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Heparin-modified cleavable adriamycin liposome preparation and preparation method thereof

A doxorubicin lipid and heparin technology, applied in the field of pharmaceutical preparations, can solve problems such as restrictions on the application of doxorubicin, affecting the quality of life of patients, and dose-dependent cardiotoxicity

Inactive Publication Date: 2015-06-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

After injection, it is widely distributed in the heart, liver, spleen, lung, and kidney, and disappears rapidly in plasma, and has many adverse reactions, the most serious being dose-dependent cardiotoxicity and neurotoxicity, which not only affect the quality of life of patients, Moreover, the application of doxorubicin is limited, which has always been the focus of chemical structure modification and new formulation research and development.

Method used

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  • Heparin-modified cleavable adriamycin liposome preparation and preparation method thereof
  • Heparin-modified cleavable adriamycin liposome preparation and preparation method thereof
  • Heparin-modified cleavable adriamycin liposome preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0047] Weigh 80 mg of soybean lecithin, 8 mg of cholesterol, and 4 mg of octadecylamine in prescription quantities respectively and place them in an eggplant-shaped bottle, and add an appropriate amount of chloroform to completely dissolve them; A dry and uniform lipid film was formed on the wall of the bottle, and the rotary evaporation under reduced pressure was continued for 2 h. Add 2 mL of 300 mmol / L ammonium sulfate solution in PBS to wash the membrane, and hydrate in a water bath at 40° C. for 1 h to form a liposome primary emulsion. Probe ultrasound (200W, 100 times) to obtain blank liposomes. The above blank liposomes were dialyzed in PBS solution for 3 hours, then added with adriamycin solution (1 mg / mL), and incubated in a water bath at 60°C for 60 minutes to obtain DOX-Lip. Take the DOX-Lip solution and an equal volume of Hep-DTSP (4mg / mL), and add triethylamine to react for 30min. The Hep-S-S-DOX-Lip suspension is obtained.

Embodiment 2

[0049] Weigh 10 mg of soybean lecithin, 1 mg of cholesterol, and 1 mg of octadecylamine respectively in prescription quantities and place them in an eggplant-shaped bottle, and add an appropriate amount of chloroform to completely dissolve them; A dry and uniform lipid film was formed on the wall of the bottle, and the rotary evaporation under reduced pressure was continued for 2 h. Add 2 mL of 300 mmol / L ammonium sulfate solution in PBS to wash the membrane, and hydrate in a water bath at 30° C. for 1 h to form a liposome primary emulsion. Probe ultrasound (200W, 100 times) to obtain blank liposomes. The above blank liposomes were dialyzed in PBS solution for 3 hours, then added with doxorubicin solution (1 mg / mL), and incubated in a water bath at 50°C for 30 minutes to obtain DOX-Lip. Take the DOX-Lip solution and an equal volume of Hep-DTSP (1 mg / mL), and add triethylamine to react for 30 min. The Hep-S-S-DOX-Lip suspension is obtained.

Embodiment 3

[0051] Weigh 40 mg of soybean lecithin, 4 mg of cholesterol, and 2 mg of octadecylamine in recipes, respectively, and place them in an eggplant-shaped bottle, and add an appropriate amount of chloroform to dissolve them completely; A dry and uniform lipid film was formed on the wall of the bottle, and the rotary evaporation under reduced pressure was continued for 2 h. Add 2 mL of 300 mmol / L ammonium sulfate solution in PBS to wash the membrane, and hydrate in a water bath at 37°C for 1 hour to form a liposome primary emulsion. Probe ultrasound (200W, 100 times) to obtain blank liposomes. The above blank liposomes were dialyzed in PBS solution for 3 hours, then added with adriamycin solution (1 mg / mL), and incubated in a water bath at 55°C for 45 minutes to obtain DOX-Lip. Take the DOX-Lip solution and an equal volume of Hep-DTSP (2mg / mL), and add triethylamine to react for 30min. The Hep-S-S-DOX-Lip suspension is obtained.

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Abstract

The invention discloses a heparin-modified cleavable adriamycin liposome preparation and a preparation method thereof. The adriamycin liposome comprises soya bean lecithin, cholesterol, octadecylamine, adriamycin and heparin-modified materials, wherein the heparin is modified on the surface of the adriamycin liposome through a disulfide bond. According to the heparin-modified cleavable adriamycin liposome prepared by a film dispersion method, after the liposome reaches tumor cells, the fracture of the disulfide bond of the liposome is triggered by highly expressed glutathione in the tumor cell, so as to remove the heparin at an outer layer and release anti-tumor medicine very well; and the role of inhibiting tumor metastasis by the heparin is put into play.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a heparin-modified bond-breakable doxorubicin liposome (Hep-S-S-DOX-Lip) preparation, and the invention also discloses the preparation of the Hep-S-S-DOX-Lip preparation Preparation. Background technique [0002] Heparin (Hep) is an acidic mucopolysaccharide widely used clinically for anticoagulant and antithrombotic. In recent years, people have found that heparin can inhibit tumor metastasis and prolong the life of malignant tumor patients when using heparin as an adjunct to the treatment and prevention of venous thrombosis complicated by cancer. Therefore, a large number of basic and clinical researches have been carried out on the anti-metastasis mechanism of heparin at home and abroad. The research results show that the anti-tumor metastasis effect of heparin involves all aspects of tumor formation and growth. Heparin promotes the release of tissue factor altern...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/728A61K47/48A61P35/04A61P35/00A61K31/704
Inventor 柯学韩苗苗杨淼张强
Owner CHINA PHARM UNIV
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