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A class of self-cleaving multifunctional liposome and its application

A multi-functional, self-cleavage technology, applied in the direction of liposome delivery, wave energy or particle radiation treatment materials, medical preparations of non-active ingredients, etc. Tissue and organ side effects and other issues, to overcome tumor drug resistance, enhance anti-tumor activity, and improve the effect of treatment

Active Publication Date: 2021-07-09
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term application has also found that liposomes also have some shortcomings as a drug delivery carrier: (1) active targeting is lacking, and the drug cannot accurately reach the disease target site to play a role, which not only affects the curative effect of the drug but also causes damage to other tissues. Toxic and side effects of organs; (2) do not have stimuli responsiveness, and can not release drugs specifically at the lesion site. Usually, liposome carriers have better stability, and it is not easy to release or release less after loading drugs, which limits Drugs play a further role; (3) can not effectively overcome the drug resistance of tumors, the mechanism of tumor drug resistance is diverse, traditional liposomes can not effectively overcome the drug resistance of tumors, and give full play to the advantages of the drug delivery system

Method used

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  • A class of self-cleaving multifunctional liposome and its application
  • A class of self-cleaving multifunctional liposome and its application
  • A class of self-cleaving multifunctional liposome and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A preparation method for self-cleaving multifunctional liposomes, comprising the following steps:

[0039] (1) Preparation of intermediate 1

[0040]

[0041] Dissolve p-cresol (6.21g, 0.05mmol) and sodium hydroxide (2.00g, 0.05mmol) in 40mL of ethanol, then add bromoacetic acid (6.95g, 0.05mmol) and sodium carbonate (2.88g, 0.03mmol) The 50mL aqueous solution formed was stirred at room temperature for 4h and then refluxed for 1h. Cool to room temperature, remove ethanol by rotary evaporation, adjust pH to 2 with concentrated hydrochloric acid, precipitate a large amount of white solid, filter with suction, and dry to obtain 8.65 g of white solid, yield 95.0%.

[0042] Intermediate 1: ESI-MS: m / z [M-COOH] - =137.04.

[0043] (2) Preparation of Intermediate 2

[0044]

[0045] Intermediate 1 (3.00g, 16.48mmol) was dissolved in 50mL of glacial acetic acid, magnetically stirred, and 6mL of 30% H 2 o 2(diluted with 10 mL of glacial acetic acid), heated to 70°C f...

Embodiment 2

[0073] Preparation of blank liposomes and drug-loaded liposomes

[0074] Blank liposome: Weigh 30mg DSPC, 18mg cholesterol, 2mg magnetic phospholipid and other membrane materials and dissolve them in 10mL chloroform solution. Ultrasound promotes the dissolution. After complete dissolution, use a vacuum rotary evaporator to remove the organic solvent to form a thin film, freeze-dry for 12 hours Thoroughly remove the organic solvent, add 9 mL of deionized water, hydrate in a water bath at 45°C to form liposomes, sonicate with a probe for 8 min, and filter to obtain a blank liposome solution.

[0075] Drug-loaded liposomes: Weigh 30mg DSPC, 18mg cholesterol, 2mg magnetic phospholipid and other membrane materials and dissolve them in 10mL chloroform solution, ultrasonically promote dissolution to obtain a membrane material solution, weigh 4.5mg doxorubicin and dissolve them in methanol solution, and Add it to the above membrane material solution, ultrasonically promote miscibility...

Embodiment 3

[0077] Paramagnetic assay

[0078] Measure the saturation magnetization and coercive force of the magnetically targeted phospholipids of the NO donor bridge chain with a vibrating sample magnetometer (VSM). The experimental program is as follows: sample mass: 5mg; sample stage: cylindrical sample stage; Chip position: attached to the bottom of the cylindrical sample stage; temperature: room temperature constant temperature; measuring magnetic field range: -20000G ~ 20000G; maximum magnetic moment: <700memu; test time: 2h; experimental data: magnetization curve (ordinate: emu / g) , saturation magnetization (Ms), mass (m), coercive force (Hc), remanence (Br); point setting: take a total of 51 points (as shown in Table 1), and measure the sample magnetic moment point by point- Magnetic field curve.

[0079] Table 1 VSM test point setting

[0080]

[0081] The result is as figure 1 As shown, when the external magnetic field is from the negative maximum to 0 to the positive ma...

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Abstract

The invention relates to a self-cleaving multifunctional liposome and its application. The preparation method is to sequentially introduce nitric oxide donor, polyethylene glycol and superparamagnetic ferric iron tetroxide into the amino terminal of distearoylphosphatidylethanolamine Nanoparticles can be used to obtain magnetically targeted phospholipids of NO donor bridges; the NO donor bridged magnetically targeted phospholipids disclosed in the present invention can be used as the main component, combined with other auxiliary materials such as distearoyl phosphatidylcholine and cholesterol Nano-liposomes are prepared; the liposomes disclosed in the present invention can encapsulate anti-tumor drugs such as doxorubicin, and the drug delivery system obtained has good stability under physiological conditions, and at the same time, it can be enriched in the magnetic field area under external magnetic field conditions, Realize magnetic targeting; NO donors can crack and release NO molecules under the action of glutathione and other triggering factors, which not only helps to improve anti-tumor activity and overcome tumor drug resistance, but also causes nano-liposomes to disintegrate, Release the loaded drug, improve the drug release efficiency of the drug delivery system, and improve the tumor treatment effect.

Description

technical field [0001] The invention relates to a class of self-cleaving multifunctional liposome and application thereof, belonging to the field of tumor targeting therapy. Background technique [0002] Cancer is one of the most terrible diseases plaguing human beings, which seriously threatens human life and health. In recent decades, although medicine and biology have made great progress, the treatment of tumors has not been significantly improved. According to a survey by the World Health Organization, since 2012, cancer patients and deaths worldwide have been increasing rapidly, among which the Asian population accounts for nearly half of the new patients. [0003] Surgery and chemotherapy are the main weapons for cancer patients to fight against the disease. Unfortunately, the therapeutic effects of chemotherapy drugs currently used in clinical practice are not satisfactory, and their main defects are poor selectivity and serious side effects. Therefore, it is immine...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/60A61K47/54A61K49/08A61K49/18A61K31/4245A61K31/704A61K41/00A61P35/00C08G65/334C08G65/335C08G65/328
CPCA61K9/127A61K9/1277A61K31/4245A61K31/704A61K41/0052A61K49/08A61K49/1812A61K47/544A61K47/545A61K47/60A61P35/00C08G65/328C08G65/3348C08G65/3356C08G2650/04C08G2650/50
Inventor 房雷徐方泽
Owner SOUTHEAST UNIV
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