Nanometer drug delivering system capable of realizing high tumor permeability and preparation method

A nano-drug delivery system and permeability technology, which is applied in the field of nano-drug delivery system and preparation with high tumor permeability, can solve the problems of tumor drug resistance restricting clinical tumor treatment and unsatisfactory anti-tumor effect of chemotherapy drugs, and achieve Good tumor penetration, small particle size, high tumor penetration effect

Inactive Publication Date: 2019-05-03
JIANGSU VOCATIONAL COLLEGE OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some substantial progress has been made in the treatment of cancer in the past few decades, the antitumor effect of chemotherapy drugs is still unsatisfactory, and the generation of tumor drug resistance is the main obstacle restricting clinical tumor treatment.

Method used

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  • Nanometer drug delivering system capable of realizing high tumor permeability and preparation method
  • Nanometer drug delivering system capable of realizing high tumor permeability and preparation method
  • Nanometer drug delivering system capable of realizing high tumor permeability and preparation method

Examples

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Embodiment 1

[0026] This embodiment relates to a nano drug delivery system with high tumor permeability and a preparation method thereof.

[0027] A method for preparing a nano-drug delivery system with high tumor permeability includes the following steps:

[0028] a. The phototherapeutic agent containing NHS active ester (B) (produced by LI-COR, USA) and functionalized polyethylene glycol (A) containing both amino and maleimide groups (produced by Creative PEGWorks, USA) React for 30 minutes in pH 7.0-8.0 buffer. The ratio of the NHS active ester of the phototherapeutic agent (B) to the amino group of the functionalized polyethylene glycol (A) is 10:1. It may be preferred that the functionalized polyethylene glycol (A) is linear or multi-arm polyethylene glycol. Further, the functionalized polyethylene glycol (A) may include Mal-PEG-NH2, 4-arm PEG, 2 arm-NH2, 2 arm-Mal or 8-arm PEG, 4 arm-NH2, 4arm-Mal Any substance. The phototherapeutic agent (B) includes either IRDye700-NHS or IRDye800-N...

Embodiment ２

[0033] This embodiment relates to a nano drug delivery system with high tumor permeability and a preparation method thereof.

[0034] A method for preparing a nano-drug delivery system with high tumor permeability includes the following steps:

[0035] a. The phototherapeutic agent (B) containing NHS active ester and the functionalized polyethylene glycol (A) containing both amino and maleimide groups are reacted in a pH 7.0-8.0 buffer for 60 minutes. The ratio of the NHS active ester of the phototherapy agent (B) to the amino group of the functionalized polyethylene glycol (A) is 2:1. It may be preferred that the functionalized polyethylene glycol (A) is linear or multi-arm polyethylene glycol. Further, the functionalized polyethylene glycol (A) may include Mal-PEG-NH2, 4-arm PEG, 2 arm-NH2, 2 arm-Mal or 8-arm PEG, 4 arm-NH2, 4 arm-Mal Any substance. The phototherapeutic agent (B) includes either IRDye700-NHS or IRDye800-NHS.

[0036] b. Purify the material obtained in step a th...

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Abstract

The invention relates to a nanometer drug delivering system capable of realizing high tumor permeability and a preparation method. The method comprises the following steps of a, enabling a phototherapy agent containing NHS active ester and functional polyethylene glycol containing amino and maleimide groups to react in a buffer solution of which the pH is 7.0-8.0 for 30-60 minutes; b, purifying substances obtained in the step a through a gel column, immediately adding RGD polypeptide containing thiol groups, and performing a light-avoiding reaction for 1 hour; and c, purifying the products obtained by the reaction in the step b through the gel column so as to obtain the polyethylene glycol nanometer drug delivering system targeted with an integrin acceptor. The nanometer drug delivering system can realize high tumor permeability, mainly the particle diameter of the polyethylene glycol nanometer drug delivering system is small, and the nanometer drug delivering system has favorable tumor penetrability.

Description

Technical field [0001] The invention relates to the field of biomedicine, in particular to a nanometer drug delivery system with high tumor permeability and a preparation method. Background technique [0002] Cancer is a major disease endangering human health, and its incidence is increasing year by year. Although some substantial progress has been made in the treatment of cancer in the past few decades, the anti-tumor effects of chemotherapeutics are still unsatisfactory. Among them, the emergence of tumor drug resistance is the main obstacle that restricts clinical tumor treatment. [0003] The structure of tumor tissue is complex, and a series of internal physical and physiological barriers make it difficult for chemotherapeutic drugs to penetrate the tumor and reach the inside of the tumor tissue, causing tumor cells to withstand sublethal doses of drug stimulation for a long time, which is an important reason for tumor resistance one. Therefore, delivering sufficient doses o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/10A61K47/18A61K41/00A61P35/00
Inventor 辛俊勃李芳张冉赵如徐星星明欣刘珂李若菡高杰潘富荣
Owner JIANGSU VOCATIONAL COLLEGE OF MEDICINE
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