A tumor-targeted radiotherapy-sensitized liposome nano-preparation and preparation method thereof

A technology of sensitizing lipids and nano preparations, which is applied in the field of biomedical materials, can solve problems such as poor radiotherapy effects, and achieve the effects of increasing radiosensitization effects, enhancing radiosensitization, and enhancing magnetic resonance imaging

Active Publication Date: 2021-05-14
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, oxygen itself also has the effect of radiotherapy sensitization, and the general hypoxia of tumors is one of the main factors causing the poor radiotherapy effect.
However, there are few reports on the technology of increasing the "ineffective redox cycle" effect of Gd-Texaphyrin

Method used

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  • A tumor-targeted radiotherapy-sensitized liposome nano-preparation and preparation method thereof
  • A tumor-targeted radiotherapy-sensitized liposome nano-preparation and preparation method thereof
  • A tumor-targeted radiotherapy-sensitized liposome nano-preparation and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0040] A preparation method of a tumor-targeted radiotherapy-sensitized liposome nano-preparation described in the present invention comprises the following steps:

[0041] (1) Preparation of the crude product of Gd-Texaphyrin-Lipid: add 1 mL of methanol to a 5 mL round-bottomed flask, and then add 10 mg of Texaphyrin-Lipid (prepared according to the preparation method in the literature, DOI retrieval number of the literature: 10.1002 / adhm. 201800857), 6 mg gadolinium acetate hydrate, 9 mg triethylamine, stirred to dissolve, 50 o C with heating and stirring for 3 hours. Subsequently, the methanol was blown dry with nitrogen, and 10 mL of cyclohexane was added to the remaining solid, and after stirring and washing the solid, the solid precipitate was collected by centrifugation. After repeated washing of the solid three times, a dark green crude product was finally obtained.

[0042] (2) Purification of the crude product of Gd-Texaphyrin-Lipid: the crude product was purified ...

Embodiment 2

[0045] A preparation method of a tumor-targeted radiotherapy-sensitized liposome nano-preparation described in the present invention comprises the following steps:

[0046] (1) Preparation of the crude product of Gd-Texaphyrin-Lipid: Add 1 mL of methanol to a 5 mL round-bottomed flask, then add 10 mg of Texaphyrin-Lipid, 6 mg of gadolinium acetate hydrate, and 9 mg of triethylamine. o C with heating and stirring for 3 hours. Subsequently, the methanol was blown dry with nitrogen, and 10 mL of cyclohexane was added to the remaining solid, and after stirring and washing the solid, the solid precipitate was collected by centrifugation. After repeated washing of the solid three times, a dark green crude product was finally obtained.

[0047](2) Purification of the crude product of Gd-Texaphyrin-Lipid: the crude product was purified using a silica gel forward chromatographic column. After loading the sample, first use the gradient elution of methanol-chloroform mobile phase for m...

Embodiment 3

[0050] A preparation method of a tumor-targeted radiotherapy-sensitized liposome nano-preparation described in the present invention comprises the following steps:

[0051] (1) Preparation of Gd-Texaphyrin-Lipid crude product: Add 1 mL N,N-dimethylformamide to a 5 mL round bottom flask, then add 10 mg Texaphyrin-Lipid, 6 mg gadolinium nitrate hydrate, 9 mg N , N-Diisopropylethylamine, after stirring and dissolving, 60 o C was heated and stirred for 5 hours. Subsequently, N,N-dimethylformamide was evaporated to dryness under reduced pressure, 5 mL of glacial ether was added to the remaining solid, the solid was stirred and washed, and the solid precipitate was collected by centrifugation. After repeated washing of the solid three times, a dark green crude product was finally obtained.

[0052] (2) Purification of the crude product of Gd-Texaphyrin-Lipid: the crude product was purified by high performance liquid chromatography and C4 reverse chromatography column. Agilent 126...

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Abstract

The invention discloses a tumor-targeted radiotherapy-sensitized liposome nano-preparation and a preparation method thereof. The prepared preparation is Texas porphyrin liposome (Gd-Nanotexaphyrin) coordinated by gadolinium ions, and has Enhanced effects of magnetic resonance imaging and radiosensitization. The hydrophilic cavity of the preparation can contain oxygen-carrying proteins, carry oxygen, improve tumor hypoxia, improve the "ineffective redox cycle" effect of Gd-Texaphyrin, and enhance the radiosensitization effect of Gd-Texaphyrin. The surface of the preparation can be modified with targeting molecules. By virtue of the active targeting ability of the targeting molecules and the passive targeting effect of the liposome itself, the preparation can be concentrated in the tumor site, increasing the uptake of Gd-Texaphyrin in the tumor. Further enhanced the radiosensitizing effect of Gd‑Texaphyrin.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a tumor-targeted radiotherapy-sensitized liposome nano-preparation and a preparation method thereof. Background technique [0002] The treatment of cancer is a difficult problem faced by human beings all over the world. Radiation therapy is an important means of cancer treatment. However, the therapeutic effect of low-dose radioactive rays is limited, and increasing the dose of radioactive rays will increase the damage of normal tissues and organs, which limits the tumor therapeutic effect of radiotherapy. Therefore, a variety of radiosensitizers have been developed to improve the tumor killing effect of radioactive rays. The research and development of radiosensitizers still faces some problems. For example, chemotherapy drugs such as cisplatin, paclitaxel, and pentafluorouracil have certain radiosensitization effects, but they have high toxicity in vivo; the cl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/54A61K41/00A61P35/00
CPCA61K9/1271A61K41/0038A61K47/24A61K47/544A61P35/00
Inventor 王凡史继云马晓途
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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