Triptolide mitochondrial targeting liposome and application thereof

A technology of triptolide and targeting liposomes, applied in the field of medicine, can solve problems such as no public reports, and achieve the effects of remarkable economic and social benefits, scientific and reasonable compatibility, and easy preparation method

Active Publication Date: 2022-02-15
安徽京和生物药业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mitochondrial targeting molecule (SS), which is modified to the surface of triptolide liposomes, makes triptolide liposomes have mitochondrial targeting, whic...

Method used

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  • Triptolide mitochondrial targeting liposome and application thereof
  • Triptolide mitochondrial targeting liposome and application thereof
  • Triptolide mitochondrial targeting liposome and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A kind of triptolide mitochondria targeting liposome of the present invention:

[0038] 1) Dissolution of raw materials:

[0039] Dissolve 1 mg of the anticancer drug triptolide, 5 mg of targeting carrier, 10 mg of lecithin and 1 mg of polyethylene glycol (PEG) in 22 mL of organic solvent dichloromethane, and sonicate until completely dissolved at an ultrasonic power of 300w;

[0040] 2) Mixing:

[0041] Mix the solutions obtained by dissolving in step 1) together, mix well to obtain a mixed solution, and remove the organic solvent by rotary evaporation at 20 r / min at 40°C to obtain a thin film formed on the wall of the vessel;

[0042] 3) Drying and hydration:

[0043] Put the film in a vacuum drying oven at 40°C to dry for 2 hours, further remove the organic solvent, add 5 mL of hydration solvent deionized sterile water to dissolve, and hydrate with magnetic stirring at a temperature of 65°C for 2 hours to obtain a hydrate;

[0044] 4) Ultrasonicate the hydrate obtai...

Embodiment 2

[0046] A kind of triptolide mitochondria targeting liposome of the present invention:

[0047] 1) Dissolution of raw materials:

[0048] Dissolve 1mg of anticancer drug triptolide, 10mg of targeting carrier, 1mg of lecithin and 1.0mg of polyethylene glycol in 25mL of organic solvent ethanol, and ultrasonicate until completely dissolved at an ultrasonic power of 200w;

[0049] 2) Mixing:

[0050] Mix the solutions obtained by dissolving in step 1) together, mix well to obtain a mixed solution, and remove the organic solvent by rotary evaporation at 20 r / min at 40°C to obtain a thin film formed on the wall of the vessel;

[0051] 3) Drying and hydration:

[0052] Put the film in a vacuum drying oven to dry at 40°C for 2 hours, further remove the organic solvent, add 6 mL of a hydration solvent with a mass concentration of 0.9% sodium chloride aqueous solution to dissolve, and hydrate with magnetic stirring at a temperature of 35°C for 5 hours to obtain a hydrate;

[0053] 4) ...

Embodiment 3

[0055] A kind of triptolide mitochondria targeting liposome of the present invention:

[0056] 1) Dissolution of raw materials:

[0057] Dissolve the anticancer drug triptolide 1 mg, targeting carrier 2.0 mg, lecithin 10 mg and polyethylene glycol 10 mg in 27 mL of organic solvent dimethyl sulfoxide, and ultrasonicate until completely dissolved at an ultrasonic power of 400w;

[0058] 2) Mixing:

[0059] Mix the solutions obtained by dissolving in step 1) together, mix well to obtain a mixed solution, and remove the organic solvent by rotary evaporation at 20 r / min at 40°C to obtain a thin film formed on the wall of the vessel;

[0060] 3) Drying and hydration:

[0061] Put the film in a vacuum drying oven at 40°C to dry for 2 hours, further remove the organic solvent, add 4 mL of hydration solvent phosphate buffer to dissolve, and hydrate with magnetic stirring at a temperature of 70°C for 1.5 hours to obtain a hydrate;

[0062] 4) Ultrasonicate the hydrate obtained in ste...

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Abstract

The invention relates to a preparation method and application of triptolide mitochondrial targeting liposome, which can effectively solve the problems of improving the anti-cancer curative effect of triptolide and reducing toxicity, and the method comprises the following steps: respectively dissolving an anti-cancer drug, a targeting carrier, lecithin and polyethylene glycol by using an organic solvent, uniformly mixing the solutions obtained by respectively dissolving, and carrying out rotary evaporation to remove the organic solvent to obtain a film formed on the vessel wall; drying the film in a vacuum drying oven, further removing the organic solvent, adding a hydration solvent for dissolution, and magnetically stirring for hydration to obtain a hydrate; and carrying out ultrasonic treatment on the hydrate, and extruding and crushing the hydrate through a polycarbonate film with the pore diameter of 1.0-0.1 mu m to obtain the triptolide mitochondrial targeting liposome. According to the present invention, the component compatibility is scientific and reasonable, the preparation method is easy to operate, and the carried positive charges are easily enriched in mitochondria so as to achieve the mitochondrial targeting drug delivery effect, such that the mitochondrial targeting liposome preparation is the innovation of the liposome mitochondrial targeting preparation, and the new way of the tumor treatment drug is developed.

Description

technical field [0001] The invention relates to medicine, in particular to a triptolide mitochondrial targeting liposome and its application. Background technique [0002] The mitochondrial space has a large number of positive charges and its matrix has a large number of negative charges, thus forming the transmembrane potential (MTP) of the mitochondrial inner membrane. MTP is negative inside and positive outside. In normal cells of the body, its value is -130mV to 150mV. When lipophilic cations (DLC) are enriched in mitochondria and the potential balance between the inside and outside of the mitochondrial membrane is reached, they will accumulate in the mitochondria. The mitochondrial membrane potential of tumor cells is often higher than that of normal cells. Therefore, directly linking lipophilic cations to small molecules through covalent bonds can only rely on electrostatic adsorption without penetrating the mitochondrial membrane through complicated mechanisms, and th...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/585A61K47/18A61P1/16A61P13/12A61P35/00A61P35/02A61P39/00C07D207/16
CPCA61K31/585A61K9/1277A61K47/186A61P35/00A61P35/02A61P39/00A61P1/16A61P13/12C07D207/16
Inventor 曾华辉谭晓柯张振强朱鑫刘斌张婷婷武香香
Owner 安徽京和生物药业科技有限公司
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