Preparation method and application of cytarabine-modified methotrexate-loaded liposome

A technology of carrying methotrexate lipids and carrying methotrexate, which is applied in the field of biomedicine and can solve the problems of high disease recurrence rate, low specificity of methotrexate, and serious side effects
CN110151698BActive Publication Date: 2020-09-04ZHEJIANG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG UNIV
Publication Date
2020-09-04

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Abstract

The invention provides preparation and application of a cytarabine-modified methotrexate-loaded liposome. The liposome is prepared by taking phospholipid, cholesterol, cytarabine-PEG2k-DSPE and methotrexate as raw materials and adopting a membrane dispersion method combined with an ultrasonic and high-pressure homogenization method through dissolution, membrane formation, hydration, ultrasonic andhigh-pressure homogenization and freeze-drying. The liposome prepared by the method has a particle diameter of about 125 nanometers, a dispersion coefficient of 0.218, a drug loading capacity of themethotrexate of about 10.37% and an entrapment ratio of about 85.26%. Nucleoside transporters 1 on the surfaces of choriocarcinoma cells can specifically recognize cytarabine and mediate the cytarabine-modified methotrexate-loaded liposome into the cells, thereby increasing the cytotoxicity of the drug. The cytarabine-modified methotrexate-loaded liposome has a simple preparation process, is easyto produce on a large scale, and provides a novel pharmaceutical preparation for the treatment of choriocarcinoma.
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Description

Technical field

[0001] The invention belongs to the field of biomedicine, and specifically relates to a preparation method of a methotrexate-loaded liposome modified with cytarabine and its application in the treatment of trophoblastic tumors. Background technique

[0002] With the promulgation of my country's comprehensive two-child policy, women's demand for reproductive growth has increased sharply, and the incidence of gestational trophoblastic tumors (including choriocarcinoma) has further increased significantly. If not diagnosed early or treated improperly, gestational trophoblastic tumors may cause severe bleeding, rupture of the uterus, removal of the uterus, etc., seriously threatening women's reproductive health and even life. Methotrexate is the first-line drug for the treatment of gestational trophoblastic tumors. However, when methotrexate is administered systemically, it has poor specific distribution ability. It is prone to liver damage, abdominal pain, gastrointe...

Claims

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