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Anti-tumor long-circulating target liposomes for injections

A liposome-targeted, anti-tumor technology, applied in anti-tumor drugs, liposome delivery, medical preparations of non-active ingredients, etc., to achieve improved anti-tumor effects, facilitate industrialization, and efficiently kill tumor cells Effect

Inactive Publication Date: 2008-12-24
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, there are still some problems in the combined application of anti-vascular drugs and anti-tumor drugs.

Method used

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  • Anti-tumor long-circulating target liposomes for injections
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  • Anti-tumor long-circulating target liposomes for injections

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] RGD-modified long-circulating liposome RGD-L [CD] simultaneously encapsulating CA-4 and adriamycin

[0046] The formulations of liposomes are: EPC:CHOL:DSPE-PEG:CA-4 (25:1.28:6.24:2) (unit: mg). Precisely weigh the prescribed amount of EPC, CHOL, DSPE-PEG, DSPE-PEG-RGD and CA-4 into a pear-shaped bottle, and add an appropriate amount of chloroform to dissolve it. 37 ℃ reduced pressure rotary evaporation into a uniform transparent film. Add 123 mM ammonium sulfate solution and sonicate in a water bath until blue opalescence appears. The 200nm polycarbonate film was extruded 5 times. Pass the prepared liposomes through a Sephadex G50 column, eluting with PBS buffer (pH 7.4) as the mobile phase, collect the liposomes, heat the collected liposomes in a 40℃ water bath, and add adriamycin Incubate the powder for 20 minutes and shake it from time to time to obtain this product.

Embodiment 2

[0048] RGD-modified long-circulating liposome RGD-L [CD] simultaneously encapsulating CA-4 and adriamycin

[0049] The formulations of liposomes are HSPC:CHOL:DSPE-PEG:CA-4 (25:1.28:6.24:2) (unit: mg). Precisely weigh the prescribed amount of HSPC, CHOL, DSPE-PEG, DSPE-PEG-RGD and CA-4 into a pear-shaped bottle, and add an appropriate amount of chloroform to dissolve it. 37 ℃ reduced pressure rotary evaporation into a uniform transparent film. Add 123 mM ammonium sulfate solution and sonicate in a water bath until blue opalescence appears. The 200nm polycarbonate film was extruded 5 times. Pass the prepared liposomes through a Sephadex G50 column, eluting with PBS buffer (pH 7.4) as the mobile phase, collect the liposomes, heat the collected liposomes in a 40°C water bath, and add Amygdalin Incubate the vegetarian powder for 20 minutes and shake it from time to time to obtain this product.

Embodiment 3

[0051] RGD-modified long-circulating liposome RGD-L [CD] simultaneously encapsulating CA-4 and adriamycin

[0052] The formulations of liposomes are: EPC:CHOL:DSPE-PEG:CA-4 (25:1.28:6.24:2) (unit: mg). Precisely weigh the prescribed amount of EPC, CHOL, DSPE-PEG, DSPE-PEG-RGD and CA-4 into a pear-shaped bottle, and add an appropriate amount of chloroform to dissolve it. 37 ℃ reduced pressure rotary evaporation into a uniform transparent film. Add 50 mM ammonium sulfate solution, and sonicate in a water bath until blue opalescence appears. The 200nm polycarbonate film was extruded 5 times. Pass the prepared liposomes through a Sephadex G50 column, eluting with PBS buffer (pH 7.4) as the mobile phase, collect the liposomes, heat the collected liposomes in a 37°C water bath, and add adriamycin Incubate the powder for 20 minutes and shake it from time to time to obtain this product.

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Abstract

The invention relates to an injection anticancer long circulating targeting liposome which is characterized in that anti-angiogenic drug is combined with anticancer drug, the liposome modified by polypeptide with tumor targeting function and hydrophilic polyethyleneglycol is adopted for loading and transporting the two drugs to tumor positions, and the tumor curative effect is enhanced through the different releasing rates and action mechanism of the two drugs.

Description

Technical field: [0001] The invention relates to an anti-tumor long-circulation targeted liposome pharmaceutical composition for injection, which is loaded with liposomes simultaneously modified with a polypeptide with tumor site targeting function and hydrophilic polyethylene glycol (PEG) , The two drugs, anti-vascular drugs and anti-tumor drugs are combined to deliver to the tumor site, and the tumor treatment effect is enhanced through the different release rates and mechanism of action of the two drugs. Background technique: [0002] Malignant tumors have always been an important disease that plagues humans, and there is currently no cure for cancer. The growth and metastasis of primary tumors depend on angiogenesis. Tumors can not only obtain nutrients and oxygen from the host through tumor blood vessels, but also continuously deliver metastatic cells to the host through tumor blood vessels, and continue to grow and induce blood vessel formation in other parts of the body, l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K45/08A61K47/42A61P35/00A61K47/34
Inventor 张强王坚成张烜张翼飞汪贻广
Owner PEKING UNIV
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