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Targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as carrier and preparation method thereof

A technology of anti-tumor drugs and nano-microspheres, which is applied in the field of anti-tumor drug nano-microspheres and its preparation, which can solve the problems that the slow-release dosage forms have not been paid attention to, and achieve the effects of uniform size, smooth shape, and prolonged release period

Active Publication Date: 2014-04-30
广州智园生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In recent years, scholars at home and abroad have done a lot of clinical research on capecitabine alone or in combination with other drugs, but the research on its use in sustained-release dosage forms has not yet received attention

Method used

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  • Targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as carrier and preparation method thereof
  • Targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as carrier and preparation method thereof
  • Targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] An anti-tumor drug nanosphere with targeting and sustained release effect using amphiphilic polyurethane as a carrier, characterized in that the specific scheme is as follows:

[0049] Microemulsion technology is emulsified solvent evaporation method.

[0050] Step 1: preparing amphiphilic polyurethane, comprising the following steps:

[0051] (1) Add 5g PEG and 20mL acetone to a three-necked flask equipped with a stirrer, reflux condenser and thermometer, stir evenly, add 0.36g HMDI to it, slowly raise the temperature to 80°C under the condition of mechanical stirring, stir for 1h, and make it mix Uniform;

[0052] (2) The temperature of the reaction system was raised to 75° C. while stirring, and the temperature was lowered to 30° C. after 1.5 hours of reaction, and 0.20 g of DMPA was added thereto. Raise the temperature to 70°C with mechanical stirring, stir for 1 hour to make it evenly mixed, and then lower the temperature to 30°C.

[0053] (3) Raise the temperat...

Embodiment 2

[0065] The difference between this embodiment and embodiment 1 is:

[0066] Step 3 prepares nano-microspheres The method for preparing nano-microspheres by nano-precipitation-dialysis method includes the following steps:

[0067] (1) Take 2 g of FA-PCEC as a solute, dissolve it in 20 mL of dichloromethane, and prepare an oil phase matrix solution with a concentration of 100 mg / mL, and disperse 0.2 g of antineoplastic drug CAP in the above matrix solution to form an oil phase; and Add 0.019g of tetramethoxysilane (TMOS) dropwise to the oil phase, and stir evenly;

[0068] (2) Use polyvinyl alcohol as the solute and water as the solvent to prepare 100 mL of an aqueous solution with a mass fraction of 1.0% polyvinyl alcohol;

[0069] (3) Slowly add the water phase described in step (2) to the oil phase solution described in step (1) drop by drop, and continue to stir at 600rpm for 2 hours; then perform dialysis in distilled water medium, changing every 2 hours Water once, dialy...

Embodiment 3

[0076] The difference between this embodiment and embodiment 1 is:

[0077] Adjust the volume of the PVA aqueous solution in Step (2) of Step 3 in Example 1 to 400 mL, that is, the volume of the second emulsified surfactant solution is 20 times the volume of the organic solvent. The obtained nano-microspheres were tested and characterized with a laser particle size analyzer and a scanning electron microscope, and it was found that the particle size of the nano-microspheres in this example was smaller than that in Example 1, because the increase in the volume of the water phase reduced the viscosity of the oil phase , which is conducive to the dispersion of the oil phase in the water phase to form emulsion droplets, which reduces the particle size of the final microspheres.

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Abstract

The invention discloses a trgeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as a carrier and a preparation method thereof. The nanoparticle is of a nucleus-shell structure provided with two shell layers; a hydrophilic section of amphiphilic polyurethane serves as the shell layer, and a hydrophobic section serves as the nucleus; the nucleus covers the medicines; a functional molecule exposes from the surface of the shell layer of the nanoparticle; organo-siloxane can be hydrolyzed to form another shell layer between the hydrophilic section and the hydrophobic section; the medicines include capecitabine, adriamycin and paclitaxel; the functional molecule is folic acid; and organo-siloxane is tetramethoxysilane. The targeting and slow-release antineoplastic medicine nanoparticle with amphiphilic polyurethane as the carrier has the characteristics that degradable polymer materials are used as the medicine release-control preparations, which enables the medicine to act on a specified wound position with the minimum dosage; and the medicine release rate can be optimized to improve the treatment effect as well as reduce the toxic and side effects.

Description

technical field [0001] The invention belongs to the technical field of chemical drugs, and relates to an anti-tumor drug nano-microsphere with targeting and slow-release functions and a preparation method thereof, which uses amphiphilic polyurethane as a carrier. Background technique [0002] Colorectal cancer (CRC) is the third leading cause of cancer death in humans, with an estimated 1 million new cases diagnosed each year in developed countries. Chemotherapy is one of the essential means. [0003] Fluorouracil is the main drug approved for chemotherapy in colorectal cancer. Capecitabine is an oral fluorouracil, which is widely used alone or in combination with other drugs to treat colorectal cancer. Combining oxaliplatin and bevacizumab, it has a certain curative effect on patients with colon cancer, but at the same time, it also produces certain side effects. Capecitabine combined with irinotecan also has some side effects in the treatment of mCRC, especially diarrh...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/7068A61K31/704A61K31/337A61K47/34A61K47/04A61K47/22A61P35/00C08G18/66C08G18/48C08G18/42C08G18/10
Inventor 魏坤彭小敏邹芬
Owner 广州智园生物科技有限公司
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