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Lipidosome with entrapment antitumor drugs and radiotherapy sensitivity enhancing function

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

Active Publication Date: 2016-05-04
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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  • Lipidosome with entrapment antitumor drugs and radiotherapy sensitivity enhancing function
  • Lipidosome with entrapment antitumor drugs and radiotherapy sensitivity enhancing function
  • Lipidosome with entrapment antitumor drugs and radiotherapy sensitivity enhancing function

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 mole 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 drip into the ammonium sulfate solution with a concentration of 0.3mol / L, and stir while dripping, to prepare liposomes with radiotherapy sensitization, and the concentration of the liposomes is 3mg / mL;

[0052] Step 2) Add a weighed water-soluble anti-tumor drug doxorubicin hydrochloride solution to the radiosensitizing liposome 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 water bath at 60°C, ...

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, add it to PBS with pH=7.4, the concentration of camptothecin liposomes without hydrophobic anti-tumor drug is 3mg / mL, and ultrasonic 2-5 hours at 100W to obtain entrapped liposomes Radiosensitizing liposomes of the hydrophobic anticancer drug camptothecin. ...

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 90nm, see figure 1 .

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Abstract

The invention provides a lipidosome with entrapment antitumor drugs and a radiotherapy sensitivity enhancing function. The lipidosome comprises a lipidosome body with the radiotherapy sensitivity enhancing function and antitumor drugs. The lipidosome body with the radiotherapy sensitivity enhancing function is prepared from, by mole, 40-60% of the lipidosome body with the radiotherapy sensitivity enhancing function, 30-50% of cholesterol and 5-15% of polyethylene glycol phospholipid. The dosage of the antitumor drugs accounts for 2-20% the mass of the lipidosome body with the radiotherapy sensitivity enhancing function. According to the lipidosome with the entrapment antitumor drugs and the radiotherapy sensitivity enhancing function, due to the nanoscale size, passive targeting can be performed at a tumor position through a tumor EPR effect, and toxic and side effects brought when drugs are distributed all over the body are lowered; the therapy effect of synchronizing radiotherapy sensitizer and drug molecules is achieved, and the clinical application and practical therapy significance are achieved.

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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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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