Legumain responsive release adriamycin sustained-release nano preparation and preparation method and application in serving as drug for preparing carrier

A nano-formulation, doxorubicin technology, used in drug combination, liquid delivery, anti-tumor drugs, etc., can solve the problems of no passive targeting effect, no long-term sustained release, etc., to reduce secondary damage, high biological Effects of Compatibility and Safety

Active Publication Date: 2016-07-06
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the product of this design is still a small molecule drug, which does not have the passive targeting effect of

Method used

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  • Legumain responsive release adriamycin sustained-release nano preparation and preparation method and application in serving as drug for preparing carrier
  • Legumain responsive release adriamycin sustained-release nano preparation and preparation method and application in serving as drug for preparing carrier
  • Legumain responsive release adriamycin sustained-release nano preparation and preparation method and application in serving as drug for preparing carrier

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[0021] A Legumain response to release doxorubicin sustained-release nano-formulation, its chemical structure is as follows:

[0022] .

[0023] According to the above technical roadmap, the preparation process can be divided into the following four parts:

[0024] 1. Design and synthesis of Legumain substrate peptide

[0025] According to Legumain's structure and catalytic properties, the design of synthetic substrate peptides is based on the design principle: take asparagine as the center and connect several neutral amino acids on both sides.

[0026] Synthesis of peptide derivatives of doxorubicin

[0027] (1) Weigh out Dox·HCl (579mg or 1mmol) and Fmoc-AAN(Trt)-L-OH (PEP: Phosphoenolpyruvate) (923mg or 1mmol) and dissolve them in DMF (50ml), add DIPEA (Ie N,N-diisopropylethylamine) (0.36ml or 2mmol), stir magnetically for 15min (room temperature, protected from light), add HATU (chemical name is 2-(7-azobenzotriazole) -N,N,N',N'-tetramethylurea hexafluorophosphate) solution (0.42g ...

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Abstract

The invention provides a Legumain responsive release adriamycin sustained-release nano preparation and a preparation method and application in serving as a drug for preparing a carrier. By means of the biological characteristic that tumor tissue highly expresses Legumain, Legumain responsive nano-hydrogel is prepared, the double targeting effect (active targeting and passive targeting) of the tumor tissue is achieved, and secondary damage of adriamycin to normal tissue is reduced; hyaluronic acid serves as the base material of an adriamycin drug carrier, hyaluronic acid widely exists in normal tissue of organisms, and hyaluronic acid has high biocompatibility and safety compared with other foreign materials; the tumor tissue further highly expresses a hyaluronic acid receptor, and therefore the targeting effect can be further achieved by taking hyaluronic acid as the carrier material.

Description

technical field [0001] The present invention relates to the field of hyaluronic acid-based environmental factor-responsive nano hydrogel drug sustained-release system, in particular to a Legumain response-release doxorubicin sustained-release nano-preparation and its preparation method and as a carrier drug for the preparation of anti-tumor drug sustained-release Applications. Background technique [0002] Adriamycin is a commonly used broad-spectrum anti-tumor chemical drug. However, as a strong cytotoxic drug, doxorubicin can cause irreversible damage to normal tissues (such as heart, liver, kidney, and normal tissues around tumors, etc.). harm. How to target drugs to tumor tissues and reduce secondary damage to normal tissues is a major difficulty in the drug treatment of malignant tumors. Due to the "infiltration and retention enhancement effect" of malignant tumor tissue, the drug-carrier system at the nanoscale can penetrate the neovascular wall of tumor tissue but n...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61K9/06A61P35/00
CPCA61K31/704
Inventor 林森南开辉陈浩李彤谢佩玲
Owner WENZHOU MEDICAL UNIV
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