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Amphipathilic block polymer micelle nano medicament carrying system and preparation method

The technology of an amphiphilic polymer and a drug-carrying system, which is applied in the field of biomedicine, can solve the problems of small drug-carrying amount, low drug encapsulation rate, affecting the utilization rate of raw materials and drug delivery efficiency, and achieves the encapsulation rate. Improve, improve utilization, increase the effect of encapsulation efficiency or drug loading

Inactive Publication Date: 2010-09-15
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since polymer micelles accommodate hydrophobic small molecule drugs through the hydrophobic microenvironment, in the research of polymer micelles used as drug carriers, it is often found that the drug encapsulation efficiency is biased during the preparation of drug-loaded micelles. Low and small drug loading, which greatly affects the utilization of raw materials and the efficiency of polymer micelles for drug delivery in vivo

Method used

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  • Amphipathilic block polymer micelle nano medicament carrying system and preparation method
  • Amphipathilic block polymer micelle nano medicament carrying system and preparation method
  • Amphipathilic block polymer micelle nano medicament carrying system and preparation method

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Experimental program
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Effect test

Embodiment 1

[0023] Take 5 mg / ml of polyethylene glycol-phosphatidylethanolamine (mPEG2000-DSPE, purchased from Avantipolar lipid company in the United States) in chloroform 1ml and 0.5 mg / ml of mitoxantrone (available from Beijing Xinze Technology Co., Ltd.) in chloroform Add 0.1ml of the solution into a round-bottomed flask, then add 0.5ml of 0.1mg / ml phosphatidylethanolamine (DSPE, purchased from Avanti polar lipid company in the United States) in chloroform suspension, mix well and evaporate in a water bath at 30°C Dry the organic solvent to form a polymer film; prepare a film without adding phosphatidylethanolamine solution in parallel in the same batch as a control. Then the drug film was vacuum-dried overnight (8 hours), and then the flask containing the drug film was placed in a 50° C. water bath, and 5 ml of double-distilled water was added to magnetically stir for 20 minutes, and the drug-loaded micelles were formed. Finally, the prepared polymer micelles were dialyzed overnight ...

Embodiment 2

[0030] Take 1 ml of methanol solution of 5 mg / ml polyethylene glycol-phosphatidylethanolamine (mPEG2000-DSPE, purchased from Avantipolar lipid company of the United States) and 0.5 mg / ml of mitoxantrone (purchased from Beijing Xinze Technology Co., Ltd.) methanol Add 0.1ml of the solution into a round-bottomed flask, then add 0.5ml of methanol suspension of 0.1mg / ml phosphatidylethanolamine (DSPE, purchased from Avanti polar lipid company in the United States), mix well, and evaporate in a water bath at 35°C. Dry the organic solvent to form a polymer film; then vacuum-dry the film overnight, then place the flask containing the film in a 40°C water bath and add 5ml of double-distilled water to magnetically stir for 20 minutes, and the drug-loaded micelles are formed. Finally, the prepared polymer micelles were dialyzed overnight with a dialysis bag with a molecular weight cut-off of 14,000 Daltons (the dialysate was double-distilled water) to separate unencapsulated free drugs. ...

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Abstract

The invention relates to a method for increasing medicament carrying amount and entrapment rate of polymer micelles on an anti-tumor medicament by using hydrophobic molecules. The polymer micelles are prepared from amphipathilic polymer such as polyethylene glycol-phosphatidyl ethanolamine (PEG-DSPE) by a membrane hydration method, and the micelles can be used for wrapping insoluble or low water-soluble anti-tumor medicaments for chemotherapy of tumor. Compared with the polymer micelles prepared without adding hydrophobic molecules, the polymer micelles obtained by adding the hydrophobic molecules such as phospholipid molecules with longer aliphatic chains (10 to 20 carbon atoms) in a certain proportion during preparing the polymer micelles by using the membrane hydration method obviously increase the entrapment rate and the medicament carrying amount on the raw material medicaments of the anti-tumor medicaments. The entrapment rate increment of the polymer micelles on the raw material medicaments improves the utilization rate of the raw material medicaments, and the medicament carrying amount of the polymer micelles improves the efficiency of medicament transmission during treating the tumor so as to lay a foundation for further increasing the curative effect of the anti-tumor medicament.

Description

Technical field: [0001] The invention belongs to the field of biomedicine, in particular to an amphiphilic block polymer micelle nano-loading system and a preparation method, specifically, adding phospholipids such as phospholipids in the process of preparing polymer micelles by membrane hydration method Acetyl ethanolamine, phosphatidylcholine, etc., and then increase the encapsulation efficiency and drug loading of micellar drugs, so as to achieve the goal of improving the utilization rate of raw materials and the delivery efficiency of drug carriers. Background technique: [0002] Polymer micelle is a kind of nanoparticle self-assembled by amphiphilic polymer in water, and its particle size range is usually between 10-100nm. The hydrophobic end constitutes the inner core of the micelle and constitutes a hydrophobic microenvironment, thus providing a space for hydrophobic drugs and having a significant solubilization effect on them. Polymer micelles have high stability, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K31/136A61P35/00
Inventor 张其清陈汉张彤李学敏
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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