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
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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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