Dextran fatty acid graft, preparation method and application

A fatty acid and dextran technology, applied in the field of preparation of anti-tumor pharmaceutical compositions, can solve the problems of unfavorable target cell uptake

Inactive Publication Date: 2011-12-07
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the hydrophilic surface properties of polymeric micelles are not conducive to the target cell uptake of carrier materials.

Method used

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  • Dextran fatty acid graft, preparation method and application
  • Dextran fatty acid graft, preparation method and application
  • Dextran fatty acid graft, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Accurately weigh 175.5mg of stearic acid, 381.8mg of DCC, 22.5mg of DMAP and 500mg of dextran (Mw=10000) into a 250ml dry round bottom flask, then add 45ml of dehydrated DMSO, heat and ultrasonically dissolve, add a small amount of anhydrous sodium sulfate. React at 60° C. for 8 h in a constant temperature heating magnetic stirrer, and protect with nitrogen. After the reaction, the reaction product was dialyzed for 48 hours with a dialysis bag (MWCO 3.5Kda, American Spectrum Laboratories Inc.), and the water was changed continuously to remove DMSO and water-soluble by-products. After dialysis, the reaction product was filtered with a 0.8 μm water membrane to remove insoluble substances such as DCC and then freeze-dried. The freeze-dried product was washed three times with ethanol to remove unreacted stearic acid. Finally, the reaction product is dissolved in deionized water and freeze-dried to obtain the dextran stearic acid graft

Embodiment 2

[0027] Accurately weigh 87.8mg of stearic acid, 191.5mg of DCC, 11.2mg of DMAP and 500mg of dextran (Mw=20000) into a 250ml dry round bottom flask, then add 45ml of dehydrated DMSO, heat and ultrasonically dissolve, add a small amount of anhydrous sodium sulfate. React at 60° C. for 8 h in a constant temperature heating magnetic stirrer, and protect with nitrogen. After the reaction, the reaction product was dialyzed for 48 hours with a dialysis bag (MWCO 3.5Kda, American Spectrum Laboratories Inc.), and the water was changed continuously to remove DMSO and water-soluble by-products. After dialysis, the reaction product was filtered with a 0.8 μm water membrane to remove insoluble substances such as DCC and then freeze-dried. The freeze-dried product was washed three times with ethanol to remove unreacted stearic acid. Finally, the reaction product is dissolved in deionized water and freeze-dried to obtain the dextran stearic acid graft

Embodiment 3

[0029]Accurately weigh 175.5mg of stearic acid, 381.8mg of DCC, 22.5mg of DMAP and 500mg of dextran (Mw=20000) into a 250ml dry round bottom flask, then add 45ml of dehydrated DMSO, heat and ultrasonically dissolve, add a small amount of anhydrous sodium sulfate. React at 60° C. for 8 h in a constant temperature heating magnetic stirrer, and protect with nitrogen. After the reaction, the reaction product was dialyzed for 48 hours with a dialysis bag (MWCO 3.5Kda, American Spectrum Laboratories Inc.), and the water was changed continuously to remove DMSO and water-soluble by-products. After dialysis, the reaction product was filtered with a 0.8 μm water membrane to remove insoluble substances such as DCC and then freeze-dried. The freeze-dried product was washed three times with ethanol to remove unreacted stearic acid. Finally, the reaction product is dissolved in deionized water and freeze-dried to obtain the dextran stearic acid graft

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Abstract

The invention provides a dextran fatty acid graft. The weight-average molecular weight of the dextran is 10000Da-4000Da, and the grafting rate of the fatty acid is 1-10%. The present invention adopts dextran with good biocompatibility as the hydrophilic material, and utilizes chemical grafting technology to controllably synthesize amphiphilic dextran fatty acid grafts, which have self-aggregation formation in aqueous media. polymer micelles, and has a lower critical micelle concentration, the dextran fatty acid graft can be used as a drug carrier, combined with anti-tumor drugs, and applied to the preparation of anti-tumor drug compositions, to achieve the control of drug active components in the The release in vivo can realize the passive targeting of drugs and reduce the toxic and side effects of drugs. The structural formula of the dextran fatty acid graft of the present invention:

Description

technical field [0001] The invention belongs to compound synthesis, and relates to a synthesis method of a dextran fatty acid graft and an application of the dextran fatty acid graft in preparing an antitumor drug composition. Background technique [0002] Drugs are mainly administered through three routes of oral administration, injection, and mucosal administration in appropriate pharmaceutical dosage forms to achieve systemic or local therapeutic effects. The traditional (drug + excipient) method of preparing common preparations is affected by biofilm absorption and transport barriers, enzyme metabolism, and normal organ distribution, resulting in low curative effect and large doses due to the inability of drugs to enter their molecular targets in large quantities. , and the non-selectivity of drug distribution leads to serious toxic side effects. [0003] Cancer is one of the most common causes of death affecting human health and causing death. There are more than 10 mi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/02A61K47/36A61P35/00
Inventor 杜永忠袁弘胡富强
Owner ZHEJIANG UNIV
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