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A radiosensitizing liposome encapsulating antitumor drugs

An anti-tumor drug, liposome technology, applied in the directions of anti-tumor drugs, liposome delivery, drug combination, etc., can solve the problems of neurotoxic side effects and the effects of toxic side effects on the body, so as to improve drug stability and reduce toxicity. Side effects, the effect of reducing the speed of elimination

Active Publication Date: 2019-03-22
XUZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of these sensitizers are administered through intravenous infusion, requiring large doses to produce sensitization, and at the same time causing severe neurotoxic side effects
(2) Combination of radiotherapy and chemotherapy: Clinically, synchronous radiotherapy and chemotherapy are used to treat tumors, and have achieved certain curative effects, but the toxic and side effects of radiotherapy and chemotherapy have a serious impact on the body

Method used

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  • A radiosensitizing liposome encapsulating antitumor drugs
  • A radiosensitizing liposome encapsulating antitumor drugs
  • A radiosensitizing liposome encapsulating antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Method for encapsulating water-soluble antitumor drugs

[0049] The selected lipid molecule with radiosensitization function has the structural formula:

[0050] ;

[0051] Step 1) Dissolve the raw materials weighed by molar fraction, including 50% of lipid molecules with radiosensitization function, 35% of cholesterol and 15% of polyethylene glycol phospholipid DSPE-PEG2000; all dissolved in an appropriate amount of ethanol solvent, Then slowly drop into the ammonium sulfate solution with a concentration of 0.3 mol / L, and stir while dropping in, to prepare liposomes with radiosensitization effect, and the concentration of the liposomes is 3 mg / mL;

[0052] Step 2) Add a weighed water-soluble anti-tumor drug doxorubicin hydrochloride solution to the liposome with radiosensitization effect prepared in step 1), and the dosage of the doxorubicin hydrochloride drug accounts for the radiosensitization effect 10% of the liposome mass; under the condition of heating in a 6...

Embodiment 2

[0054] Method for Encapsulating Hydrophobic Antitumor Drugs

[0055] The selected lipid molecule with radiosensitization function has the structural formula:

[0056] ;

[0057]Dissolve the raw materials weighed by mole fraction, including 50% of lipid molecules with radiosensitization function, 40% of cholesterol and 10% of polyethylene glycol phospholipids in an appropriate amount of chloroform solvent, and then add hydrophobic antitumor Drug camptothecin, the amount of the hydrophobic antineoplastic drug camptothecin accounts for 10% of the mass of the radiosensitizing liposome; after fully mixing, put it into a single-necked flask, and use a rotary evaporator to remove chloroform Solvent, after forming an oil film, then added to PBS with pH = 7.4, the concentration of camptothecin liposomes not carrying the hydrophobic anti-tumor drug was 3 mg / mL, and ultrasonicated at 100 W for 2-5 hours to obtain Liposomes with radiosensitizing effect loaded with hydrophobic anticanc...

Embodiment 3

[0059] Characterization of liposome morphology for radiosensitization

[0060] Observing the morphology of embodiment 1 radiosensitization effect liposome with transmission electron microscope, the result shows, has obvious lipid bilayer structure, and particle diameter is about 90 nm, see figure 1 .

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Abstract

The invention provides a radiosensitizing liposome loaded with antitumor drugs, which includes liposomes with radiosensitization and antitumor drugs; each raw material in the liposomes with radiosensitization And its mole fraction is: lipid molecule 40-60% with radiosensitization function, cholesterol 30-50%, polyethylene glycol phospholipid 5-15%; 2-20% of the plastid mass; radiosensitizing liposomes loaded with anti-tumor drugs can be passively targeted to tumors through the tumor EPR effect due to their nanoscale size, reducing the risk of drug systemic distribution. Toxic and side effects; the present invention realizes the therapeutic effect of synchronous radiotherapy sensitizer and drug molecule, and possesses clinical applicability and realistic therapeutic significance.

Description

technical field [0001] The invention relates to a radiosensitizing liposome loaded with antitumor drugs and belongs to the field of preparation of tumor drugs. Background technique [0002] The treatment of tumors is still based on surgery, radiotherapy and chemotherapy. The synergistic treatment of radiotherapy and chemotherapy has become the main means of tumor treatment. In recent years, many studies have confirmed that the curative effect of simultaneous radiotherapy and chemotherapy is better than that of radiotherapy and chemotherapy separately. Toxic side effects of the body. [0003] In recent years, the number of patients treated with tumor radiotherapy has been increasing day by day. Due to the existence of hypoxia in solid tumors, it is still difficult to cure the tumors even if the maximum possible radiation dose or the radiation method is changed. In order to effectively cure tumors, scientists use radiosensitizers or a combination of radiotherapy and chemothe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/28A61K47/24A61K47/22A61K45/06A61P35/00
CPCA61K9/127A61K45/06A61K47/22A61K47/24A61K47/28
Inventor 刘洪梅于如同解彦东周秀萍张亚飞蔡一帆李白杨
Owner XUZHOU MEDICAL COLLEGE
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