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Anti-cancer medicine liposome preparation sensitive to ray

A technology of liposome preparations and anticancer drugs, which is applied in the direction of liposome delivery, antineoplastic drugs, drug combinations, etc., can solve the problems of high toxicity of sensitizing drugs, increased clinical application, poor drug targeting, etc., and achieves improvement Anti-tumor effect, prolongation of circulation time, and effect of improving compliance

Inactive Publication Date: 2010-12-22
FUDAN UNIV SHANGHAI CANCER CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problems of radiosensitizing drugs currently used in clinical practice include high toxicity of sensitizing drugs, poor targeting of drugs, or daily radiotherapy combined with daily medication, which increases the inconvenience of clinical application, etc.
However, the radiation-sensitive anticancer drug liposome preparation has not yet been patented and reported in the literature

Method used

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  • Anti-cancer medicine liposome preparation sensitive to ray

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Containing 144.4mg hydrogenated soybean lecithin (HSPC), 68.1mg cholesterol (cholesterol), 54.8mg polyethylene glycol 2000-distearoylphosphatidylethanolamine (DSPE-PEG2000), 14.7mg dipalmitoylphosphatidylcholine ( DPPC), dissolved in 12ml of organic solvent, and 3ml of 8mg / ml cisplatin sodium chloride solution was prepared in addition, after mixing, it was homogenized at high speed, and the organic solvent was removed under reduced pressure on a rotary evaporator to make it a uniform suspension. For 1 hour, a translucent liposome suspension formed.

[0026] In this example, the sum of the molar percentages of PC and PG in phospholipids is 51%.

[0027] With the preparation prepared in this embodiment as the experimental group, and the same dose of cisplatin solution as the control group, compared with the control group, under the C060r ray 6Gy scheme, the survival time of the tumor-bearing mice was extended from 23 days to 37 (medication After 1h radiotherapy data) day...

Embodiment 2

[0038] Add an organic solvent solution containing 57 mg of dipalmitoylphosphatidylglycerol (DPPG) into an eggplant-shaped bottle, place it in a water bath at 30°C, and remove the organic solvent by rotary evaporation to form a film, then keep vacuum for 1 hour to remove the solvent completely, and pour into the eggplant-shaped bottle. Add 1ml of 10mg / ml 5-Fu HEPES solution into the bottle, vibrate vigorously, place at room temperature for 2h, and oscillate ultrasonically to form a translucent and uniform liposome suspension.

[0039] In this example, the sum of the molar percentages of PC and PG in phospholipids is 100%.

[0040]The preparation prepared in this example was used as the experimental group, and the same dose of 5-Fu solution was used as the control group. Compared with the control group, under the same radiotherapy regimen, the survival time of tumor-bearing mice was prolonged by 10-15 days .

Embodiment 3

[0042] An organic solution containing 12.6 mg dioleoylphosphatidylglycerol (DOPG), 12.8 mg dipalmitoylphosphatidylcholine (DPPC), 4.7 mg polyethylene glycol 2000-distearoylphosphatidylethanolamine (DSPE-PEG2000) Add the solvent solution into the eggplant-shaped bottle, water bath, rotary evaporation to form a film, add 1ml of 40mg / ml cyclophosphamide solution to the eggplant-shaped bottle, shake, place at room temperature for 2h, pass through the high-pressure homogenizer 10 times, and form Translucent suspension of liposomes.

[0043] In this example, the sum of the molar percentages of PC and PG in phospholipids is 95%.

[0044] The preparation prepared in this example was used as the experimental group, and the same dose of cyclophosphamide solution was used as the control group. Compared with the control group, under the same radiotherapy regimen, the survival time of tumor-bearing mice was prolonged by 7-10 days.

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Abstract

The present invention belongs to field of pharmaceutical preparation, and relates to an anti-cancer medicine liposome preparation which is sensitive to beam. According to the invention, the liposome preparation is prepared through enveloping the active compound comprising the anti-cancer medicine with lipid. The medicine is released under the function of beam. The preparation can concentrate the tumor chemotherapy and radio-therapeutic sensitivity intensifier which have radio-therapeutic sensitivity intensifying effect to the tumor position, and releases the tumor chemotherapy and radio-therapeutic sensitivity intensifier from the liposome for exerting the curative effect. The preparation increases the effective concentration of tumor chemotherapy and radio-therapeutic sensitivity intensifier which have radio-therapeutic sensitivity intensifying effect at the focus position and the staying time in vivo and the efficiency of entering the infected cell, thereby increasing the anti-tumoreffect of medicine, reducing the medicine taking dose and medicine toxicity and prolonging the life duration of tumor patient. The preparation of the invention can be used for treating various tumors.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a radiation-sensitive anticancer drug liposome preparation. Background technique [0002] Malignant tumors are one of the major diseases that threaten human life in the world today. Among the common causes of death among residents, tumors rank first in developed countries and second in developing countries. [0003] At present, the main methods for treating tumors are surgery, chemotherapy and radiation. About 45% of tumor patients can be cured, and the cure rate of radiotherapy is 18%. In the treatment of tumor patients, about 70% have received radiotherapy. The curative effect of radiotherapy is very important to improve the clinical curative effect of tumor. Improving the curative effect of radiotherapy can be studied from two aspects, radiation physics and radiation biology. Improving the radiosensitivity of tumors is a major research direction of radiation biology....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K45/06A61K47/24A61P35/00
Inventor 杨焕军徐宇虹蒋国梁陈剑葛勇前
Owner FUDAN UNIV SHANGHAI CANCER CENT