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Compound with fluorescence imaging and targeted therapeutic effect and preparation method thereof

A technology of targeted therapy and fluorescence imaging, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, luminescence/biological dyeing preparations, etc., which can solve the problem of ineffective detection of whether the drug reaches the lesion site

Inactive Publication Date: 2016-07-13
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of the present invention is to provide a complex with fluorescence imaging and targeted therapy and its preparation method, which solves the problem that the previous single imaging or single treatment cannot effectively detect whether the drug reaches the lesion site

Method used

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  • Compound with fluorescence imaging and targeted therapeutic effect and preparation method thereof
  • Compound with fluorescence imaging and targeted therapeutic effect and preparation method thereof
  • Compound with fluorescence imaging and targeted therapeutic effect and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0018] With the magnesium / aluminum molar ratio being 2:1, weigh 0.5769gMg(NO 3 ) 2 ·6H 2 O, 0.422gAl(NO 3 ) 3 9H 2 O and 10mg doxorubicin were dissolved in 40ml deionized water to make a mixed salt solution, and 0.4g NaOH and 0.3g folic acid were dissolved in 40ml deionized water to make an alkali solution; the mixed salt solution and alkali solution were poured into the opened In the fully back-mixed liquid film reactor, the rotor speed is controlled at 3000 rpm, the reaction mixture stays in the reactor for 2 minutes, and then the obtained slurry is poured into a crystallization tank, and crystallized at a constant temperature of 100°C for 12 hours. Then filter with ethanol, wash, put the filter cake in an oven at 60°C for 18 hours, and grind it finely to obtain a complex with fluorescence imaging and targeted therapy.

[0019] The compound with fluorescence imaging and targeted therapy prepared above is doxorubicin and folic acid co-intercalated hydrotalcite, and its c...

Embodiment 2

[0021] With the magnesium / aluminum molar ratio being 3:1, weigh 0.577gMg(NO 3 ) 2 ·6H 2 O, 0.281gAl(NO 3 ) 3 9H 2 O and 20mg doxorubicin were dissolved in 40ml deionized water to make a mixed salt solution, and 0.4g NaOH and 0.3g folic acid were dissolved in 40ml deionized water to make an alkali solution; the mixed salt solution and alkali solution were poured into the opened In the fully back-mixed liquid film reactor, the rotor speed is controlled at 4000 rpm, the reaction mixture stays in the reactor for 2 minutes, and then the obtained slurry is poured into a crystallization tank, and crystallized at a constant temperature of 100°C for 24 hours. Then filter with ethanol, wash, put the filter cake in an oven at 60°C for 24 hours, and grind it finely to obtain a complex with fluorescence imaging and targeted therapy.

[0022] The compound with fluorescence imaging and targeted therapy prepared above is doxorubicin and folic acid co-intercalated hydrotalcite, and its ch...

Embodiment 3

[0024] With the magnesium / aluminum molar ratio being 2:1, weigh 0.5769gMg(NO 3 ) 2 ·6H 2 O, 0.422gAl(NO 3 ) 3 9H 2 O and 30mg doxorubicin were dissolved in 40ml deionized water to make a mixed salt solution, and 0.4gNaOH and 0.3gFA were dissolved in 40ml deionized water to make an alkaline solution; In the back-mixing liquid film reactor, the rotor speed is controlled at 5000 rpm, the reaction mixture stays in the reactor for 2 minutes, and then the obtained slurry is poured into the crystallization tank, and crystallized at a constant temperature of 100 ° C for 36 hours, and then Suction filtration with ethanol, washing, drying the filter cake in an oven at 60°C for 30 hours, and grinding to obtain a complex with fluorescence imaging and targeted therapy.

[0025] The compound with fluorescence imaging and targeted therapy prepared above is doxorubicin and folic acid co-intercalated hydrotalcite, and its chemical formula is: Mg 0.624 Al 0.376 (OH) 2 DOX 0.020 FA 0.1...

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Abstract

The invention discloses a compound with fluorescence imaging and a targeted therapeutic effect and a preparation method thereof. According to the invention, a method for carrying out rapid nucleation reaction by virtue of a liquid-liquid reaction full-backmixing membrane reactor is adopted for jointly intercalating an anticancer drug adriamycin and targeting molecule folic acid into a hydrotalcite interlayer, so that pharmaceutical molecules are fixed on the hydrotalcite interlayer, release of the pharmaceutical molecules can be in a controllable state, and cytotoxicity of the pharmaceutical molecules on normal cells is greatly reduced; besides, adriamycin has red fluorescence and can enhance fluorescence imaging effect of the hydrotalcite interlayer when being intercalated into the hydrotalcite interlayer; meanwhile, folic acid molecule jointly intercalated serves as a targeting molecule, so that cancer cells take in more compounds, and diagnosis and treatment are carried out at the same time.

Description

technical field [0001] The invention belongs to the technical field of preparation of antineoplastic drugs, and in particular relates to a compound with functions of fluorescence imaging and targeted therapy and a preparation method thereof. technical background [0002] Cancer has always been one of the major diseases that are difficult for people to overcome. Early diagnosis and treatment of cancer play an important role in human health. (Zhang Da, Zhou Feifei, Xing Da. Targeted tumor imaging and photothermal therapy of functionalized graphene oxide. Science Bulletin, 2013, 58:586–592) The traditional methods of cancer treatment mainly include radiotherapy, surgery, and chemotherapy. Due to the remarkable effect of chemotherapy and the convenience of operation, it is widely used in the field of cancer treatment. However, due to the excessive lethality of chemotherapy drugs on normal cells and tissues, it will produce great side effects, thus limiting its development. ...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K47/22A61K47/02A61K31/704A61P35/00
CPCA61K49/0021A61K31/704A61K47/02A61K47/22A61K49/005
Inventor 梁瑞政关山月张少敏安鸽卫敏
Owner BEIJING UNIV OF CHEM TECH
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