drugs, but long-term application of corticosteroids has different degrees of adverse reactions and cannot improve the trend of inflammatory recurrence in patients. [0003] Since psoriasis occurs on the skin, the external treatment of traditional Chinese medicine can directly play a local therapeutic effect on the disease and reduce systemic side effects. The transdermal ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/22A61K31/56A61K31/12A61P17/06A61P29/00A61P39/06C08G65/332C08G65/333
CPCA61K9/127A61K9/1277A61K47/22A61K9/0014A61K31/56A61K31/12A61P17/06A61P29/00A61P39/06C08G65/3324C08G65/33306A61K2300/00
Inventor 郭腾冯年平朱春赟刘卫范蕴隆卢键滢
Owner SHANGHAI UNIV OF T C M
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