Chloroquine and adriamycin co-supported liposome and preparation method thereof

A doxorubicin and liposome technology, applied in the field of chloroquine and doxorubicin co-loaded liposome and its preparation, can solve the problems of cell drug resistance, poor anticancer effect and the like, and achieves wide selection of phospholipids, The effect of reducing dosage and suppressing multidrug resistance

Active Publication Date: 2011-08-03
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the doxorubicin preparations that have been approved for clinical use or are undergoing clinical evaluation are mainly liposome preparations, such as the product named Mycet liposome doxorubicin for the combination therapy of recurrent breast cancer, although to a certain extent It reduces the toxicity of doxorubicin to the heart and to normal cells, but there is still the problem that it is easy to make the cells resistant to the drug and the anti-cancer effect is not good.

Method used

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  • Chloroquine and adriamycin co-supported liposome and preparation method thereof
  • Chloroquine and adriamycin co-supported liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Weigh 500mg of soybean lecithin (purity of phosphatidylcholine > 76%) and 100mg of cholesterol dissolved in 20mL of ether, then add 10mL of pH=4.0 citric acid-sodium citrate buffer, mix well and emulsify, then evaporate the organic solvent under reduced pressure diethyl ether, and sonicate for 5 min with a cell disruptor to obtain 10 mL of a blank liposome suspension, which is used as a blank liposome for later use. The average particle diameter (number average) of the blank liposome suspension was measured to be 129 nm.

Embodiment 2

[0034] Weigh 420mg of dipalmitoylphosphatidylcholine (DPPC), 60mg of phosphatidylethanolamine (PE) and 100mg of cholesterol, dissolve in 10mL of ether, mix well, put the solution in a ground-mouthed round bottom flask, and keep the temperature at 37°C Evaporate the organic solvent diethyl ether under reduced pressure with a rotary evaporator on a water bath, so that film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 5 mL of 0.1mol / L citric acid-sodium citrate buffer solution (pH=3.6) to the lipid film , rotate on a rotary evaporator until the liposome hydration turns into a milky white liposome suspension, ultrasonically pulverize for 10 minutes to reduce the particle size, and obtain 10 mL of a blank liposome suspension, which is used as a blank liposome for later use. The average particle diameter of the blank liposome suspension was measured to be 133nm.

Embodiment 3

[0036] Weigh 500mg soybean lecithin (phosphatidylcholine purity>76%), 40mg cholesterol and polyethylene glycol monomethyl ether (molecular weight is 2000) cholesterol succinate (CHS-PEG 2000 ) 80mg, dissolved in 20mL ether, mixed evenly, then added 10mL 0.1mol / L citric acid-sodium citrate buffer solution (pH=3.6), mixed evenly to form an emulsion, then distilled off the organic solvent ether under reduced pressure, and crushed with cells Ultrasound for 5 minutes to obtain 10 mL of blank liposome suspension, which is used as blank liposome for later use. The average particle diameter of the blank liposome suspension was measured to be 137nm.

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Abstract

The invention discloses a chloroquine and adriamycin co-supported liposome, which is prepared from medicaments, phospholipid, cholesterol compounds, an internal buffer system and a pH value regulator, wherein a weight ratio of the medicaments to the phospholipid to the cholesterol compounds is (1:2)-(100:1)-35, and the medicaments comprises chloroquine medicaments and adriamycin medicaments. The chloroquine and adriamycin common-carried liposome has the characteristics of inhibiting the tolerance of multiple medicaments and reducing medicinal toxicity under the synergistic action of chloroquine and adriamycin. The invention also discloses a preparation method for the chloroquine and adriamycin co-supported liposome, a preparation process is simple, controlled parameters are few, reaction conditions are low, production cost can be reduced conveniently and the chloroquine and adriamycin co-supported liposome is easy to industrially produce.

Description

technical field [0001] The invention relates to the technical field of liposome medicaments, in particular to a liposome co-loaded with chloroquine and doxorubicin and a preparation method thereof. Background technique [0002] In the past 50 years, significant progress has been made in the prevention and treatment of cancer. However, due to the difficulty in early diagnosis of cancer and the lack of effective technical solutions for the treatment of cancer metastasis, it is still a difficult problem to cure cancer. Therefore, it is very important and urgent to find new methods for cancer treatment . [0003] Doxorubicin is a commonly used drug for cancer chemotherapy (Multidrug resistance in cancer: role of ATP-dependent transporter). It was first isolated from a Streptomyces by the Faroitalia Research Laboratory in Milan in the early 1960s. The second anthracycline antibiotic to be discovered after The structures of doxorubicin and daunorubicin are basically the same, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/00A61K9/127A61K31/704A61K31/4706
CPCA61K31/704A61K9/1278A61K9/127A61K31/4706A61P35/00A61K2300/00
Inventor 邱利焱姚铭飞
Owner ZHEJIANG UNIV
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