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Application of novel liposome-entrapped mitoxantrone combined chemotherapeutic drug in antineoplastic treatment

A technology of mitoxantrone lipid and chemotherapeutic drugs, which is applied in the directions of antitumor drugs, liposome delivery, drug combination, etc., can solve the problems of unsatisfactory effect and no combined application of mitoxantrone liposome chemotherapeutic drugs, etc. , to achieve significant anti-tumor efficacy, reduce myelosuppressive toxicity and myocardial toxicity, and improve the effect of survival rate

Inactive Publication Date: 2016-02-03
JILIN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although MTO has a good anti-tumor effect clinically, its severe adverse reactions (bone marrow suppression, dose-limiting cardiotoxicity, gastrointestinal toxicity, fatigue, etc.) limit its clinical use.
[0006] At present, dosage forms such as mitoxantrone lipid nanoparticles have been studied at home and abroad, but the effects are not satisfactory
Domestic research in this field is still in its infancy, and liposome preparations using cardiolipin-containing liposomes to encapsulate mitoxantrone have not been reported other than the relevant results of our research group, and there is no mitoxantrone yet. Related reports on combined application of liposomes and other chemotherapeutic drugs

Method used

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  • Application of novel liposome-entrapped mitoxantrone combined chemotherapeutic drug in antineoplastic treatment
  • Application of novel liposome-entrapped mitoxantrone combined chemotherapeutic drug in antineoplastic treatment
  • Application of novel liposome-entrapped mitoxantrone combined chemotherapeutic drug in antineoplastic treatment

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: Preparation of mitoxantrone liposome (LEM) formulation

[0058] 1,1',2,2'-4 myristoyl cardiolipin, lecithin and cholesterol in a molar ratio of 1:5:10 were lyophilized into powder form. Sterile mitoxantrone saline solution at a concentration of 1.0 mg / ml was added to the dried lipids. The molar ratio of drug to lipid is 1:15. The above mixture was hydrated at room temperature for 2 h, and then the hydrated suspension was sonicated in a bath sonicator for 10 min to obtain LEM.

[0059] The encapsulation efficiency of the liposome obtained in the present invention is 89.41±1.26%. The liposome mean diameter 100-120nm that this method makes ( figure 1 ), the liposome stability reached 94% in 8h.

Embodiment 2

[0060] Embodiment 2: Preparation of mitoxantrone liposome (LEM) formulation

[0061] Cardiolipin, phosphatidylcholine and cholesterol are lyophilized into powder with a molar ratio of 1:7:12. A 0.5 mg / ml mitoxantrone saline solution was mixed with the dry lipids. The molar ratio of drug to fat is 1:12.5. The mixture was hydrated at room temperature for 2 h and sonicated for 10 min. Liposomes encapsulating mitoxantrone are available. The amount of mitoxantrone in the liposomes was determined by a spectrophotometer at 658 nm. The drug entrapment rate was calculated by the following formula: entrapment rate=(drug concentration after dialysis / drug concentration before dialysis)×100%.

[0062] The encapsulation efficiency of the mitoxantrone liposome prepared by the above method is 94.62 ± 3.19%, the particle diameter of the gained liposome is 57.63 ± 1.24nm, and the stability is good. At room temperature, the mitoxantrone lipid The stability within 8 hours is good, and the le...

Embodiment 3

[0065] Embodiment 3: In vitro cytotoxicity test of LEM

[0066] The HL60 leukemia cells in the logarithmic growth phase were inoculated into 96-well cell culture plates (cell grouping: normal saline group, blank liposome group, LEM group, MTO group) for culture, and then added different concentrations of LEM or MTO, each Concentration 3 replicate wells, in 5% CO 2 , Cultured in a cell culture box at 37°C for 72 hours, and evaluated the cytotoxic effect of LEM and MTO on different cell lines by MTT method, so as to preliminarily predict the strength of LEM and its sensitivity to different types of tumor cells. Negative control was normal saline or blank liposome control. The cytotoxicity of the two preparations was studied by MTT method.

[0067] Calculate the cell survival rate according to the formula, and calculate the IC50 according to the linear equation.

[0068] Cell survival rate={D(570) value of treatment group / D(570) value of control group}×100%

[0069] Cell inhi...

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Abstract

The invention discloses an application of a novel liposome-entrapped mitoxantrone combined chemotherapeutic drug in antineoplastic treatment. According to the invention, a new liposome-entrapped mitoxantrone preparation containing components such as cardiolipin is prepared internationally, and is used for being combined with other clinical routine first-line chemotherapeutics for antineoplastic treatment. The invention expounds the preparation method and symptom research of the novel liposome preparation, the preparation has the characteristics of high entrapment rate, uniform particle size distribution, good stability, prolongation of chemotherapeutics half life, and reduction of toxic and side effect; compared with other treatment methods, in breast cancer and leukemia tumor animal models, antineoplastic curative effect of the new liposome-entrapped mitoxantrone preparation and other chemotherapeutics is more obvious.

Description

technical field [0001] The invention discloses the application of novel mitoxantrone liposome combined with chemotherapeutic drugs in antitumor treatment. It involves the application of mitoxantrone liposome preparation in combination with other clinical conventional first-line chemotherapy drugs in the treatment of tumors, and also involves the preparation method of mitoxantrone liposome and related characterization research. Background technique [0002] In China, the health burden of cancer is increasing year by year. Every year, more than 1.6 million people are diagnosed with cancer and 1.2 million people die of cancer. It is worth noting that 20% of new cancer patients worldwide are in China, and 24% of cancer deaths are in China. At present, for every 5 deaths in China, 1 person dies from cancer; and among the population aged 0-64, 1 person dies from cancer for every 4 deaths. "Trend higher. The World Health Organization (WHO) published the "Global Cancer Report 201...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/136A61K45/06A61K31/675A61K31/337A61K33/24A61P35/00
Inventor 裴瑾韩冰郝强张正宋丽萍丛登立李燕田琳杨越王曾孙雨馨陈景霖
Owner JILIN UNIV
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