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

A targeted drug delivery and tumor cell technology, which is applied in the direction of anti-tumor drugs, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. Drug properties, reversing drug resistance, and improving the effect of anti-tumor drug efficacy

Inactive Publication Date: 2007-11-07
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
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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 cell nucleus targeting administration system capable of reversing tumor cell resistance

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Embodiment

[0016] Example: Oligochitosan-fatty acid graft drug-loaded micelles in anti-tumor drug effects (breast cancer cells, MCF-7 cells) and reverse drug resistance of drug-resistant cells (breast cancer drug-resistant cells, MCF-7-adr cells) application in sex

[0017] 1) Preparation of low molecular weight chitosan (chitooligosaccharide)

[0018] Get 90g of chitosan (92.5% degree of deacetylation) with a commercially available molecular weight of 450kDa, add it to 3000mL of 1.25% (v / v) hydrochloric acid aqueous solution, under the temperature condition of 55~60°C, after swelling for 2 hours, Add 5% cellulase (w / w), and degrade at a temperature of 55-60°C. Control the reaction temperature and time to obtain low molecular weight chitosan (chitooligosaccharide). The resulting degradation reaction solution was fractionated by ultrafiltration using 50Kda and 10Kda ultrafiltration membranes (Biomax-10, Millipore Co., USA), and the ultrafiltrate with a molecular weight of 10-50Kda was t...

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Abstract

The present invention is application of cell nucleus targeting administration system in antitumor medicine capable of reversing tumor cell resistance. The cell nucleus targeting administration system consists of cell nucleus targeting administration carrier and enveloped antitumor medicine, and the cell nucleus targeting administration carrier is chitosan-fatty acid grafting micelle. The chitosan-fatty acid grafting micelle of the present invention has low cytotoxicity, and cell nucleus targeting function of permeating cell membrane fast with less destruction by intracellular lysosome. The grafting micelle with hydrophobic kernel can envelop hydrophobic antitumor medicine targeting cell nucleus 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 cell nucleus-targeted drug delivery system, and relates to the application of a cell nucleus-targeted drug delivery system in the preparation of an antitumor drug whose molecular target is located in the nucleus and which 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 new drug delivery systems that can reverse the drug resistance of dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K45/00A61P35/00
Inventor 胡富强杜永忠袁弘游剑
Owner ZHEJIANG UNIV
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