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Nano-drug taking irinotecan as carrier as well as preparation method and application of nano-drug

An irinotecan and nano-drug technology, applied in the field of medicine, can solve the problems of killing and inhibiting difficult tumor tissues, monomer degradation toxicity, slow onset of effect, etc., to achieve the treatment of metastatic colorectal cancer, reduce toxic side effects, increase dispersive effect

Pending Publication Date: 2021-06-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For the carrier design of oral chemotherapy drugs and oral non-steroidal anti-inflammatory drugs, because of the gastrointestinal irritation of non-steroidal anti-inflammatory drugs and the strong acidic environment of the stomach, the involvement of oral carrier systems is very challenging
Among VEGFR inhibitors, although most of them are oral preparations, it is difficult for the two drugs to co-localize to kill and inhibit tumor tissue.
[0006] Traditional polymer carriers have the problems of complex preparation, high cost, degradation toxicity of monomers, low drug loading, and slow onset of action.

Method used

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  • Nano-drug taking irinotecan as carrier as well as preparation method and application of nano-drug
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  • Nano-drug taking irinotecan as carrier as well as preparation method and application of nano-drug

Examples

Experimental program
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Effect test

Embodiment 1

[0040]Example 1 According to the optimal mass ratio of irinotecan:carprofen at 2:1, three groups of 10 mg irinotecan were weighed and placed in three 1.5 ml EP tubes, and 200 μl DMSO was added to irinotecan 1.5 ml EP and ultrasonically weighed three groups of 5 mg carprofen respectively and dissolved them in the above solution to form a mixed solution. Slowly drop the mixed solution into 5 ml 0.5 mg / ml PVP aqueous solution, limit the dropping rate to 2 s / drop, stir at 500 r / min for 2.5 min, centrifuge at 2000-6000 r / min for 3-10 min, take The particle size and Zeta potential of the supernatant were measured, and finally figure 1 and figure 2 . The particle size of the obtained nanoparticles is about 78 nm, and the Zeta potential is about 27 mv.

Embodiment 2

[0041] Example 2 According to the preparation method in Example 1, the obtained irinotecan and carprofen nanoparticles were prepared, and the solution was concentrated by gradient centrifugation, and 20 μl was dropped into the copper grid, and phosphotungstic acid was added to the Dry under infrared light for 5 min, and take transmission electron microscope pictures after the water evaporates, and finally get image 3 . The resulting particle size was around 73 nm.

Embodiment 3

[0042] Example 3 According to the optimal mass ratio of irinotecan: carprofen at 2:1, weigh three groups of 10 mg irinotecan and place them in three 1.5 ml EP tubes, add 200 μl DMSO to irinotecan 1.5 ml EP and ultrasonically weighed three groups of 5 mg carprofen respectively and dissolved them in the above solution to form a mixed solution. Slowly drop the mixture into 5 ml 0.5 mg / ml PVP aqueous solution, limit the dropping rate to 2 s / drop, stir at 500 r / min for 2.5 min, centrifuge at 2800 r / min for 5 min, and take the supernatant for 3.5 min ml to measure the particle size for 1 h. After measuring the particle size, the three groups of nanoparticles were placed in a refrigerator at 4 °C, and the particle size was measured at the same time every day. Three more groups were prepared according to the same method, and the particle size was measured and stored in -20 °C freezer. After thawing at room temperature, the particle size change was measured at the same time every day,...

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Abstract

The invention discloses a nano-drug taking irinotecan as a carrier and a preparation method of the nano-drug. The metabolic toxicity of the irinotecan is reduced; and meanwhile, the application range of the irinotecan as a small molecular carrier is expanded. The nano-drug is mainly composed of the irinotecan, a COX-2 inhibitor or a VEGFR inhibitor and a dispersing agent. The COX-2 inhibitor, the VEGFR inhibitor and the irinotecan can be prepared into the nano-drug through a pi-pi accumulation effect, a hydrophobic effect, an electrostatic effect, a hydrogen bond effect and the like under the assistance of a proper dispersing agent. Based on physical forces, such as pi-pi accumulation, the COX-2 inhibitor or the VEGFR inhibitor exerts efficacy as a prototype drug. The nano-drug is prepared through a solvent conversion method; the method is simple; the quality is controllable; the drug loading capacity is high; proliferation of metastatic colorectal cancer cells is effectively inhibited; angiogenesis is reduced; and the microenvironment is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nano-medicine with irinotecan as a carrier, a preparation method thereof and its application in tumor treatment. Background technique [0002] Cancer is one of the top three diseases affecting human life expectancy in terms of morbidity and mortality. In China, the clinical treatment conditions are limited, and the death rate is gradually increasing year by year. Metastasis occurs in advanced colorectal cancer, so stage IV is called metastatic colorectal cancer. The 5-year relative survival rates for patients diagnosed with stage I or II disease were 91 % and 82 %, respectively, which dropped to 15 % for stage IV disease. Clinically, the first-line chemotherapy regimen consisting of irinotecan, 5-fluorouracil and leucovorin for advanced metastatic colorectal cancer has an effective rate of less than 40%. Adverse events during irinotecan chemotherapy include neut...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K45/00A61P35/00A61P35/04B82Y5/00B82Y40/00
CPCA61K47/545A61K45/00B82Y5/00B82Y40/00A61P35/00A61P35/04
Inventor 姜虎林邢磊宋琪
Owner CHINA PHARM UNIV
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