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Polymeric micelle medicine composition and preparation method thereof

A technology of polymer glue, composition, applied in the field of medicine

Active Publication Date: 2013-04-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the polyethylene glycol-polyester polymer micellar drug delivery system with the function of reversing tumor multidrug resistance has not been reported yet.

Method used

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  • Polymeric micelle medicine composition and preparation method thereof
  • Polymeric micelle medicine composition and preparation method thereof
  • Polymeric micelle medicine composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 Synthesis of monomethoxypolyethylene glycol-polylactic acid block copolymer (mPEG2000-PDLLA2482)

[0061] Take 4 g of monomethoxypolyethylene glycol (Mw 2000), place it at 120 °C for 3 hours in vacuum, add 6 g of lactide monomer and 5 μl of stannous isooctanoate (equivalent to 0.063% of the total amount of monomer) in In the polymerization tube, vacuumize for 30 minutes, seal the tube, and polymerize at 140°C for 6 hours. The polymerized product was dissolved in 20ml of dichloromethane, dropped into pre-cooled excess ether, and the product was precipitated at -20°C. The precipitate was filtered and washed with ether. The operation was repeated three times, and then the filter residue was dried under reduced pressure at room temperature for 48 hours to obtain a block copolymer mPEG-PDLLA with high purity (the yield was about 78%). NMR results see figure 1 , the gel permeation chromatography results of the polymer are shown in figure 2 .

Embodiment 2

[0062] Example 2 Synthesis of monomethoxypolyethylene glycol-polylactic acid block copolymer (mPEG5000-PDLLA3034)

[0063] Take 3 g of monomethoxypolyethylene glycol (Mw 5000), place it at 120 °C for 3 hours in vacuum, add 7 g of lactide monomer and 5 μl of stannous isooctanoate (equivalent to 0.063% of the total amount of monomer) in In the polymerization tube, vacuumize for 30 minutes, seal the tube, and polymerize at 140°C for 6 hours. The polymerized product was dissolved in 20ml of dichloromethane, dropped into pre-cooled excess ether, and the product was precipitated at -20°C. The precipitate was filtered and washed with ether. The operation was repeated three times, and then the filter residue was dried under reduced pressure at room temperature for 48 hours to obtain a block copolymer mPEG-PDLLA with high purity (the yield was about 88%).

[0064] The structure of mPEG2000 / 5000-PDLLA block copolymer is as follows:

[0065]

Embodiment 3

[0066] Example 3 Synthesis of polylactic acid-polyethylene glycol-polylactic acid block copolymer (PDLLA550-PEG2000-PDLLA550)

[0067] Take 6g of polyethylene glycol (Mw 2000), put it under vacuum drying at 120°C for 3 hours, add 4g of lactide monomer, 5μl of stannous isooctanoate (equivalent to 0.063% of the total amount of monomer) in the polymerization tube, Vacuum for 30 minutes, seal the tube, and polymerize at 140°C for 6 hours. The polymerized product was dissolved in 20ml of dichloromethane, dropped into pre-cooled excess ether, and the product was precipitated at -20°C. The precipitate was filtered and washed with ether. The operation was repeated three times, and then the filter residue was dried under reduced pressure at room temperature for 48 hours to obtain the block copolymer PDLLA-PEG-PDLLA (the yield was about 85%).

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Abstract

The invention relates to a polymeric micelle medicine composition encapsulating hydrophobic anti-tumour drug and multidrug resistance reversal agent pluronic at the same time and a preparation method thereof. The polymeric nano micelle composition contains polyethylene glycol-polyester segmented copolymer (or derivative thereof), tumour multidrug resistance reversal agent pluronic and anti-tumour drug. The functional anti-tumour drug nano micelle provided by the invention can effectively reverse multidrug resistance phenomenon of tumour, achieves the aim of targeted high-efficiency tumour treatment and has greater advantage compared with a common anti-tumour drug polymeric micelle preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a polymer micelle composition loaded with antitumor drugs and a tumor multidrug resistance reversal agent and a preparation method thereof. The polymer micelle composition has the ability to reverse tumor multidrug resistance features. Background technique [0002] Malignant tumors are common and frequently-occurring diseases that seriously threaten human life and health, and have become the leading cause of human death worldwide. At present, the clinical treatment of malignant tumors is still dominated by chemotherapy. However, most anticancer drugs have extremely poor water solubility, which brings great inconvenience to the development and clinical use of their preparations. For example, a large amount of surfactants are added to the formulations of taxane antineoplastic drugs on the market to increase the solubility of the drugs. Paclitaxel injection Taxol (Taxol) is to diss...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/34A61P35/00
Inventor 乔明曦陈大为朱嘉程亮赵秀丽胡海洋
Owner SHENYANG PHARMA UNIVERSITY
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