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Anti-tumor long-circulating target liposomes for injections

A long-circulation liposome and anti-tumor technology, applied in the direction of anti-tumor drugs, liposome delivery, medical preparations of non-active ingredients, etc., to achieve improved anti-tumor effect, simple production, and efficient killing of tumor cells

Inactive Publication Date: 2011-04-27
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
  • Anti-tumor long-circulating target liposomes for injections
  • Anti-tumor long-circulating target liposomes for injections

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] RGD-L[CD], a RGD-modified long-circulating liposome loaded with both CA-4 and doxorubicin

[0047] The formulations of the liposomes were: 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, add appropriate amount of chloroform to dissolve. Rotary evaporation under reduced pressure at 37°C formed a uniform transparent film. Add 123mM ammonium sulfate solution, and sonicate in a water bath until blue opalescence appears. A polycarbonate film of 200 nm was extruded 5 times. Pass the prepared liposomes through a SephadexG50 column, elute with PBS buffer (pH7.4) as the mobile phase, collect the liposome fraction, heat the collected liposomes in a water bath at 40°C, and add doxorubicin Incubate the powder for 20 minutes and shake it frequently to obtain this product.

Embodiment 2

[0049] RGD-L[CD], a RGD-modified long-circulating liposome loaded with both CA-4 and doxorubicin

[0050]The formulations of the liposomes were: 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, add appropriate amount of chloroform to dissolve. Rotary evaporation under reduced pressure at 37°C formed a uniform transparent film. Add 123mM ammonium sulfate solution, and sonicate in a water bath until blue opalescence appears. A polycarbonate film of 200 nm was extruded 5 times. Pass the prepared liposomes through a Sephadex G50 column, elute with PBS buffer (pH7.4) as the mobile phase, collect the liposome fraction, heat the collected liposomes in a water bath at 40°C, add Adriamycin Incubate the plain powder for 20 minutes and shake it frequently to obtain this product.

Embodiment 3

[0052] RGD-L[CD], a RGD-modified long-circulating liposome loaded with both CA-4 and doxorubicin

[0053] The formulations of the liposomes were: 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, add appropriate amount of chloroform to dissolve. Rotary evaporation under reduced pressure at 37°C formed a uniform transparent film. Add 50mM ammonium sulfate solution, and sonicate in a water bath until blue opalescence appears. A polycarbonate film of 200 nm was extruded 5 times. Pass the prepared liposomes through a SephadexG50 column, elute with PBS buffer (pH7.4) as the mobile phase, collect the liposome fraction, heat the collected liposomes in a water bath at 37°C, and add doxorubicin Incubate the powder for 20 minutes and shake it frequently 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 a liposome simultaneously modified with a polypeptide having tumor site targeting function and hydrophilic polyethylene glycol (PEG) , to deliver two kinds of anti-vascular drugs and anti-tumor drugs to the tumor site, and enhance the tumor treatment effect through the different release rates and mechanisms of the two drugs. Background technique: [0002] Malignant tumors have always been an important disease that plagues human beings, and there is currently no cure for cancer. Primary tumor growth and metastasis depend on angiogenesis. Tumors can not only obtain nutrients and oxygen from the host through tumor blood vessels, but also continuously transport metastatic cells to the host through tumor blood vessels, and continue to grow and induce blood vessel formation in other parts of the body, leading to tumor met...

Claims

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Application Information

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