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Preparation and application of a targeted 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 inhibition of transfer, simple preparation, and uniform particle size distribution Effect

Active Publication Date: 2022-03-11
TIANJIN UNIV OF SCI & TECH
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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 targeted liposome designed and prepared by the present invention not only It can target the drug to the tumor site, and can also inhibit the tumor metastasis mediated by E-selectin, so it has obvious innovation and creativity

Method used

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  • Preparation and application of a targeted thermosensitive liposome modified by e-selectin peptide ligand
  • Preparation and application of a targeted thermosensitive liposome modified by e-selectin peptide ligand
  • Preparation and application of a targeted thermosensitive liposome modified by e-selectin peptide ligand

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Linkage of E-selectin peptide ligand 8-CR to DSPE-PEG2000-Mal.

[0052] Weigh 18.9mg of 8-CR and dissolve in 4ml of HEPES buffer solution (20mMHEPES, 10mM EDTA, pH=6.5), weigh 31.3mg of DSPE-PEG2000-Mal and dissolve in 4ml of chloroform, fully dissolve and place on a rotary evaporator at 50°C to remove the organic solvent. Then it was hydrated and dissolved with HEPES buffer solution at 55°C for 15 minutes, and added to the polypeptide solution, that is, the molar ratio of 8-CR to DSPE-PEG2000-Mal was 2:1, and stirred at room temperature under the protection of argon. 48 hours. After the reaction, the above system was dialyzed in a dialysis bag with a molecular weight cut off of 3000 for 48 hours, and then freeze-dried to obtain DSPE-PEG2000-Mal-8CR.

Embodiment 2

[0053] Example 2 Preparation of blank liposomes.

[0054] Preparation of plain blank liposomes.

[0055] Weigh 166mg, 18mg, 6mg, 10mg of dipalmitoylphosphatidylcholine, cultured phosphatidylethanolamine, myristoyl lysolecithin, DSPE-PEG2000-Mal respectively and dissolve them in chloroform to form a solution. The organic solvent was removed on the instrument (55° C., 60 r / min), and then the above-mentioned liposomes were placed in a vacuum drying oven for vacuum drying for 3 hours. Add 6 ml of citric acid / sodium citrate buffer solution with pH=7.2 to the dried liposomes and hydrate and dissolve them in a rotary evaporator (58° C., 100 r / min) for 25 minutes. The above liposome solution was ultrasonically disrupted for 5 min with a cell disruptor, and passed through a 0.22 μm membrane to obtain ordinary blank liposome G.

[0056] Preparation of targeting blank liposomes.

[0057] Weigh respectively 166mg, 18mg, 6mg and 10mg of dipalmitoylphosphatidylcholine, cultured phosphati...

Embodiment 3

[0058] Example 3 Preparation of drug-loaded liposomes.

[0059] Preparation of common drug-loaded liposomes.

[0060] Weigh dipalmitoylphosphatidylcholine, cultured phosphatidylethanolamine, myristoyl lysolecithin, DSPE-PEG2000-Mal, paclitaxel 166mg, 18mg, 6mg, 10mg, 8mg and dissolve in chloroform to form a solution, fully dissolve Afterwards, the organic solvent was removed on a rotary evaporator (55° C., 60 r / min), and then the liposomes were dried in a vacuum oven for 3 hours. Add 6 ml of citric acid / sodium citrate buffer solution with pH=7.2 to the dried liposomes and hydrate and dissolve them in a rotary evaporator (58° C., 100 r / min) for 25 minutes. The above-mentioned liposome solution was ultrasonically disrupted with a cell disruptor for 5 minutes, and passed through a 0.22 μm membrane to obtain ordinary drug-loaded liposome E.

[0061] Preparation of targeted drug-loaded liposomes.

[0062] Weigh dipalmitoylphosphatidylcholine, cultured phosphatidylethanolamine, m...

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Abstract

The present invention relates to a preparation method and application of tumor targeting liposome modified by E-selectin polypeptide ligand, and the targeting liposome is composed of phosphatidylethanolamine-polyethylene glycol-maleimide-E The selectin peptide-ligand conjugate, dipalmitoyl phosphatidylcholine, cultured phosphatidylethanolamine and myristoyl lysolecithin are prepared. The conjugate DSPE-PEG-Mal-8CR involved is chemically coupled and synthesized by E-selectin peptide ligand 8-CR and phosphatidylethanolamine-polyethylene glycol-maleimide, and the tumor prepared by the present invention Targeting long-circulating thermosensitive liposomes, loaded with different anti-tumor drugs, can actively target tumor angiogenesis and inhibit the migration of tumor cells, which is of great significance for the treatment of tumor metastasis and recurrence.

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. [0002] technical background [0003] 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. [0004] 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 b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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 UNIV OF SCI & TECH
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