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Folic acid-mediated (polyethylene glycol) PEG-graphene oxide doxorubicine-loaded nanoparticle and preparation method thereof

A technology of PEG- and doxorubicin, which is applied in the field of medicine, can solve the problems of human side effects, poor curative effect, and drug resistance of tumor cells, and achieve the effects of reducing side effects, improving drug targeting, and prolonging plasma half-life

Active Publication Date: 2014-05-14
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The anti-tumor chemotherapeutic drugs currently used in clinical practice have obvious killing effect on tumor cells, but they cannot selectively avoid normal tissue cells, causing serious toxic and side effects to the human body, poor curative effect, and prone to drug resistance of tumor cells

Method used

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  • Folic acid-mediated (polyethylene glycol) PEG-graphene oxide doxorubicine-loaded nanoparticle and preparation method thereof
  • Folic acid-mediated (polyethylene glycol) PEG-graphene oxide doxorubicine-loaded nanoparticle and preparation method thereof
  • Folic acid-mediated (polyethylene glycol) PEG-graphene oxide doxorubicine-loaded nanoparticle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Take about 1.2 mg of DOX, weigh it accurately, dissolve it in 8 mL of PBS buffer with pH 7.0, mix it with 1.2 mg of the carrier material PEG-GO-FA, place it on a magnetic stirrer, and heat it at room temperature at 300 r min -1 Stir in the dark for 48 hours, filter through a polymer ultrafiltration membrane (≥100k), collect the filter cake and filtrate respectively, wash the filter cake repeatedly with buffer solution to obtain DOX*PEG-GO-FA nanoparticles, and store the product at 4 °C.

Embodiment 2

[0028] Take about 2.4 mg of DOX, weigh it accurately, dissolve it with 8 mL of PBS buffer with pH 7.0, mix it with 1.2 mg of the carrier material PEG-GO-FA, place it on a magnetic stirrer, and heat it at room temperature at 700 r min -1 Stir in the dark for 24 hours, filter through a polymer ultrafiltration membrane (≥100k), collect the filter cake and filtrate respectively, and wash the filter cake repeatedly with buffer solution to obtain DOX*PEG-GO-FA nanoparticles. The product was stored at 4°C.

Embodiment 3

[0030] Take about 3.6 mg of DOX, weigh it accurately, dissolve it with 8 mL of PBS buffer with pH 7.0, mix it with 1.2 mg of the carrier material PEG-GO-FA, place it on a magnetic stirrer, and set it at room temperature at 1400 r min -1 Stir in the dark for 12 hours, filter through a polymer ultrafiltration membrane (≥100k), collect the filter cake and filtrate respectively, and wash the filter cake repeatedly with buffer solution to obtain DOX*PEG-GO-FA nanoparticles. The product was stored at 4°C.

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Abstract

The invention relates to a folic acid-mediated (polyethylene glycol) PEG-graphene oxide doxorubicine-loaded nanoparticle and a preparation method thereof. The preparation method includes carrying out functional modification on graphene oxide with folic acid and PEG, and loading a model drug doxorubicine. According to the invention, the drug loading capacity of the nanoparticle is increased, drug targeting property is improved, and the half-life of plasma and mean residence time are remarkably prolonged, so as to improve the curative effect of doxorubicine. The invention can reduce the toxic and side effects of doxorubicine, and prolong the drug resistance time and improve drug targeting property, so as to enhance the antitumor effect of doxorubicine. The invention has important clinical significance for some medicaments with wide antitumor spectrum but severe adverse effect and high toxicity.

Description

technical field [0001] The invention relates to folic acid-mediated PEG-graphene oxide-loaded doxorubicin nanoparticles and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Doxorubicin is also known as Doxrubincin (DOX), the chemical name is 10-[(3-amino-2,3,6-trideoxy-a-L-lesuhexyl)-oxygen]-7 ,8,9,10-Tetrahydro-6,8,11-trihydroxy-8-(glycolyl)-1-methoxy-5,12-naphthalenedione. DOX is a cycle non-specific anti-cancer chemotherapy drug. This product has effects on cells in all phases, but it is most sensitive to the early stage of S phase, followed by M phase, and has a delaying effect on G1, S and G2 phases. Its mechanism of action is that it can directly act on DNA, insert into the double helix strand of DNA, unwind its characteristic structure, change the template properties of DNA, and inhibit DNA polymerase, thereby inhibiting both DNA and RNA synthesis. In addition, this product has the function of forming superoxy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/704A61K47/34A61P35/00
Inventor 吴琳华纪宏宇唐景玲史士强石淑贞庄宇婷
Owner HARBIN MEDICAL UNIVERSITY
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