Magnetic nano-carrier with targeted hydrophobic drug delivery to tumor and preparation method thereof

A magnetic nanocarrier, tumor targeting technology, applied in drug combinations, antitumor drugs, pharmaceutical formulations, etc., to reduce drug usage, reduce damage, and achieve the effect of magnetic targeting delivery

Inactive Publication Date: 2010-01-27
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there have been a large number of reports on the encapsulation of drugs by polymer micelles, but there are few reports on the simultaneous encapsulation of magnetic iron oxid...

Method used

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  • Magnetic nano-carrier with targeted hydrophobic drug delivery to tumor and preparation method thereof
  • Magnetic nano-carrier with targeted hydrophobic drug delivery to tumor and preparation method thereof
  • Magnetic nano-carrier with targeted hydrophobic drug delivery to tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] To high purity N 2 (purity≥99.999%, Changchun Juyang Gases Co., Ltd.) added iron acetylacetonate [Fe(acac) 3 ](1×10 -3 mol, purity ≥ 97%, Sigma-Aldrich Company), 1,2-dodecanediol (5×10 -3 mol, purity ≥ 90%, Sigma-Aldrich), oleic acid (3 × 10 -3 mol, analytically pure, Tianjin Guangfu Fine Chemical Research Institute), oleylamine (3 × 10 -3 mol, purity ≥ 70%, Sigma-Aldrich Company) mixing, benzyl ether (10 mL, purity 99%, Sigma-Aldrich Company), magnetic stirring. The mixture was heated at 200°C for 2h; then the N 2 , and then heated at about 300°C for 1h, stopped heating, and cooled to room temperature.

[0027] Add 20 mL of absolute ethanol to the three-necked flask, centrifuge at 14,000 rpm for 20 min, and discard the supernatant; add 25 μL of oleic acid, 25 μL of oleylamine, and 5 mL of n-hexane to the black precipitate to redissolve the black precipitate, centrifuge at 6,000 rpm for 10 min, and discard the supernatant; Add 10 mL of ethanol, centrifuge at 10,00...

Embodiment 2

[0031] Introduce high-purity N into the three-necked flask connected with the condenser in advance. 2 (purity ≥ 99.999%, Changchun Juyang Gas Co., Ltd.), make the three-necked bottle full of N 2 .

[0032] Weigh 2.0 g of MePEG (Mn=2000 g / mol, Sigma-Aldrich Company), 5.0 g of D-lactide (D, L-Lactide, ≥99.5 mol%, Beijing Yuanshengrong Technology Co., Ltd.), glycolide (Glycolide, ≥ 99.5mol%, Beijing Yuanshengrong Technology Co., Ltd.) 1.0g, the ratio of the substance of mixed lactide and glycolide is 4: 1, add N 2 In the protected three-neck flask, add 50mL toluene, 0.205mL stannous octoate [Sn(Oct) 2 , ~95%, Sigma-Aldrich], mixture N 2 Under protection, it was heated to toluene reflux (about 111° C.), and the reaction was carried out for 10 h. Heating was stopped to terminate the reaction. Add 100mL of methanol precipitation product to the three-neck flask, add 60mL of dichloromethane to the precipitate to dissolve it, filter the obtained solution with suction, add the obta...

Embodiment 3

[0034] Introduce high-purity N into the three-necked flask connected with the condenser in advance. 2 (purity ≥ 99.999%, Changchun Juyang Gas Co., Ltd.), make the three-necked bottle full of N 2 . Weigh 2.0 g of MePEG (Mn=2000 g / mol, Sigma-Aldrich Company), 5.0 g of D-lactide (D, L-Lactide, ≥99.5 mol%, Beijing Yuanshengrong Technology Co., Ltd.), glycolide (Glycolide, ≥ 99.5mol%, Beijing Yuanshengrong Technology Co., Ltd.) 1.0g, the ratio of the substance of mixed lactide and glycolide is 4: 1, add N 2 In the protected three-neck flask, add 50mL toluene, 0.05mL stannous octoate [Sn(Oct) 2 , ~95%, Sigma-Aldrich], mixture N 2 Under protection, it was heated to toluene reflux (about 111°C), and the reaction was carried out for 9h. Heating was stopped to terminate the reaction. Add 100mL of n-hexane precipitated product to the three-neck flask, add 60mL of dichloromethane to the precipitate to dissolve it, suction filter the obtained solution, add the obtained filtrate into h...

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Abstract

The invention belongs to the technical field of biomedical polymer material and nanobiomaterial, particularly relates to a magnetic nano-carrier with targeted hydrophobic drug delivery to tumor and a preparation method thereof. The magnetic nano-carrier is formed by encapsulating superparamagnetic nano-particles with amphiphilic segmented copolymer methoxy polye thylene glycol-poly(lactide- glycolide) (MePEG-PLGA) micelles. First, a large amount of MePEG-PLGA with good dispersion is synthesized by the improved solution polymerization process, and then the MePEG-PLGA is used as raw materials to encapsulate Fe3O4 nano-particles by the solvent evaporation process to obtain a magnetic nano drug carrier. The carrier is expected to solve the solubility problem of insoluble drugs, achieves slow release of drugs, and achieves the passive-targeting of the drugs by the EPR effect of tumor; Fe3O4 nano-particles are used in the active-targeting of the drugs to reduce the dosage and the side effect and improve the treatment efficiency; besides, the carrier can be used in the magnetic resonance imaging (MRI) of tumor.

Description

technical field [0001] The invention belongs to the field of biomedical polymer materials and nano-biotechnology, and in particular relates to a magnetic nanocarrier for tumor-targeted delivery of hydrophobic drugs and a preparation method thereof. Background technique [0002] Cancer remains one of the most terrifying diseases and a major threat to human life. Cancer is the leading cause of death in the United States for people under the age of 85, surpassing heart disease as the number one killer for the first time. This worrying statistic is not because cancer rates have risen, but because deaths from heart disease have fallen by nearly half while cancer-related deaths have remained virtually unchanged. Chemotherapy, the traditional standard therapy for most cancers, is not always successful even after more than 50 years of research, because traditional chemotherapy indiscriminately delivers toxic anticancer drugs to tumors and normal organs and tissues, thus damaging no...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/02A61K49/12A61P35/00
Inventor 徐力郭轶丁国斌吕言云张学忠
Owner JILIN UNIV
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