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Folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle and preparation method thereof

An anti-tumor drug and tumor-targeting technology, applied in the field of medicine, achieves the effect of less operation steps, convenient separation, and favorable promotion and application

Inactive Publication Date: 2017-11-24
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Superparamagnetic iron oxide nanoparticles SPIONs are widely used as magnetic resonance imaging contrast agents, but have not been reported as targeting carriers for insoluble drug PTX

Method used

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  • Folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle and preparation method thereof
  • Folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle and preparation method thereof
  • Folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle and preparation method thereof

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Embodiment 1

[0034] The folic acid-mediated antitumor drug superparamagnetic tumor-targeting nanoparticles of the present invention comprises the following steps:

[0035] A. Mix 12g of polyethylene glycol and 0.1g of polyethyleneimine evenly, and heat up to 78°C within 8 minutes to obtain a mixed solution; add 0.5g of iron acetylacetonate to the mixed solution, and continue stirring at 78°C for 8 minutes , heated to 250°C, kept warm for 0.5h, stopped heating, cooled to 50°C, obtained a mixed solution containing iron oxide nanoparticles, removed unreacted organic matter, collected iron oxide nanoparticles, dispersed them in deionized water to obtain oxidation Iron nanoparticle solution; the whole process is carried out under magnetic stirring, and argon gas is introduced to remove oxygen;

[0036]B. Mix 18mg of folic acid, 3mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 1mg of N-hydroxysuccinimide with 3g of deionized water, adjust with NaOH pH to 9, stirring in a dark...

Embodiment 2

[0040] The folic acid-mediated antitumor drug superparamagnetic tumor-targeting nanoparticles of the present invention comprises the following steps:

[0041] A. Mix 13g of polyethylene glycol and 0.2g of polyethyleneimine evenly, and heat up to 79°C within 9 minutes to obtain a mixed solution; add 0.6g of iron acetylacetonate to the mixed solution, and continue stirring at 79°C for 9 minutes , heated to 255°C, kept warm for 0.8h, stopped heating, cooled to 52°C, obtained a mixed solution containing iron oxide nanoparticles, removed unreacted organic matter, collected iron oxide nanoparticles, dispersed them in deionized water to obtain oxidation Iron nanoparticle solution; the whole process is carried out under magnetic stirring, and argon gas is introduced to remove oxygen;

[0042] B. Mix 19mg of folic acid, 3.2mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 2mg of N-hydroxysuccinimide with 4g of deionized water, and wash with NaOH Adjust the pH to 10, s...

Embodiment 3

[0046] The folic acid-mediated antitumor drug superparamagnetic tumor-targeting nanoparticles of the present invention comprises the following steps:

[0047] A. Mix 14g polyethylene glycol and 0.3g polyethyleneimine evenly, and heat up to 80°C within 10min to obtain a mixed solution; add 0.7g iron acetylacetonate to the mixed solution, and continue stirring at 80°C for 10min , heated to 260°C, kept warm for 1h, stopped heating, cooled to 54°C, obtained a mixed solution containing iron oxide nanoparticles, removed unreacted organic matter, collected iron oxide nanoparticles, and dispersed them in deionized water to obtain iron oxide Nanoparticle solution; the whole process is carried out under magnetic stirring, and argon gas is introduced to remove oxygen;

[0048] B. Mix 20mg of folic acid, 3.5mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 3mg of N-hydroxysuccinimide and 5g of deionized water, and wash with NaOH Adjust the pH to 10, stir in a dark room a...

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Abstract

The invention discloses a folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle. A superparamagnetic iron oxide nanoparticle is adopted as the carrier, and high temperature thermal decomposition method is employed to synthesize polyethylene glycol-polyethyleneimine modified uperparamagnetic iron oxide nanoparticle, then a folic acid ligand is grafted on the surface of iron oxide by chemical method, and then an antitumor drug is loaded into the iron oxide nanoparticle by electrostatic adsorption and hydrogen bonding, thus obtaining the folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle. According to the invention, the dual targeting effect can strengthen the anti-tumor effect of the antitumor drugs, and the folic acid mediated antitumor drug superparamagnetic tumor targeted nanoparticle has small toxic and side effect, thus being a tumor treatment nanoparticle preparation with substantial development value.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a folic acid-mediated antitumor drug superparamagnetic tumor-targeting nanoparticle and a preparation method thereof. Background technique [0002] One of the biggest killers that threaten human life and health is tumor. Chemical drugs are an indispensable means of treating nasopharyngeal carcinoma. However, chemical drugs are non-specific to cancerous cells and normal human cells, so that they not only kill cancerous cells during treatment, but also It also kills normal cells, causing serious toxic and side effects throughout the body. In recent years, searching for safe and effective targeted drugs has become a hotspot in the treatment of tumors. [0003] The nano drug delivery system can realize the control of drug delivery and release at the molecular level, and the passive or active targeting of the drug at the tumor site can be achieved through carrier modifica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/02A61K47/22A61K47/10A61K47/34A61K47/60A61K47/59A61K31/337A61K41/00A61P35/00
CPCA61K41/0052A61K9/0009A61K9/501A61K9/5015A61K9/5031A61K31/337A61K2300/00
Inventor 徐勤张宝林苑灿灿苏礼超
Owner GUILIN MEDICAL UNIVERSITY
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