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Taxol liposome preparation with active tumor targeting function as well as preparation method and application thereof

A liposome preparation and active targeting technology, which is applied in liposome delivery, medical preparations of non-active ingredients, antineoplastic drugs, etc., can solve the problems of poor water solubility, large toxic and side effects, short half-life, etc., and achieve enhanced Targetability, uniformity of mass, effect of reduced distribution

Inactive Publication Date: 2017-08-08
SICHUAN PROVINCIAL PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the above-mentioned deficiencies in existing small molecule antineoplastic drug dosage forms such as poor water solubility, short half-life and large toxic and side effects, and provide a paclitaxel liposome preparation with active tumor targeting function

Method used

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  • Taxol liposome preparation with active tumor targeting function as well as preparation method and application thereof
  • Taxol liposome preparation with active tumor targeting function as well as preparation method and application thereof
  • Taxol liposome preparation with active tumor targeting function as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 A paclitaxel liposome formulation A with active tumor targeting function

[0040] Calculated in mol / mol, paclitaxel, egg yolk lecithin, cholesterol, cultured phosphatidylethanolamine, tbFGF-PEG in the prescription 2000 -The dosage ratio of DSPE and water for injection is 2:60:25:5:3:50.

[0041] First, the tbFGF polypeptide is linked to maleimide-polyethylene glycol-phospholipid (DSPE-PEG-MAL) by chemical coupling. DSPE-PEG-MAL can be purchased from a reagent company. The specific reaction process is in DSPE -Add excess tbFGF polypeptide to the PBS (pH 7.4) solution of PEG-MAL, incubate at 4°C for 2 hours, make the sulfhydryl group of tbFGF react with the maleyl group of DSPE-PEG-MAL to form S-C bond through Michael reaction, and centrifugal filter Remove uncoupled tbFGF to obtain tbFGF-PEG-DSPE.

[0042] Next, the prescribed amount of paclitaxel, egg yolk lecithin, cholesterol, cultured phosphatidylethanolamine and tbFGF-PEG 2000 - DSPE was dissolved in ab...

Embodiment 2

[0043] Example 2 A paclitaxel liposome preparation B with active tumor targeting function

[0044] Calculated in mol / mol, paclitaxel, egg yolk lecithin, cholesterol, cultured phosphatidylethanolamine, tbFGF-PEG in the prescription 4000 -The dosage ratio of DSPE and water for injection is 1:40:40:3:10:200.

[0045] Adopt the same method of embodiment 1 to prepare tbFGF-PEG 4000 -Chol.

[0046] The prescribed amount of paclitaxel, egg yolk lecithin, cholesterol, cultured phosphatidylethanolamine and tbFGF-PEG 4000 - DSPE is dissolved in absolute ethanol to form a solution, heated to 40°C; the above solution is slowly injected into water for injection, so that the raw material solution and the aqueous solution fully react; the above alcohol-containing liposome solution is heated at 40°C with a rotary evaporator Ethanol was removed under reduced pressure to obtain a liposome solution; the liposomes were sized with a high-pressure homogenizer, and homogenized under pressures of ...

Embodiment 3

[0047] Example 3 A paclitaxel liposome preparation C with active tumor targeting function

[0048] Calculated in mol / mol, paclitaxel, egg yolk lecithin, cholesterol, cultured phosphatidylethanolamine, tbFGF-PEG in the prescription 1000 -The dosage ratio of DSPE and water for injection is 10:80:10:15:1:20.

[0049] Adopt the same method of embodiment 1 to prepare tbFGF-PEG 1000 -DSPE.

[0050] The prescribed amount of paclitaxel, egg yolk lecithin, cholesterol, cultured phosphatidylethanolamine and tbFGF-PEG 1000 - DSPE is dissolved in absolute ethanol to form a solution, heated to 50°C; the above solution is slowly injected into water for injection, so that the raw material solution and the aqueous solution fully react; the above alcohol-containing liposome solution is evaporated at 50°C The ethanol was removed under reduced pressure to obtain a liposome solution; the liposomes were sized with a high-pressure homogenizer, and homogenized under a pressure of 300 bar and 700 ...

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Abstract

The invention discloses a taxol liposome preparation with an active tumor targeting function. The preparation is prepared from taxol, egg yolk lecithin, cholesterol, phosphatidylethanolamine pegol, tbFGF-PEG-DSPE (truncated basic fibroblast growth factor-polyethylene glycol-distearoyl phosphatidylethanolamine) and injection water. According to the preparation, tbFGF capable of being specifically combined with tumor cells and tumor angiogenic blood vessels and maleinimide-polyethylene glycol-phospholipid (DSPE-PEG-MAL) are chemically coupled, thus preparing the tbFGF-PEG-DSPE, and a liposome is prepared from a coupling product and wraps the taxol, thus building a liposome dosage form with long circulation and active tumor targeting functions; therefore, the active tumor targeting and tumor resisting effects are enhanced.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a paclitaxel liposome preparation with active tumor targeting function and its preparation method and application. Background technique [0002] Cancer is one of the major diseases that threaten human health. It has become the first cause of death for human beings, and its incidence continues to rise. However, typical chemotherapeutic drugs have disadvantages such as poor water solubility, short half-life, narrow therapeutic index, and high systemic toxicity. Finding high-efficiency, low-toxic anticancer drugs and new preparations to completely conquer cancer is one of the important research topics in the world medical community. Paclitaxel has anti-tumor activity, and as a second-line treatment drug for advanced ovarian cancer, it has shown encouraging curative effects in the treatment of breast cancer, lung cancer, leukemia, gastrointestinal cancer and vascular reste...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/42A61K47/24A61K31/337A61P35/00
Inventor 蔡璐璐闫峻峰曾代文白皎皎杨钏瑶
Owner SICHUAN PROVINCIAL PEOPLES HOSPITAL
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