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Tumor triggered targeting ammonium hydrogen carbonate lipidosome as well as preparation method and application

An ammonium bicarbonate lipid, targeting technology, used in liposome delivery, antitumor drugs, pharmaceutical formulations, etc.

Pending Publication Date: 2019-12-03
WUHAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, ABC liposomes can only release drugs extracellularly

Method used

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  • Tumor triggered targeting ammonium hydrogen carbonate lipidosome as well as preparation method and application
  • Tumor triggered targeting ammonium hydrogen carbonate lipidosome as well as preparation method and application
  • Tumor triggered targeting ammonium hydrogen carbonate lipidosome as well as preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] Preparation method of tumor-triggered targeting ammonium bicarbonate liposomes loaded with DOX:

[0124] 18 mg distearoyl phosphoethanolamine (DSPE) and 80 mg methoxypolyethylene glycol (5000) propionaldehyde (mPEG 5000 -CHO) were dissolved in 2 mL of solvent (the volume ratio of chloroform, methanol and water was 65:35:8). After mixing the two solutions, add 100 µL of triethylamine. The mixture was then kept at 40-42°C and stirred for 12 hours. Excess DSPE was removed by dialysis (dialysis bag molecular weight cut-off 3500 Da) in a solvent. Then the crude product was treated with 0.01mol / L NaHCO 3 The solution (pH = 8-8.5) was dialyzed. The residue was lyophilized to give white powder DSPE-imine-PEG 5000 , yield 64.7%.

[0125] DPPC (5mg), cholesterol (1.8mg), DSPE-imine-PEG 5000 (3mg) and DSPE-PEG 2000 -FA (0.2 mg) was dissolved in 2 mL of chloroform, and using a rotary evaporator, the chloroform was evaporated to produce a thin lipid film. Add saturated aque...

Embodiment 2

[0128] The preparation method of the tumor-triggered targeting ammonium bicarbonate liposome loaded with paclitaxel (PTX):

[0129] 18 mg distearoyl phosphoethanolamine (DSPE) and 80 mg methoxypolyethylene glycol (5000) acetaldehyde (mPEG 5000 -CHO) were dissolved in 2 mL of solvent (the volume ratio of chloroform, methanol and water was 65:35:8). After mixing the two solutions, add 100 µL of triethylamine. The mixture was then kept at 40-42°C and stirred for 12 hours. Excess DSPE was removed by dialysis (dialysis bag molecular weight cut-off 3500 Da) in a solvent. Then the crude product was treated with 0.01mol / L NaHCO 3 The solution (pH = 8-8.5) was dialyzed. The residue was lyophilized to give white powder DSPE-imine-PEG 5000 , yield 69.8%.

[0130] DPPC (5mg), cholesterol (1.8mg), DSPE-imine-PEG 5000 (3mg), DSPE-PEG 2000 - FA (0.2 mg) and PTX (1 mg) were dissolved in 2 mL of chloroform, and using a rotary evaporator, the chloroform was evaporated to produce a thin ...

Embodiment 3

[0133] Preparation method of tumor-triggered targeting ammonium bicarbonate liposomes simultaneously loaded with DiO and DOX:

[0134] 18 mg distearoyl phosphoethanolamine (DSPE) and 80 mg methoxypolyethylene glycol (5000) propionaldehyde (mPEG 5000 -CHO) were dissolved in 2 mL of solvent (the volume ratio of chloroform, methanol and water was 65:35:8). After mixing the two solutions, add 100 µL of triethylamine. The mixture was then kept at 40-42°C and stirred for 12 hours. Excess DSPE was removed by dialysis (dialysis bag molecular weight cut-off 3500 Da) in a solvent. Then the crude product was treated with 0.01mol / L NaHCO 3 The solution (pH = 8-8.5) was dialyzed. The residue was lyophilized to give white powder DSPE-imine-PEG 5000 , yield 64.7%.

[0135] DPPC (5mg), cholesterol (1.8mg), DSPE-imine-PEG 5000 (3mg), DSPE-PEG 2000 - FA (0.2 mg) and DiO (0.1 mg) were dissolved in 2 mL of chloroform, and using a rotary evaporator, the chloroform was evaporated to produce...

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Abstract

The invention discloses a preparation method and an application of tumor triggered targeting ammonium hydrogen carbonate lipidosome. According to the preparation method, long-chain PEG (polyethylene glycol) phospholipids (PE-imine-PEG) containing pH-sensitive imine linkage are synthesized from PE (phosphatidyl ethanolamine) and mPEG-CHO (methoxy poly(ethylene glycol) aldehyde); and a tumor triggered targeting ammonium hydrogen carbonate lipidosome nanomaterial is prepared from phospholipids, cholesterol, PE-imine-PEG, DSPE-PEG-folate and an aqueous ABS (ammonium hydrogen carbonate) solution asraw materials. The tumor triggered targeting ammonium hydrogen carbonate lipidosome not only has the characteristic of long circulation in blood, but also can exert the targeting characteristic in the tumor microenvironment; by means of the folic acid ligand-receptor action, the lipidosome can enter tumor cells, and can produce CO2 bubbles at the increased temperature or in acidic endosome / lysosome; and permeable defects can be produced in a phospholipid bilayer by the produced CO2 bubbles, a drug is rapidly released in cells, and the tumor cells are killed accordingly.

Description

technical field [0001] The present invention relates to a tumor-triggered targeting ammonium bicarbonate liposome nanomaterial, and the present invention also relates to a preparation method of the tumor-triggered targeting ammonium bicarbonate liposome nanomaterial, and the tumor-triggered targeting ammonium bicarbonate liposome nanomaterial It can be used as an antitumor drug carrier. Background technique [0002] Over the past few decades, nanomedicine has provided many exciting new opportunities for the development of new strategies for cancer treatment. Due to the abnormal vascular structure and ineffective lymphatic drainage in solid tumors, nanoparticles can accumulate in tumor tissues through the enhanced permeability and retention (EPR) effect in blood circulation. In addition, researchers have developed stimuli-responsive nanoparticles for tumor-specific therapy. Stimuli include exogenous stimuli (eg, temperature, magnetic fields, light, ultrasound, etc.) and end...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/10A61K47/28A61K31/704A61P35/00
CPCA61K9/127A61K47/24A61K47/10A61K47/28A61K31/704A61P35/00
Inventor 邹涛陈淑窈李莉夏甜李游
Owner WUHAN UNIV OF SCI & TECH
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