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Application of cytoplasm targeting administration system capable of reversing tumor cell resistance

A technology for targeted drug delivery and tumor cells, which is applied to anti-tumor drugs, medical preparations with inactive ingredients, drug combinations, etc. drug resistance, improving antitumor efficacy

Inactive Publication Date: 2007-11-07
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although microparticles and nanoparticles prepared with chitosan as the basic material have been widely used in the research of drug carrier materials, due to the hydrophilic structure of chitosan itself, it is difficult for it to be taken up by cells in large quantities, and it is impossible to realize subcellular organelles. target

Method used

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  • Application of cytoplasm targeting administration system capable of reversing tumor cell resistance
  • Application of cytoplasm targeting administration system capable of reversing tumor cell resistance

Examples

Experimental program
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Effect test

Embodiment 1

[0017] Embodiment 1: chitosan oligosaccharide-fatty acid graft drug-loaded micelles in antitumor drug effect (breast cancer cell, MCF-7 cell) and reversal drug-resistant cell (breast cancer drug-resistant cell, MCF-7-adr cell) resistance application in medicine

[0018] 1) Preparation of oligochitosan-stearic acid graft and determination of physical and chemical properties

[0019] Get the chitosan oligosaccharide 0.4g that the average molecular weight is 34kDa, accurately weigh, add 30mL distilled water after stirring and dissolving, add the carbodiimide (the mol ratio of chitosan and carbodiimide is 1: 100) EDC), stirred to dissolve. According to chitooligosaccharide:stearic acid (molar ratio) 1:50, take stearic acid and dissolve it in 20mL absolute ethanol. The mixture of the above two solutions was reacted at a constant temperature of 80° C. for 5 hours under the condition of 400 rpm magnetic stirring, cooled to room temperature (25° C.), and continued to stir for 6 hour...

Embodiment 2

[0042] Example 2: Oligochitosan-fatty acid graft drug-loaded micelles in anti-tumor drug effect (ovarian cancer cells, SKOV-3 cells) and reverse drug-resistant cells (ovarian cancer drug-resistant cells, SKOV-3-adr cells) resistance application in medicine

[0043] 1) Preparation of oligochitosan-stearic acid graft

[0044] Take 0.4g of chitosan oligosaccharides with an average molecular weight of 34kDa, accurately weigh, add 30mL of distilled water to stir and dissolve, then add carbodiimide in proportion (the molar ratio of chitosan and carbodiimide is 1:100) (EDC), stirred to dissolve. According to chitooligosaccharide:stearic acid (molar ratio) 1:50, take stearic acid and dissolve it in 20mL absolute ethanol. The mixture of the above two solutions was reacted at a constant temperature of 80° C. for 5 hours under the condition of 400 rpm magnetic stirring, cooled to room temperature (25° C.), and continued to stir for 6 hours. The final reaction solution was placed in a ...

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Abstract

The present invention is application of cytoplasm targeting administration system in antitumor medicine capable of reversing tumor cell resistance. The cytoplasm targeting administration system consists of cytoplasm targeting administration carrier and enveloped antitumor medicine, and the cytoplasm targeting administration carrier is chitosan-fatty acid grafting micelle. The chitosan-fatty acid grafting micelle of the present invention has low cytotoxicity, and cytoplasm targeting function of permeating cell membrane fast with less destruction by intracellular lysosome. The grafting micelle with hydrophobic endoplasm can envelop hydrophobic antitumor medicine targeting cytoplasm to form medicine carrier micelle. The present invention can raise the curative effect of antitumor medicine and reverse the medicine resistance of tumor cell.

Description

technical field [0001] The invention belongs to the application of a cytoplasmic targeted drug delivery system, and relates to the application of a cytoplasmic targeted drug delivery system in the preparation of antitumor drugs whose molecular targets are located in the cytoplasm and can reverse the drug resistance of tumor cells. Background technique [0002] Tumor has always been a major disease that directly threatens human health. Due to the lack of molecular targeting of drugs themselves, tumor chemotherapy has major treatment problems such as low cure rate, multidrug resistance, and huge toxic and side effects. One of the important reasons for the failure of clinical chemotherapy is the resistance of tumor cells to chemotherapy drugs. The cause of death of most cancer patients is directly or indirectly related to the resistance of tumor cells to anti-tumor drugs. Therefore, finding and studying drug delivery systems that can reverse the drug resistance of drug-resista...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/36A61P35/00
Inventor 胡富强杜永忠袁弘游剑
Owner ZHEJIANG UNIV
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