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Preparation method of mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticle

A technology of oleanolic acid and mitochondria, applied in the field of medicine, can solve the problems of limited clinical application and development, poor water solubility, large differences, etc.

Pending Publication Date: 2020-11-13
HENAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug has poor water solubility, the solubility in water is only 1 μg / mL, poor intestinal mucosal permeability and heavy first-pass effect, resulting in low bioavailability and large inter-individual variability. These properties limit its clinical application and development
At present, the pharmaceutical preparations of oleanolic acid sold in the market are only tablets and capsules. Relevant scholars at home and abroad have carried out research on new formulations of oleanolic acid. Most of the new formulations have complicated preparation processes and low drug loading. High equipment requirements
Moreover, there is a problem of relatively low targeting, which makes the drug curative effect poor and prone to side effects

Method used

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  • Preparation method of mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticle
  • Preparation method of mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticle
  • Preparation method of mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticle

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Embodiment 1

[0027] When the present invention is implemented, the nanoparticles are made of anticancer drugs, targeting carriers, lecithin, cholesterol and deionized sterile water; specifically, accurately weigh 5.0 mg lecithin, 10.0 mg α-TOS- TPP, 5.0 mg oleanolic acid, 5.0 mg cholesterol (1:2:1:1) were respectively dissolved in 100ml of dichloromethane, the above solutions were mixed, and the dichloromethane was removed by rotary evaporation at 20 r / min at 40 °C to obtain The film formed on the vessel wall was vacuum-dried at 40°C for 2 hours, added 5ml of deionized sterile water, hydrated with magnetic stirring at 65°C for 2 hours, ultrasonicated at 250w for 5 minutes, and extruded at 60°C to 0.4μm, 0.2μm, 0.1 μm polycarbonate membrane to obtain mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticles. The particle size is 137.72 nm, the polydispersity coefficient is 0.228, and the surface charge is +43.70 mV.

Embodiment 2

[0029] When the present invention is implemented, the nanoparticles are made of anticancer drugs, targeting carriers, lecithin, cholesterol and deionized sterile water; specifically, accurately weigh 1.0 mg lecithin, 5.0 mg α-TOS- TPP, 1.0 mg oleanolic acid, 1.0 mg cholesterol (1:5:1:1) were respectively dissolved in 25ml ethanol, mixed the above solutions, 20 r / min, 40 ℃ rotary evaporation to remove ethanol, to obtain Vacuum-dried at 40°C for 2 hours, added 6ml of deionized sterile water, hydrated with magnetic stirring at 65°C for 2 hours, ultrasonicated at 250w for 5 minutes, and extruded through 0.4μm, 0.2μm, 0.1μm polycarbonate at 60°C membrane to obtain mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticles. The particle size is 110.12nm, the polydispersity coefficient is 0.218, and the surface charge is +26.26 mV.

Embodiment 3

[0031] When the present invention is implemented, the nanoparticles are made of anticancer drugs, targeting carriers, lecithin, cholesterol and deionized sterile water; specifically, accurately weigh 2.0 mg lecithin, 10.0 mg α-TOS- TPP, 4.0 mg oleanolic acid, 6.0 mg cholesterol (1:5:2:3) were respectively dissolved in 100ml dimethyl sulfoxide, mixed the above solutions, 20 r / min, 40 ℃ rotary evaporation to remove dimethyl sulfoxide to obtain a thin film formed on the wall of the container, vacuum-dried at 40°C for 2 hours, added 4 ml of deionized sterile water, hydrated with magnetic stirring at 65°C for 2 hours, ultrasonicated at 250w for 5 minutes, and squeezed at 60°C 0.4 μm, 0.2 μm, 0.1 μm polycarbonate membranes to obtain mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticles. The particle size is 149.74 nm, the polydispersity coefficient is 0.183, and the surface charge is +27.41 mV.

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Abstract

The invention relates to a preparation method of mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticles. The bioavailability and the targeting property of the medicine can be effectively improved. The technical scheme is as follows: the preparation method comprises the following steps of: respectively dissolving an anti-cancer drug, a targeting carrier, lecithin and cholesterolin an organic solvent until the materials are totally dissolved, mixing the dissolved solutions together, carrying out rotary evaporation to remove the organic solvent to obtain a film formed on the wall, drying the film in a vacuum drying oven, thoroughly removing the organic solvent, adding a hydration solvent, magnetically stirring the hydrated product, carrying out ultrasonic treatment, sequentially passing through polycarbonate films with different pore diameters, and carrying out extrusion crushing to obtain the mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticles. According to the nanoparticle, triphenylphosphine connected to tocopherol is utilized, positive charges carried by triphenylphosphine are easily enriched in mitochondria, so that the effect of mitochondria targeted drug delivery is achieved, and the nanoparticle is an innovation on mitochondria targeted preparations of nanoparticles.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for preparing mitochondria-targeted tocopherol-oleanolic acid double-drug nanoparticles. Background technique [0002] α-tocopheryl succinate (α-TOS) is an esterified derivative of α-tocopherol (α-TOH), the main component of vitamin E. As a natural antioxidant, the antioxidant effect of vitamin E in the body has been recognized. Vitamin E is easily oxidized during storage and application, so its esterified derivatives are often used as commercial supply forms, and α-TOS is one of them. In recent years, studies have found that α-TOS has a wide range of anti-tumor activities in addition to being a supply precursor of vitamin E, and can exert anti-cancer effects through various mechanisms, such as inducing apoptosis, inhibiting the function of nuclear transcription factor KB, and inhibiting angiogenesis. Wait. In addition, α-TOS can selectively kill cancer cells without adverse r...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/55A61K47/69A61K9/14A61K47/28A61K47/24A61K31/355A61K31/56A61P35/00
CPCA61K47/545A61K47/551A61K31/56A61K31/355A61K9/145A61K47/6929A61P35/00A61K2300/00
Inventor 曾华辉谭晓柯朱鑫张振强武香香
Owner HENAN UNIV OF CHINESE MEDICINE
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