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Magnetic tumor double-target polymer nano micelle and preparation thereof

A nanomicelle and dual-targeting technology, which is applied in the fields of polymer chemistry and biomedical engineering, can solve problems such as difficult particle size control, low drug loading rate, and weak particle magnetism, so as to enhance tumor targeting effect and prolong Excellent blood circulation time and chain flexibility

Inactive Publication Date: 2010-01-06
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when used as a diagnostic contrast agent for magnetic resonance imaging, there are still problems to be solved, such as weak particle magnetism, low drug loading rate, poor release effect, and difficult to achieve precise control of particle size.

Method used

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  • Magnetic tumor double-target polymer nano micelle and preparation thereof
  • Magnetic tumor double-target polymer nano micelle and preparation thereof
  • Magnetic tumor double-target polymer nano micelle and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of folate-PEG-PCL or folate-PEG-PLA as folate-PEG-PCL or folate-PEG-PLA carrier materials for tumor dual-targeting nanomicelles modified by folic acid

[0030] (1) Preparation of allyl-terminated PEG homopolymer

[0031]Mix 4ml of tetrahydrofuran solution of potassium naphthyl with 0.5ml of allyl alcohol and stir in a dry reaction flask for 15 minutes. Then add 20ml of anhydrous tetrahydrofuran and 18-crown ether-6 tetrahydrofuran solution (containing 1.5g 18-crown ether-6 and 5ml anhydrous tetrahydrofuran) under the protection of argon, and after stirring for 15 minutes, place the mixture in an ice-salt bath Cool, and slowly pass through dry ethylene oxide, and maintain low temperature for 24 hours so that the polymerization reaction continues. Finally, it was left at room temperature for 3 days.

[0032] (2) Preparation of allyl-PEG-PCL or allyl-PEG-PLA amphiphilic block copolymer terminated by allyl group

[0033] Under the protection of argon, dry 0.2...

Embodiment 2

[0039] Preparation of tumor dual-targeting polymer nano drug-loaded micelles

[0040] (1) Preparation of superparamagnetic Fe3O4 nanoparticles SPIO

[0041] Mix 0.7g iron acetylacetonate, 2.9g 1,2-hexadecanediol, 2ml oleic acid, 2ml oleylamine and 20ml dibenzyl ether under nitrogen protection and heat at 200°C for two hours, then raise the temperature to 300°C Reflux for one hour. After the obtained black product was cooled to room temperature, it was reprecipitated in ethanol, centrifuged to remove excess solvent, dissolved in n-hexane and sealed for storage.

[0042] (2) Preparation of tumor dual-targeting polymer nano drug-loaded micelles

[0043] Dissolve 10mg of folate-PEG-PCL or folate-PEG-PLA, 2mg of anticancer drugs, 1.3ml of triethylamine, and 1.5mg of SPIO in a mixed solvent containing 1.0ml of tetrahydrofuran and 1.0ml of dimethyl sulfoxide. Slowly added dropwise to 5ml deionized water. Then, they were dialyzed in deionized water for 2 days to remove organic sol...

Embodiment 3

[0045] Test experiment of basic properties of tumor dual-targeting polymer nano drug-loaded micelles

[0046] The particle size of the obtained micelles is measured by a dynamic light scattering system, and its shape is determined by observation with a transmission electron microscope. The test results are shown in figure 1 .

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Abstract

The invention relates to a nanomicelle of magnetic tumor double-targeting polymer and a preparation method thereof. The nanomicelle of magnetic tumor double-targeting polymer is a nuclear shell structure; the surface of an outer shell is connected with targeted ligand, an inner core is enclosed with nano-particles of super paramagnetic ferriferrous oxide and anticarcinogen with hydrophobic property; in virtue of the physical effect of an external magnetic field and induction of the targeting ligand, the tumor double-targeting function of the nanomicelle is realized. The invention also provides the preparation method of the nanomicelle of magnetic tumor double-targeting polymer: polyethylene glycol with end capping by folacin, and poly Epsilon-caprolactone or sandwich copolymer of poly propiolactone are taken as raw materials and enclosed with the nano-particles of super paramagnetic ferriferrous oxide and the anticarcinogen with hydrophobic property, and then dialysed to obtain the nanomicelle of magnetic tumor double-targeting polymer. The drug carrier system of the nanomicelle reinforces the treatment effect of the anticarcinogen with hydrophobic property on tumor, prolongs the circulating time of the anticarcinogen in human body, intensifies the targeting action of drugs, improves the release efficiency and partial concentration of drugs, and reduces the dosage and toxic and side effect of drugs.

Description

technical field [0001] The invention relates to a drug carrier and a preparation method thereof, in particular to a magnetic tumor double-targeting polymer nano-micelle and a preparation method thereof, belonging to the fields of polymer chemistry and biomedical engineering. Background technique [0002] Cancer is one of the most important diseases that endanger the health of all human beings. At present, there are more than 10 million new cancer patients in the world every year, and more than 6 million deaths. The seriousness of the harm and the difficulty of treatment have attracted great attention from the public, government and scientific circles in many countries. The development of means that can treat such diseases more effectively is of great significance to the promotion of human health. [0003] Anticancer drugs Chemotherapy is the most important cancer treatment after surgery. At present, most small molecule anticancer drugs are poor in water solubility, and sur...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/02A61K9/107A61K9/127A61P35/00
Inventor 帅心涛李皓杨小强
Owner SUN YAT SEN UNIV
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