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Preparation and application of target thermosensitive liposome modified by E-selectin peptide ligand

A technology targeting liposomes and peptide ligands, applied in the direction of liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., to achieve uniform particle size distribution, simple preparation, and inhibition of metastasis Effect

Active Publication Date: 2018-10-12
TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present there is no targeted liposome that can simultaneously solve the problem of tumor cell metastasis on the above basis, and the transfer of tumor is the most important cause of tumor death at present. The targ

Method used

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  • Preparation and application of target thermosensitive liposome modified by E-selectin peptide ligand
  • Preparation and application of target thermosensitive liposome modified by E-selectin peptide ligand
  • Preparation and application of target thermosensitive liposome modified by E-selectin peptide ligand

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0049] Example 1

[0050] Linkage of E-selectin peptide ligand 8-CR and DSPE-PEG2000-Mal.

[0051] Weigh 18.9 mg of 8-CR and dissolve it in 4 ml of HEPES buffer solution (20 mM HEPES, 10 mM EDTA, pH = 6.5), weigh 31.3 mg of DSPE-PEG2000-Mal and dissolve in 4 ml of chloroform, and dissolve it in a rotary evaporator at 50°C. Remove organic solvents. Then it was hydrated and dissolved with HEPES buffer solution at 55°C for 15 minutes, and added to the peptide solution, that is, the molar ratio of 8-CR to DSPE-PEG2000-Mal was 2:1, and stirred at room temperature under argon protection 48 hours. After the reaction, the above system was placed in a dialysis bag with a molecular weight cut-off of 3000 for dialysis for 48 hours, and then freeze-dried to obtain DSPE-PEG2000-Mal-8CR.

Example Embodiment

[0052] Example 2 Preparation of blank liposomes.

[0053] Preparation of ordinary blank liposomes.

[0054] Weigh 166mg, 18mg, 6mg, and 10mg of dipalmitoylphosphatidylcholine, cultured phosphatidylethanolamine, myristoyl lysolecithin, and DSPE-PEG2000-Mal, respectively, and dissolve them in chloroform to form a solution, which is fully dissolved and then rotary evaporated The organic solvent was removed on the instrument (55°C, 60r / min), and then the liposomes were placed in a vacuum drying oven for vacuum drying for 3 hours. The dried liposomes were hydrated and dissolved in a rotary evaporator (58°C, 100r / min) by adding 6ml of a pH=7.2 citric acid / sodium citrate buffer solution for 25 minutes. The above liposome solution was ultrasonically disrupted with a cell disruptor for 5 min, and passed through a 0.22 μm membrane to obtain ordinary blank liposome G.

[0055] Preparation of targeted blank liposomes.

[0056] Weigh 166mg, 18mg, 6mg, and 10mg of dipalmitoylphosphatidylcholine, ...

Example Embodiment

[0057] Example 3 Preparation of drug-loaded liposomes.

[0058] Preparation of common drug-loaded liposomes.

[0059] Weigh 166mg, 18mg, 6mg, 10mg and 8mg of dipalmitoylphosphatidylcholine, cultured phosphatidylethanolamine, myristoyl lysolecithin, DSPE-PEG2000-Mal, paclitaxel and dissolve them in chloroform to form a solution. Then, the organic solvent was removed on a rotary evaporator (55°C, 60r / min), and then the liposomes were placed in a vacuum drying oven for vacuum drying for 3 hours. The dried liposomes were hydrated and dissolved in a rotary evaporator (58°C, 100r / min) with 6ml pH=7.2 citric acid / sodium citrate buffer solution for 25min. The liposome solution was ultrasonically disrupted with a cell disruptor for 5 min, and passed through a 0.22 μm membrane to obtain ordinary drug-loaded liposome E.

[0060] Preparation of targeted drug-loaded liposomes.

[0061] Weigh 166mg, 18mg, 6mg, 10mg, 8mg of dipalmitoylphosphatidylcholine, cultured phosphatidylethanolamine, myristo...

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Abstract

The invention relates to a preparation method and application of target thermosensitive liposome modified by an E-selectin peptide ligand. The target thermosensitive liposome is prepared from phosphatidyl ethanolamine-polyethylene glycol-maleimide-E selectin peptide ligand conjugate, dipalmitoyl phosphatidylcholine, phosphatidylethanolamine pegol and myristoyl lysoph-osphatidylcholine. Selectin peptide ligand 8-CR and phosphatidyl ethanolamine-polyethylene glycol-maleimide are subjected to chemical coupling synthesis to obtain the related conjugate DSPE-PEG-Mal-8CR, and after carrying different antineoplastic drugs, the prepared tumor targeted long circulation thermosensitive liposome can initiatively target at tumor angiogenesis, inhibit cell migration, and have important significance ontumor metastasis and relapse.

Description

technical field [0001] The invention belongs to the technical field of biomedical preparations, and relates to E-selectin ligands that can compete with tumor cells for binding to E-selectin to block or inhibit the migration of tumor cells, and in particular to a targeting agent modified by E-selectin peptide ligands. Preparation of thermosensitive liposome and its application in antitumor. technical background [0002] E-selectin can specifically recognize the terminal domains of certain glycoproteins and glycolipid molecules on the surface of tumor cells, and the interaction between E-selectin and tumor cells mediated by this recognition can make tumor cells endothelial Cell adhesion, and then migration with the blood flow, resulting in the spread and migration of tumor cells. [0003] The structural characteristics of the natural ligands of E-selectin have not yet been fully elucidated. Some studies have suggested that the natural ligands specifically recognized by it may...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/62A61K31/337A61K31/555A61K31/704A61P35/00A61P35/04
CPCA61K47/62A61K47/6911A61P35/00A61P35/04A61K31/337A61K31/555A61K31/704
Inventor 郁彭郭娜赵龙李凤燕付颖郝甜甜杜春阳王浩猛李明媛滕玉鸥王栋
Owner TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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