Organic metal carborane target formulation and its preparation method

An organometallic, carborane technology, applied in drug combinations, antineoplastic drugs, radioactive carriers, etc., can solve the problems that magnetic nanomaterial boron carrier has not been covered and reported, and can inhibit the growth of tumor cells, increase the retention rate, Good targeting effect

Inactive Publication Date: 2007-05-30
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Although the above method can effectively transport boron-containing compounds to some tumor cells, it is not the best method, and there are still many problems: for example, boron-containing compounds are usually required to have certain water solubility; liposome and receptor-mediated Although the system has a certain directionality, it is often enriched in the reticuloendothelial system after injection; the drug loading of liposomes is generally only 5%, and the rest are some inactive phospholipids and cholesterol and other large groups.
At present, in the research of BNCT, the application of magnetic nanomaterials to realize the targeted transport of boron carriers has not been involved or reported at home and abroad.

Method used

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  • Organic metal carborane target formulation and its preparation method
  • Organic metal carborane target formulation and its preparation method
  • Organic metal carborane target formulation and its preparation method

Examples

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Embodiment 1

[0041] Example 1 Preparation of organometallic carborane targeting formulations based on magnetic nanoparticles

[0042] According to the present invention, the organometallic carborane targeting preparation is prepared according to the following steps, and the organometallic carborane used has the structure shown in formula (I):

[0043]

[0044] (1) The Fe / Ru bimetallic center carborane with the structure shown in formula (I) is dissolved in DMSO to prepare a concentration of 2.0*10 -5 M solution;

[0045] (2) Use a high-purity Fe sheet as the anode, use glassy carbon as the cathode, and perform electrolysis in a 0.1M tetraheptylammonium-bromide (THA-Br) isopropanol (2-propanol) solution, and deposit magnetic nanoclusters. The as-deposited magnetic nanoclusters were heat-treated in water, and then the cluster powder was heated and annealed at about 200 °C to obtain surface-functionalized monodisperse Fe 3 o 4 magnetic nanoparticles. Its particle size ranges from 20nm...

Embodiment 2

[0048] Example 2 Preparation of organometallic carborane targeting formulations based on magnetic nanocomposites

[0049] The organometallic carborane targeting preparation based on the magnetic nanocomposite was prepared according to the method of Example 1, the difference being that the saturated suspension in the above step (2) was prepared as follows:

[0050] One-dimensional polylactic acid (PLA) nanofibers were prepared by electrospinning technology: PLA was dissolved in chloroform solvent with a concentration of 10% (wt%), and magnetically stirred for 2 hours. Then pour it into a 5ml syringe with a stainless steel needle with a diameter of 500um. The stainless steel needle is connected to the positive electrode of the voltage, the aluminum foil collection device is connected to the negative electrode of the voltage, the spinning voltage is 10KV, the collection distance from the needle to the aluminum foil is 10um, and the advancing speed is 1um / h .

[0051] The magneti...

Embodiment 3

[0052] Example 3 Experimental Research on the Effect of Boron Carrier / Targeting Agent on Tumor Cells

[0053]In this example, the effects of different metallocarborane boron carriers and / or targeting agents on K562 sensitive cells and multidrug resistant tumor cells were studied and compared. The metallocarborane and targeting agent shown in formula (I) in the above-mentioned example are respectively interacted with cells, and anticancer drug daunorubicin DNR (1.77*10 -3 M) As a fluorescent molecular probe, the molar concentration ratio of the drug to the probe is 10:1, observed under a confocal laser fluorescence microscope.

[0054] Comparison of Carborane and Magnetic Nanoparticle-Based Carborane-Targeting Formulations

[0055] In K562 sensitive cells and multi-drug resistant tumor cell lines, carborane and magnetic nanoparticle-based carborane targeting preparations were added for incubation, and drug molecules were used as fluorescent probes to observe under confocal la...

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Abstract

The invention discloses a making method of organic metal carborane targeting agent based on magnetic nanometer material, which is characterized by the following: proceeding self-assemblage for magnetic nanometer particle Fe3O4 and one / two meal central carborane with surface decorated; making targeting agent move to tumour position under external magnetic field.

Description

technical field [0001] The invention relates to a boron carrier in the field of biological nanotechnology (and medical nanomaterials), in particular to a method for preparing an organometallic carborane targeting preparation based on magnetic nanomaterials and an organic compound prepared by the method. Metallocarborane-targeted formulations provide a new approach to address the core issues of boron neutron capture therapy (BNCT). Background technique [0002] Tumor is one of the current killers that endanger human health. Surgical operations, radiotherapy, chemotherapy and other methods have been able to successfully cure some tumors, but there are still many malignant tumors with unsatisfactory treatment effects. Moreover, with traditional radiation therapy, normal tissues near tumor cells will inevitably be irradiated, and there is still a risk of recurrence. The ideal way to treat malignant tumors is to kill tumor cells while minimizing damage to adjacent normal tissues...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/02A61K51/04A61P35/00
Inventor 王雪梅吴春惠宋敏李景源张仁云吴德洪燕红顾忠泽陈宝安
Owner SOUTHEAST UNIV
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