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Octreotide-modified gold spherical shell nano liposome and preparation method thereof

A nano-liposome and octreotide technology, applied in the field of medicine, can solve the problems of uncontrollable release and poor targeting, and achieve the effects of no toxic side effects, mild experimental conditions, and reduced damage

Inactive Publication Date: 2017-03-15
YANSHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the conventional liposome drug delivery system has a series of defects, such as uncontrollable release of chemotherapy drugs, poor targeting, etc.

Method used

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  • Octreotide-modified gold spherical shell nano liposome and preparation method thereof
  • Octreotide-modified gold spherical shell nano liposome and preparation method thereof
  • Octreotide-modified gold spherical shell nano liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] 14mg soybean lecithin (purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd.), 2.0mg cholesterol (purchased from Tianjin Damao Chemical Instrument Supply Station) and 2.0mg oleanolic acid (purchased from Sichuan Shifang Huakang Pharmaceutical Raw Material Factory ), dissolved in 1 mL of absolute ethanol, and obtained a lipid ethanol solution by magnetic stirring; 1.2 mg of glutathione was dissolved in 4 mL of pH=6.0 phosphate buffer as a hydration medium, and 1 mL of lipid The ethanol solution was dropped into 4mL 35°C hydration medium drop by drop at a uniform speed to obtain a liposome suspension; then stirred for 1 hour to remove the absolute ethanol in the liposome suspension to obtain glutathione-modified olean acid nanoliposomes;

[0031] At -20°C, 30 μL of 240 mM sodium borohydride (NaBH 4 ) solution, quickly dropwise into 1mL of 0.1mM gold chloride solution, shake vigorously, and react for 1min to obtain a gold nanoparticle solution with a particle size ...

Embodiment 2

[0037]25mg soybean lecithin (purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd.), 5mg cholesterol (purchased from Tianjin Damao Chemical Instrument Supply Station) and 2.5mg oleanolic acid (purchased from Sichuan Shifang Huakang Pharmaceutical Raw Material Factory) , dissolved in 1 mL of absolute ethanol, and obtained a lipid ethanol solution by magnetic stirring; 3.5 mg of glutathione was dissolved in 7 mL of pH=6.5 phosphate buffer as a hydration medium, and 1 mL of lipid ethanol was The solution was dropped into 7 mL of hydration medium at 45°C drop by drop at a constant speed to obtain a liposome suspension; then stirred for 1.5 hours to remove absolute ethanol in the liposome suspension to obtain glutathione-modified oleanolic acid Nanoliposomes;

[0038] At -20°C, 50 μL of 250 mM sodium borohydride (NaBH 4 ) solution, quickly dropwise into 1mL of 0.7mM gold chloride solution, shake vigorously, and react for 4 minutes to obtain a gold nanoparticle solution with...

Embodiment 3

[0044] 42 mg soybean lecithin (purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd.), 9.0 mg cholesterol (purchased from Tianjin Damao Chemical Instrument Supply Station) and 3.0 mg oleanolic acid (purchased from Sichuan Shifang Huakang Pharmaceutical Raw Material Factory ), dissolved in 1mL absolute ethanol, and obtained lipid ethanol solution by magnetic stirring; 6.0mg glutathione was dissolved in 10mL pH=7.0 phosphate buffer as a hydration medium, and 1mL lipid Pour the ethanol solution dropwise into 10 mL of hydration medium at 55°C at a constant speed to obtain a liposome suspension; then stir for 2 hours to remove the absolute ethanol in the liposome suspension to obtain glutathione-modified olean acid nanoliposomes;

[0045] At -20°C, 80 μL of 270 mM sodium borohydride (NaBH 4 ) solution, quickly added dropwise to 1mL of 1.5mM gold chloride solution, shaken vigorously, and reacted for 8 minutes to obtain a gold nanoparticle solution with a particle size of 5-1...

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Abstract

The invention relates to an octreotide-modified gold spherical shell nano liposome which is formed by forming a compact nano gold spherical shell on the surface of an oleanolic acid nano liposome and coating an octreotide ligand on the gold spherical shell surface. The particle size of the octreotide-modified gold spherical shell nano liposome is 50-200nm, and the surface plasma resonance absorption wavelength is 650-950nm. The preparation method mainly comprises the following steps: modifying the oleanolic acid liposome with glutathione so that the oleanolic acid liposome surface is provided with mercapto groups; carrying out crystal seed growth to prepare the gold spherical shell nano liposome; and finally, under mild conditions, coupling octreotide onto the gold nanoparticle surface through surface amino and hydroxy groups under the condition that the octreotide solution / gold spherical shell nano liposome volume ratio is (0.3-1):1, and carrying out co-incubation to obtain the octreotide-modified gold spherical shell nano liposome. The method is simple to operate, easy to control and mild in conditions. The treatment effect on cancer is enhanced by utilizing the photothermal effect of nano gold spherical shells, controlled release of drugs and specific targeting property of octreotide to tumor cells.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a nano liposome and a preparation method thereof. Background technique [0002] At present, the incidence of malignant tumors is increasing worldwide, and new drugs and new therapies are emerging in an endless stream. However, these treatments have very large side effects on the body, and most malignant tumors are difficult to cure. Therefore, we are looking for a specific, safe, non-toxic Side effects of cancer treatments remain a major problem in global cancer treatment. [0003] Studies have found that natural plant anti-tumor drugs have significant anti-cancer effects and low toxic and side effects. Oleanolic acid is a natural anti-tumor drug widely distributed in a variety of plants, such as wine grapes, hawthorn, jujube and so on. Oleanolic acid has a variety of biological and pharmacological activities, such as anti-tumor, anti-virus, anti-oxidation and anti-inflammatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/51A61K41/00A61K31/56A61K47/42A61P35/00
CPCA61K9/127A61K9/0002A61K9/5115A61K31/56A61K41/0052A61K47/42A61K2300/00
Inventor 高大威王倩倩刘艳平骆丽垚邢珊珊
Owner YANSHAN UNIV
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