Polyethylene glycol nano drug delivery system with enhanced anti-tumor effect and preparation method thereof

A nano-drug delivery system and polyethylene glycol technology, applied in the field of biomedicine, can solve the problems of unsatisfactory anti-tumor effect of chemotherapeutic drugs, tumor drug resistance restricting clinical tumor treatment, etc., to achieve enhanced anti-tumor effect and good tumor Penetration, improve the effect of distribution

Inactive Publication Date: 2019-03-29
JIANGSU VOCATIONAL COLLEGE OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Polyethylene glycol nano drug delivery system with enhanced anti-tumor effect and preparation method thereof
  • Polyethylene glycol nano drug delivery system with enhanced anti-tumor effect and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] This embodiment relates to a tumor-targeted polyethylene glycol nano drug delivery system with the function of enhancing anti-tumor effect,

[0024] Specifically, the drug delivery system includes: functionalized polyethylene glycol (A) as a carrier molecule, phototherapeutic agent (B) as a drug, and RGD polypeptide (C) as a target.

[0025] The polyethylene glycol nano drug delivery system is prepared through the following steps:

[0026] a. The RGD polypeptide containing maleimide group (C) (produced by Peptides International, USA) and the sulfhydryl group of polyethylene glycol (A) (produced by Creative PEGWorks, USA) were mixed in a ratio of 10:1 React in pH7.0-8.0 buffer for 30-60 minutes; in this example, the functionalized polyethylene glycol (A) can be linear or multi-armed polyethylene glycol, including but not limited to HS-PEG - Any of NH2, 4-arm PEG, 2 arm-NH2, 2 arm-SH or 8-arm PEG, 4 arm-NH2, 4 arm-SH. In addition, RGD(C) includes cRGDfK-Mal or cRGDyK-Ma...

Embodiment 2

[0030] This example relates to a tumor-targeted polyethylene glycol nano drug delivery system with the function of enhancing anti-tumor effect. Specifically, the drug delivery system includes: functionalized polyethylene glycol (A) as carrier molecule, phototherapeutic agent (B) is the drug, with RGD polypeptide (C) as the target.

[0031] The polyethylene glycol nano drug delivery system is prepared through the following steps:

[0032] a. React the maleimide group-containing RGD polypeptide (C) with the sulfhydryl group of polyethylene glycol (A) in a pH 7.0-8.0 buffer solution for 30-60 minutes at a ratio of 3:1; In this example, the functionalized aforementioned polyethylene glycol (A) can be linear or multi-armed polyethylene glycol, including but not limited to HS-PEG-NH2, 4-arm PEG, 2 arm-NH2, 2 arm-SH or 8-armPEG, 4 arm-NH2, 4 arm-SH any material. In addition, RGD(C) includes cRGDfK-Mal or cRGDyK-Mal.

[0033] b. After the above reaction product is purified by a gel...

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Abstract

The invention relates to a polyethylene glycol nano drug delivery system with enhanced anti-tumor effect and a preparation method thereof. The drug delivery system takes functionalized polyethylene glycol as a carrier molecule, a phototherapy agent as a medicament and RGD polypeptide as a target head. The system can realize the enhancement of the anti-tumor effect, mainly because the polyethyleneglycol nano drug delivery system has small particle size, has good tumor penetrability, has active tumor targeting property, and can improve the distribution of the drugs in tumors so as to reach thetreatment concentration.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a polyethylene glycol nano drug delivery system with enhanced anti-tumor effect and a preparation method. Background technique [0002] Cancer is a major disease that endangers 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 antitumor effect of chemotherapy drugs is still unsatisfactory, and the generation of tumor drug resistance is the main obstacle restricting clinical tumor treatment. [0003] The structure of tumor tissue is complex, and a series of physical and physiological barriers inside make it difficult for chemotherapy drugs to penetrate the tumor and reach the inside of the tumor tissue, making tumor cells withstand sublethal doses of drug stimulation for a long time, which is an important reason for tumor drug resistance one. Therefore, delivering a suffi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/64A61K41/00A61P35/00
CPCA61K41/0042A61K47/64A61K47/6935A61P35/00
Inventor 李芳张冉明欣辛俊勃姜毅李若菡徐星星刘珂高杰潘富荣
Owner JIANGSU VOCATIONAL COLLEGE OF MEDICINE
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