Anti-tumor pH-sensitive liposome, its freeze-dried powder preparation and their preparation method

A technology of freeze-dried powder injection and liposome, which can be used in anti-tumor drugs, liposome delivery, freeze-dried delivery, etc. Enhances compliance and reduces toxic side effects

Inactive Publication Date: 2011-12-14
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This kind of liposome is beneficial to improve the anti-tumor effect of the drug, but its sensitivity to the change of environmental pH value has not been found

Method used

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  • Anti-tumor pH-sensitive liposome, its freeze-dried powder preparation and their preparation method
  • Anti-tumor pH-sensitive liposome, its freeze-dried powder preparation and their preparation method
  • Anti-tumor pH-sensitive liposome, its freeze-dried powder preparation and their preparation method

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Experimental program
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Effect test

Embodiment 1

[0031] Take by weighing 30mg phosphatidylethanolamine, 30mg cholesterol, 10mg oleic acid and be dissolved in 10ml organic solvent (V 氯仿 :V 甲醇 =9:1), the mixed solution was evaporated to dryness under pressure until a uniform lipid film was formed. Add 2ml of vinorelbine tartrate drug solution (drug concentration: 5mg / ml) with pH=7.4 to dissolve and ultrasonicate to form a homogeneous suspension, supplement with PBS buffer solution with pH7.4 to make the final volume 20ml, and hydrate for 30min in a water bath at 37°C Then obtain vinorelbine tartrate pH-sensitive liposomes, add mannitol 3.5 mg as a freeze-drying protective agent, freeze-dry after 12 hours at -80°C to obtain the lyophilized powder of vinorelbine tartrate, and use normal saline before use Reconstitute. The obtained vinorelbine tartrate pH-sensitive liposome average particle diameter is 290nm, and transmission electron microscope photo is as attached figure 1 As shown, the particle size distribution is as attac...

Embodiment 2

[0033] Take by weighing 90mg phosphatidylethanolamine, 90mg cholesterol, 30mg oleic acid and be dissolved in 30ml organic solvent (V 氯仿 :V 甲醇 =9:1), the mixed solution was evaporated to dryness under pressure until a uniform lipid film was formed. Add 6ml of the drug solution of vinorelbine tartrate (drug concentration is 5mg / ml) of pH=7.4 to dissolve and ultrasonicate to form a uniform suspension, supplement with the PBS buffer solution of pH7.4 so that the final volume is 60ml, and carry out high pressure milking to reduce the particle size evenly. Vinorelbine tartrate pH-sensitive liposomes were obtained after hydration for 30 minutes in a water bath at 37°C, and 10.5 mg of mannitol was added as a freeze-drying protective agent. Dry powder, reconstitute with saline before use. The obtained vinorelbine tartrate pH-sensitive liposome average particle diameter is 232nm, and transmission electron microscope photo is as attached image 3 As shown, the particle size distributi...

Embodiment 3

[0035] Take by weighing 150mg phosphatidylethanolamine, 150mg cholesterol, 15mg oleic acid and be dissolved in 30ml organic solvent (V 氯仿 :V 甲醇 =9:1), the mixed solution was evaporated to dryness under pressure until a uniform lipid film was formed. Add 6ml of the drug solution of vinorelbine tartrate (drug concentration is 5mg / ml) of pH=7.4 to dissolve and ultrasonicate to form a uniform suspension, supplement with the PBS buffer solution of pH7.4 so that the final volume is 60ml, and carry out high pressure milking to reduce the particle size evenly. Vinorelbine tartrate pH-sensitive liposomes were obtained after hydration for 30 minutes in a water bath at 37°C, and 15.75 mg of mannitol was added as a lyoprotectant, which was pre-frozen at -80°C for 12 hours and then freeze-dried to obtain vinorelbine tartrate lyosomes. Dry powder, reconstitute with saline before use. The average particle diameter of the prepared vinorelbine tartrate pH-sensitive liposome is 252nm.

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Abstract

The invention relates to an anti-tumor pH-sensitive liposome, a freeze-dried powder injection preparation thereof and a preparation method thereof. The anti-tumor pH-sensitive liposome mainly consists of the following raw materials in parts by weight: 1 part of an anti-tumor active pharmaceutical ingredient , 1-20 parts of phospholipids, 1-20 parts of cholesterol and 0.5-10 parts of oleic acid, the phospholipids are one of phosphatidylethanolamine, dioleoylphosphatidylethanolamine and hydrogenated phospholipids. The present invention uses phosphatidylethanolamine as phospholipid, and the polar group of this phospholipid is protonated in an acidic environment, thereby causing changes in the structure of liposomes. Better release effect.

Description

Technical field: [0001] The invention relates to an anti-tumor pH-sensitive liposome, in particular to vinorelbine tartrate pH-sensitive liposome, its freeze-dried powder preparation and its preparation method. Background technique: [0002] Vinorelbine tartrate (Vinorelbine Bitartrate, VB) is a semi-synthetic vinca alkaloid. Microtubule formation, cell division arrest in mitotic metaphase, is a cell cycle specific drug. Like other vinblastines, vinorelbine tartrate can also inhibit the cycle of amino acids and the metabolism of glutathione; the activity of Ca-ATPase dependent on calmodulin; the biological oxidation of cells and the biosynthesis of nucleic acids and oils; Clinically, it is mainly used for non-small cell lung cancer, metastatic breast cancer, advanced ovarian cancer, malignant lymphoma, etc. However, after the drug is injected intravenously, it has relatively serious side effects, such as bone marrow suppression, gastrointestinal toxicity, and hair loss. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K31/475A61K47/28A61P35/00
Inventor 林贵梅张芳邵伟
Owner SHANDONG UNIV
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