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Boron delivery agent and preparation method thereof

A delivery agent, boron compound technology, applied in the field of tumor treatment, can solve the problem of low tumor targeting, achieve the effects of simple loading method, stable physical and chemical properties, and strong external environment tolerance

Active Publication Date: 2022-04-01
DALIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] 4-dihydroxyboryl phenylalanine (BPA) and sodium undecahydromercapto dodecaboride (BSH) are currently the only two boron compounds approved for clinical use, although they have good therapeutic effects , but the tumor targeting is low, so the design and development of new boron delivery agents with higher tumor specificity is a key factor to improve tumor targeting

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preparation example Construction

[0022] The invention provides a boron delivery agent and its preparation method and application. Ferritin nanoparticles are used as transport carriers, boron compounds are loaded in the inner core of ferritin nanoparticles, and the boron compounds are transported to In the tumor cells, the therapeutic effect is produced by capturing low-energy thermal neutrons to kill tumor cells.

[0023] The purpose of the present invention is to use ferritin shell as a carrier to prepare boron delivery body. The key technology is how to load boron reagent into ferritin shell, and improve the loading capacity and encapsulation efficiency of boron reagent by adjusting the preparation parameters. The selected ferritin Including horse spleen ferritin, plant ferritin, ferritin H chain expressed by prokaryotic microorganisms, ferritin H chain expressed by eukaryotic microorganisms and ferritin from other sources, especially ferritin H chain expressed by microorganisms, with large yield and low pri...

Embodiment 1

[0026] 1. This embodiment provides a ferritin boron delivery agent. The ferritin is horse spleen ferritin, and the boron compound is 4-dihydroxyboryl phenylalanine BPA.

[0027] 2. Preparation method of ferritin boron delivery agent

[0028] (1) Dilute the horse spleen ferritin solution with Tris-HCl buffer solution with a pH of 7.4 to 5mg / mL, add 0.1M HCl solution to adjust the pH to about 5.0, add 100μL thioglycolic acid / 40mL protein solution, mix well, and After standing in the refrigerator for 16 hours, the solution turned from brownish red to colorless, then added 2mL of 2,2'-dipyridyl saturated ethanol solution, the solution turned dark red, and then dialyzed in Tris-HCl buffer solution with pH 7.4, the retention The molecular weight is 7.0kD, and a colorless and transparent apoferritin solution was obtained after 2 days;

[0029] (2) Slowly add 0.1M HCl solution to the apoferritin solution to adjust the pH to 2.0;

[0030] (3) BPA is dissolved in a Tris-HCl buffer sol...

Embodiment 2

[0037] 1. This embodiment provides a ferritin boron delivery agent. The ferritin H chain expressed by Escherichia coli has a molecular weight of 2.3 kD. The boron compound is 4-dihydroxyborylphenylalanine BPA.

[0038] 2. Preparation method of ferritin boron delivery agent

[0039](1) Dissolve ferritin in Tris-HCl buffer solution with pH 7.4, slowly add 0.1M HCl solution to adjust the pH to 2.0;

[0040] (2) BPA is dissolved in Tris-HCl buffer solution with a pH of 7.4, and acetonitrile is added to adjust the solubility of BPA;

[0041] (3) Slowly add BPA solution to ferritin solution, add acetonitrile to a final concentration of 10.0% (v / v), stir at room temperature for 2 hours, slowly add 0.1M NaOH solution to the solution to adjust the pH to 9.0, and let stand in the refrigerator for 2 hours;

[0042] (4) The above solution is dialyzed in a Tris-HCl buffer solution with a pH of 9.0, the molecular weight cut-off is 7.0kD, and then replaced with a Tris-HCl buffer dialysate w...

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Abstract

The invention belongs to the technical field of tumor treatment, and discloses a boron delivery agent and a preparation method thereof. Ferritin nano-particles are used as a boron compound conveying carrier, a boron compound is loaded in a core of the ferritin nano-particles, the boron compound is conveyed into tumor cells by virtue of a tumor targeting effect of the ferritin nano-carrier, and then the tumor cells are killed by capturing low-energy thermal neutrons to generate a treatment effect. The boron delivery agent not only has a tumor targeting characteristic, but also has the advantages of stable physicochemical properties, simple boron compound loading method, good biocompatibility, good dispersibility, uniform particle size and the like, and has a wide application prospect in tumor boron neutron capture therapy.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment, and in particular relates to a boron delivery agent and a preparation method thereof. Background technique [0002] Boron neutron capture therapy (BNCT) is a radiation therapy that can selectively kill tumor cells. After the boron delivery agent with specific affinity for tumor cells enters the human body, it will be selectively enriched in tumor cells. Medium, non-radioactive isotopes 10 After B captures low-energy thermal neutrons (0.025eV), a nuclear fission reaction occurs to produce α particles ( 4 He) and recoil lithium-7 ( 7 Li), which can kill tumor cells due to high linear energy transfer. The path length of α-particles (5-9 μm, approximately one cell diameter) is very short, and its destructive effect is limited to boron-containing cells, and does not affect adjacent normal cells, so the damage to surrounding tissues of the tumor is small. Therefore, BNCT is a binary, cell-s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/51A61K47/42A61K47/54A61K47/62A61K47/60A61K47/69A61P35/00B82Y5/00B82Y40/00
CPCY02A50/30
Inventor 张英奚宇菲张姝华邵佳琪何惠
Owner DALIAN UNIV
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