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Gold nano-paclitaxel conjugate, and preparation method and application thereof

A technology of paclitaxel and conjugates, applied in gold nanometer-paclitaxel conjugates and the fields of preparation and application thereof, to achieve the effects of increasing concentration, improving bioavailability and pharmacokinetic properties

Inactive Publication Date: 2015-04-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, the product or clinical research of gold nanoparticles as a drug carrier has not been reported, and its preclinical research mainly focuses on the concentration, loading and delivery of gene drugs, while there are few reports related to chemotherapy drugs

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  • Gold nano-paclitaxel conjugate, and preparation method and application thereof
  • Gold nano-paclitaxel conjugate, and preparation method and application thereof
  • Gold nano-paclitaxel conjugate, and preparation method and application thereof

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Embodiment Construction

[0049] The present invention is further illustrated by way of examples below, but the present invention is not limited to the scope of the examples.

[0050] The present invention relates to a figure 1The design and construction of the gold nano-paclitaxel conjugate shown, the preparation method of each component of the conjugate, the preparation method of the conjugate, and its drug delivery application. The preparation of the gold nano-drug conjugate of the present invention includes: (1) preparation of the inner core of gold nanoparticles; (2) synthesis of thiolated biocompatible ligands; (3) synthesis of thiolated paclitaxel derivatives; (4) gold Preparation of nano drug conjugates.

[0051] The preparation method of gold nano-paclitaxel conjugate uses dihydrolipoic acid polyethylene glycol monomethyl ether ester as a biocompatible ligand, and 7-O-paclitaxel glutarate polyethylene glycol thioglycolic acid as a paclitaxel thiol derivative The gold nano-paclitaxel conjugat...

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Abstract

The present invention relates to design and construction of a gold nanoparticle-drug conjugate, which has solubilization on hard-soluble drug, increases unit volume concentration of the drug, improves bioavailability and pharmacokinetic properties of the drug, and has a size less than 30nm. The invention also relates to preparation methods of various components of the conjugate, a preparation method of the conjugate, and drug delivery application thereof.

Description

technical field [0001] The present invention relates to the design and construction of a gold nanoparticle-paclitaxel conjugate ( figure 1 ), which has a solubilizing effect on the insoluble drug paclitaxel, and the prepared gold nano-paclitaxel conjugate can increase the concentration of the drug per unit volume, improve the bioavailability and pharmacokinetic properties of the drug, and can be used for tumor treatment. Background technique [0002] Chemotherapy is an important method of cancer treatment, but most common solid tumors still lack effective drugs, and many antitumor drugs have poor solubility, develop drug resistance during clinical use, and have serious side effects. Therefore, it has become one of the important methods to solve the above problems to load anti-tumor drugs on nanocarriers with high selectivity and targeting, and accurately deliver them to the lesion to exert their drug effects. [0003] The current research is mainly to encapsulate insoluble ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/337A61K47/02A61K47/34A61P35/00
Inventor 丁娅张灿刘肇彧吴迪洪瑾张文婕
Owner CHINA PHARM UNIV