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Nanostructure lipid preparation for improving doxorubicin tumor active targeting and kidney protection and preparation method

A nanostructured lipid, active targeting technology, applied in antitumor drugs, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of high nephrotoxicity and poor tumor targeting, etc. Achieve uniform particle size and strong tumor targeting effect

Inactive Publication Date: 2021-03-23
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to overcome the shortcomings of poor tumor targeting and high nephrotoxicity in the prior art, and provide a nanostructured lipid preparation that improves active tumor targeting and renal protection of adriamycin

Method used

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  • Nanostructure lipid preparation for improving doxorubicin tumor active targeting and kidney protection and preparation method
  • Nanostructure lipid preparation for improving doxorubicin tumor active targeting and kidney protection and preparation method
  • Nanostructure lipid preparation for improving doxorubicin tumor active targeting and kidney protection and preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0046] A method for preparing a nanostructured lipid preparation for improving active tumor targeting and renal protection of doxorubicin, comprising the following steps:

[0047] (1) Take salvianolic acid A, doxorubicin hydrochloride and Maize 52 in the ratio of 5:3:300:5000 by mass ratio, dissolve them in deionized water, and make the water phase;

[0048] Take soybean lecithin and distearoyl phosphatidylethanolamine-polyethylene glycol-E-[c(RGDfK) in the ratio of 50:3:1000 by mass ratio 2 ], be dissolved in dehydrated alcohol, make the first solution;

[0049] Take glyceryl behenate and distearoylphosphatidylethanolamine-polyethylene glycol-folic acid in a mass ratio of 30:3:500, and dissolve them in chloroform to make a second solution:

[0050] The volume ratio is 10:1, the first solution and the second solution are combined and stirred evenly to make an oil phase;

[0051] (2) The oil phase is dropped into the water phase, then, the organic solvent is removed by heatin...

Embodiment 2

[0055] A method for preparing a nanostructured lipid preparation for improving active tumor targeting and renal protection of doxorubicin, comprising the following steps:

[0056] (1) Take salvianolic acid A, doxorubicin hydrochloride and poloxamer in a mass ratio of 1:1:100:5000, dissolve them in deionized water, and make an aqueous phase;

[0057] Take dioleoylphosphatidylethanolamine and distearoylphosphatidylethanolamine-polyethylene glycol-E-[c(RGDfK) in a ratio of 20:1:1000 by mass ratio 2 ], be dissolved in dehydrated alcohol, make the first solution;

[0058] Take isopropyl palmitate and distearoylphosphatidylethanolamine-polyethylene glycol-folic acid in a mass ratio of 10:1:500, and dissolve them in chloroform-dimethylsulfoxide (volume ratio 1:1) , making the second solution:

[0059] The volume ratio is 5:1, the first solution and the second solution are combined and stirred evenly to make an oil phase;

[0060] (2) Drop the oil phase into the water phase, then h...

Embodiment 3

[0064] A method for preparing a nanostructured lipid preparation for improving active tumor targeting and renal protection of doxorubicin, comprising the following steps:

[0065] (1) Get salvianolic acid A, doxorubicin hydrochloride and sodium cholate in the ratio of 10:5:500:5000 by mass ratio, dissolve them in deionized water, and make the water phase;

[0066] Take dimyristoylphosphatidylglycerol and distearoylphosphatidylethanolamine-polyethylene glycol-E-[c(RGDfK) in a mass ratio of 100:5:1000 2 ], be dissolved in absolute ethanol-dimethyl sulfoxide (volume ratio 1:1), make the first solution;

[0067] Take glyceryl laurate and distearoylphosphatidylethanolamine-polyethylene glycol-folic acid in a mass ratio of 50:5:500, and dissolve them in dimethyl sulfoxide to make a second solution:

[0068] The volume ratio is 15:1, the first solution and the second solution are combined and stirred evenly to make an oil phase;

[0069] (2) Drop the oil phase into the water phase,...

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Abstract

The invention discloses a nanostructure lipid preparation for improving doxorubicin tumor active targeting and kidney protection and a preparation method. The preparation method comprises the steps ofdissolving salvianolic acid A, doxorubicin hydrochloride and a surfactant in deionized water to prepare a water phase; dissolving an emulsifier and distearoyl phosphoethanolamine-polyethylene glycol-E-[c(RGDfK)2] in a first organic solvent to prepare a first solution; dissolving lipid and distearoyl phosphoethanolamine-polyethylene glycol-folic acid in a second organic solvent to prepare a secondsolution, combining the first solution and the second solution, and performing uniform stirring to prepare an oil phase; and dropwise adding the oil phase into the water phase, then performing heating to remove the organic solvent, and performing cooling to obtain the nanostructure lipid preparation. The nanostructure lipid preparation for improving doxorubicin tumor active targeting and kidney protection prepared by the invention has the advantages of relatively small and uniform particle size, strong tumor targeting, enhanced anti-tumor effect and reduced renal toxicity.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a nanostructured lipid preparation and a preparation method for improving active tumor targeting and kidney protection of adriamycin. Background technique [0002] Malignant tumors have become one of the most serious diseases that threaten human health and cause human death in the world today. It is predicted that the total number of cancer patients will continue to increase in the next ten years. Doxorubicin hydrochloride is an anti-tumor drug widely used in clinical medicine at the present stage. It has high-efficiency and broad-spectrum anti-cancer effects. The activities of I and II) are related to the formation of free radicals that damage DNA. It has a killing effect on tumor cells in various growth cycles, and is widely used in various malignant tumors. However, more and more clinical studies have shown that doxorubicin hydrochloride has problems such as poor targeting a...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/216A61K31/704A61K47/54A61K47/62A61P35/00
CPCA61K9/5146A61K31/704A61K31/216A61K47/545A61K47/62A61P35/00A61K2300/00
Inventor 刘志东祁东利张兵李楠郭盼皮佳鑫邓秀平李佳玮
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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