DSPE-PEG-FA-modified nanometer paclitaxel liposome and preparation method thereof

A technology of phosphatidylethanolamine and polyethylene glycol, which is applied in the directions of liposome delivery, medical preparations of inactive ingredients, and pharmaceutical formulations, can solve the problem of low efficacy of folic acid-paclitaxel nanoliposomes, affecting drug efficacy, problems such as low drug efficacy, to achieve the effects of good drug encapsulation efficiency, good colloidal stability, and high encapsulation efficiency
CN102188382BInactive Publication Date: 2014-01-15李红霞
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
李红霞
Publication Date
2014-01-15
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. A molar ratio of the DSPE-PEG2000-FA to egg yolk lecithin is 0.05% to 0.15%, and a particle size of the liposome is less than 150 nm. A preparation method of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome comprises the following steps: first, preparing a DSPE-PEG2000-FA into a DSPE-PEG2000-FA micelle; second, performing incubation on the DSPE-PEG2000-FA micelle and a paclitaxel liposome together to obtain a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. Materials, which are forbidden to be used in clinical practice, are not used as crude materials in the present invention. According to the invention, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has a small particle size, and the content of the DSPE-PEG2000-FA is low; besides, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has good drug entrapment efficiency and good colloid stability. Moreover, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome can be absorbed effectively by an ovarian cancer cell having properties of sensitiveness to folic acid (+) and drug resistance, and the cytotoxicity of folic acid dependence is displayed; therefore, the efficacy of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome is stronger than that of a paclitaxel injection.
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Description

technical field

[0001] The invention relates to a medicine for treating tumors, in particular to a nano-paclitaxel liposome modified by phosphatidylethanolamine-polyethylene glycol 2000-folate and a preparation method thereof; Applications in cancer drugs. Background technique

[0002] When cytotoxic drugs are used for chemotherapy of tumors, the failure of chemotherapy is often caused by the failure of the drugs to reach an effective concentration in the tumor site, and the toxicity and side effects will also increase.

[0003] Ovarian cancer is the culprit of gynecological tumors, with a high mortality rate. Because more than 90% of ovarian cancers are folate receptor-positive, with a high expression level, while normal ovarian epithelial folate receptors are negative, in folate receptor (folic acid)-mediated targeted therapy for ovarian cancer, drugs are combined with folic acid to utilize The overexpression of folate receptors in tumor cells, with folate receptors as t...

Claims

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