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Misonidazole pH sensitive liposome and preparation method thereof

A technology of misonidazole and liposome, which is applied in the field of tumor radiotherapy sensitization, can solve the problems of low sensitization ratio and small neurotoxicity, achieve high pH sensitivity, reduce neurotoxicity, and increase radiosensitization ratio Effect

Inactive Publication Date: 2018-06-15
重庆市人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In order to reduce the toxic and side effects of nitroimidazole compounds, researchers have successfully developed Etanidazole (SR-2508), Pimonidazole (Ro 03-8799), Sanazole (AK-2123), Nimorazole, Doranidazole and other nitroimidazole derivatives, clinical trials have confirmed that these compounds have hypoxic cell radiation sensitization, and have relatively small neurotoxicity, but the sensitization ratio is lower than MISO

Method used

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  • Misonidazole pH sensitive liposome and preparation method thereof
  • Misonidazole pH sensitive liposome and preparation method thereof
  • Misonidazole pH sensitive liposome and preparation method thereof

Examples

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Embodiment 1

[0041] Embodiment 1: A kind of misonidazole pH-sensitive liposome is obtained by adopting the following mass ratio: 5 parts of misonidazole, 30 parts of phosphatidylethanolamine, 5 parts of cholesterol, 10 parts of linoleic acid, and the mass percentage is 0.3% carboxymethyl chitosan 1 part, vitamin E 2 parts. Wherein the misonidazole pH sensitive liposome particle size distribution diagram is as follows figure 1 Shown, misonidazole pH-sensitive liposome site map is as follows figure 2 Shown, misonidazole pH-sensitive liposome scanning electron microscope picture is as image 3 Shown, misonidazole pH-sensitive liposome release curve in different pH solutions is as follows Figure 4 shown.

[0042] A preparation method of misonidazole pH-sensitive liposomes, comprising the following steps:

[0043] S1: Take 30 parts of phosphatidylethanolamine, 5 parts of cholesterol, 10 parts of linoleic acid and 2 parts of vitamin E in a flask, then add chloroform to dissolve, connect th...

Embodiment 2

[0047] Embodiment 2: a kind of preparation method of misonidazole pH sensitive liposome, comprises the following steps:

[0048] A1: Take 30 parts of phosphatidylethanolamine, 5 parts of cholesterol, 10 parts of linoleic acid, and 2 parts of vitamin E in a flask, add chloroform to dissolve, and add 5 parts of misonidazole aqueous solution, and perform ultrasound to form an emulsion, and then Connect the flask to a rotary evaporator to evaporate under reduced pressure to form a gel state;

[0049] A2: Add PBS buffer solution to the flask, the pH of the PBS buffer solution is 7.4, evaporate under reduced pressure to form an aqueous suspension; use gel chromatography or ultracentrifugation to remove the substances not included in the aqueous suspension to obtain lipid Plastid suspension;

[0050] A3: Sonicate the liposome suspension and pass it through a microporous membrane to obtain liposomes;

[0051] A4: Add 1 part of carboxymethyl chitosan solution with a mass percentage o...

Embodiment 3

[0052] Embodiment 3: a kind of preparation method of misonidazole pH sensitive liposome, comprises the following steps:

[0053] B1: Take 30 parts of phosphatidylethanolamine, 5 parts of cholesterol, 10 parts of linoleic acid and 2 parts of vitamin E in a flask, add dimethyl sulfoxide to mix as phase A, add 5 parts of pure water, glycerin and misonidazole Mix as Phase B, mix Phase A and Phase B, pour into a blender, stir at 55°C for 5 minutes, then take it out and emulsify in an emulsifier for 30 seconds, and then emulsify in a high-pressure emulsifier for 5 times;

[0054] B2: Put the product emulsified in the high-pressure emulsifier in step B1 into an ultrasonic oscillator for defoaming, then add PBS buffer solution with a pH of 7.4 to form a liposome suspension;

[0055] B3: Put the liposome suspension into a dialysis bag, dialyze to remove free misonidazole, then perform ultrasonication and pass through a microporous membrane to obtain liposomes;

[0056] B4: Add 1 part ...

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Abstract

The invention discloses a misonidazole pH sensitive liposome, which comprises a bulk drug and auxiliary materials. The bulk drug is misonidazole, and the auxiliary materials are phosphatidyl ethanolamine, cholesterol, linoleic acid, and carboxymethyl chitosan. The invention also discloses a preparation method of the misonidazole pH sensitive liposome. The preparation method comprises following steps: step one, adding phosphatidyl ethanolamine, cholesterol and linoleic acid into a flask according to a certain mass ratio, then adding chloroform to dissolve the above-mentioned components, connecting the flask to a rotary evaporator to volatize chloroform and forming a film on the inner wall of a beaker; step two, adding a PBS solution of misonidazole into the beaker, carrying out hydration inthe absence of light to obtain a liposome solution; step three, filling the liposome solution into a dialysis bag, carrying out dialysis to remove free misonidazole, carrying out an ultrasonic treatment, and filtering the solution by a microporous filter membrane to obtain liposome; and step four, adding a carboxymethyl chitosan solution into the liposome, and carrying out hydration to obtain themisonidazole pH sensitive liposome. The misonidazole pH sensitive liposome has the advantages that the preparation method is simple, the particle size is uniform, and the pH sensitivity is high.

Description

technical field [0001] The invention relates to the field of tumor radiotherapy sensitivity enhancement, in particular to a misonidazole pH-sensitive liposome and a preparation method thereof. Background technique [0002] The rapid and disordered growth of solid malignant tumors leads to insufficient angiogenesis and insufficient blood oxygen supply, resulting in the appearance of hypoxic cells in the tumor. Hypoxic cells can reduce the damage of oxygen free radicals to DNA proliferation, making their ability to resist radiation 2 to 3 times higher than normal oxygen-containing tumor cells, resulting in solid tumors that are not sensitive to radiation therapy or cannot be completely controlled, even after radiation therapy. relapse. Thus, the existence of hypoxic cells is one of the main reasons for the failure of radiotherapy. [0003] Radiosensitizers refer to certain chemical substances that can enhance the killing effect of radiation on hypoxic cells in tumors and cau...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/4168A61K9/127A61K47/36A61P35/00
CPCA61K41/0038A61K9/127A61K9/1277A61K31/4168A61K47/36
Inventor 罗治彬何美魏巍王琛
Owner 重庆市人民医院
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