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Targeting thermosensitive liposome

A heat-sensitive liposome and targeting technology, applied in liposome delivery, antineoplastic drugs, drug combination, etc.

Inactive Publication Date: 2012-07-11
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no report on the modification of thermosensitive liposomes containing anti-tumor drugs by CREKA at home and abroad.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0147] Linkage of tumor-homing peptide CREKA to DSPE-PEG2000-maleimide

[0148] Weigh CREKA (1.1mg), DSPE-PEG2000-maleimide (5mg), that is, the molar ratio of CREKA and DSPE-PEG2000-maleimide is 2: 1, dissolve in 3ml PBS (i.e. reactant concentration of 2 mg / ml), adjust the pH to 7, and stir at room temperature for 24 hours under the protection of nitrogen. The material obtained from the above reaction was placed in a dialysis bag with a molecular weight cut off of 2000 for dialysis for 48 hours, and then freeze-dried to obtain DSPE-PEG2000-CREKA.

Embodiment 2

[0150] Linkage of tumor-homing peptide CREKA to DSPE-PEG2000-maleimide

[0151] Weigh CREKA (1.1mg), DSPE-PEG2000-maleimide (10mg), that is, the molar ratio of CREKA and DSPE-PEG2000-maleimide is 1:1, dissolve in 5.55ml PBS (i.e., react concentration of 2 mg / ml), adjust the pH to 7, and stir at room temperature for 24 hours under the protection of nitrogen. The material obtained from the above reaction was placed in a dialysis bag with a molecular weight cut off of 2000 for dialysis for 48 hours, and then freeze-dried to obtain DSPE-PEG2000-CREKA.

Embodiment 3

[0153] Linkage of tumor-homing peptide CREKA to DSPE-PEG2000-maleimide

[0154] Weigh CREKA (1.1mg), DSPE-PEG2000-maleimide (5mg), that is, the molar ratio of CREKA and DSPE-PEG2000-maleimide is 2:1, dissolve in 6.1ml PBS (i.e. the reaction concentration of 1 mg / ml), adjust the pH to 7, and stir at room temperature for 24 hours under the protection of nitrogen. The material obtained from the above reaction was placed in a dialysis bag with a molecular weight cut off of 2000 for dialysis for 48 hours, and then freeze-dried to obtain DSPE-PEG2000-CREKA.

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Abstract

The invention belongs to the field of targeted drug delivery systems, and particularly relates to a targeting thermosensitive liposome combination. The targeting thermosensitive liposome combination is characterized in that: the combination comprises thermosensitive liposome, the surface of which is modified by tumor homing peptide CREKA (cys-arg-glu-lys-ala) or peptide with a CREKA core sequence, and the thermosensitive liposome contains antitumor medicine. The invention also relates to a preparation method of the targeting thermosensitive liposome combination and an application of the targeting thermosensitive liposome combination in the preparation of drugs for treating malignant tumors. The targeting thermosensitive liposome has a good tumor-targeting effect and a good antitumor effect.

Description

technical field [0001] The invention relates to a targeted drug delivery system, in particular to a targeted thermosensitive liposome composition modified with a tumor homing peptide. The present invention also relates to the preparation method of the targeted thermosensitive liposome composition and the use of the targeted thermosensitive liposome composition in the preparation of medicines for treating malignant tumors. Background technique [0002] Liposomes have been extensively developed over the past forty years as carriers of chemotherapeutic drug delivery systems, especially in tumor therapy. In recent years, thermosensitive liposomes that combine physicochemical targeting and pulse release properties have attracted more and more attention in the field of antitumor. [0003] Thermosensitive liposomes (thermosensitive liposomes, TSL) are a class of liposomes made of thermosensitive materials whose phase transition temperature is slightly higher than normal tissue tem...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/42A61P35/00
Inventor 张烜王欣张强
Owner PEKING UNIV
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