Polymer nanoparticles double-loaded with docetaxel and flavonoid compounds and preparation method of polymer nanoparticle

A technology of docetaxel and nanoparticles, which is applied in the field of anti-tumor drugs, can solve the problems of reducing drug resistance of tumor cells, and the level cannot be satisfied, and achieve the effects of prolonging the action time, less damage, and excellent application prospects

Inactive Publication Date: 2018-11-20
CHENGDU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent CN107913249A discloses several combinations containing DTX and some traditional Chinese medicine monomers, which can reduce the drug resistance of tumor cells to a certain extent, but the degree cannot meet people's needs

Method used

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  • Polymer nanoparticles double-loaded with docetaxel and flavonoid compounds and preparation method of polymer nanoparticle
  • Polymer nanoparticles double-loaded with docetaxel and flavonoid compounds and preparation method of polymer nanoparticle
  • Polymer nanoparticles double-loaded with docetaxel and flavonoid compounds and preparation method of polymer nanoparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 A preparation method of nanoparticles loaded with docetaxel and fisetin

[0053]Weigh 50.0 mg of PEG-PCL (1:1, MW: 10k) and dissolve in 5 ml of ethyl acetate, 5 mg of fisetin and 4 mg of docetaxel in 2 ml of absolute ethanol, and mix the two solutions into a round bottom flask, Form a film layer under the working conditions of a rotary evaporator (45°C, 50rpm, 30min); measure 5ml of PBS solution (0.01M, pH 7.4, 65°C) to dissolve the film, and disperse the nanoparticles uniformly in the aqueous solution by ultrasonic ; and then filtered through a 0.45 μm microporous membrane, and freeze-dried to obtain a solid powder. Its hydrated average particle size diagram is shown in figure 2 As shown in A.

Embodiment 2

[0054] Example 2 A preparation method of nanoparticles loaded with docetaxel and luteolin

[0055] Weigh 200.0mg of PEG-PCL (1:1, MW:20k) and dissolve in 3ml of ethyl acetate, 20.0mg of sweet clover and 16mg of docetaxel are dissolved in 2ml of absolute ethanol, and mix the two solutions into an organic phase for later use; Weigh 50.0mg of poloxamer F127 and dissolve it in 20ml of ultrapure water as the aqueous phase for later use; slowly add the organic phase to the aqueous phase under the emulsification condition (9600rpm / min) of the T25 probe sonicator, and work continuously for 10min . Transfer the emulsified emulsion to a round-bottomed flask, and use a rotary evaporator to filter under reduced pressure (37°C, 60rpm, 15min) to remove the organic solvent to prepare the drug-loaded nanoemulsion, and store it at 4°C. Its hydrated average particle size diagram is shown in figure 2 Shown in B.

Embodiment 3

[0056] Example 3 A preparation method of nanoparticles loaded with docetaxel and fisetin

[0057] Weigh 200.0mg of PEG-PCL (1:2, MW:15k) and dissolve in 3ml of dichloromethane, 14.0mg of fisetin and 10.0mg of docetaxel in 1ml of absolute ethanol, and mix the two solutions into an organic Phase standby; Weigh 50.0mg of polyvinyl alcohol and dissolve it in 20ml ultrapure water as the water phase for standby; Slowly add the organic phase to the water phase under the emulsification condition (9600rpm / min) of the T25 probe ultrasonic emulsion homogeneous disperser, and work continuously 10min. Transfer the emulsified emulsion to a round-bottomed flask, and use a rotary evaporator to filter under reduced pressure (37°C, 60rpm, 15min) to remove the organic solvent to prepare the drug-loaded nanoemulsion, and store it at 4°C. Its hydrated average particle size diagram is shown in image 3 As shown in A.

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Abstract

The invention provides polymer nanoparticles double-loaded with docetaxel and flavonoid compounds. The polymer nanoparticles, with a PEG-PCL material as a carrier, are loaded with docetaxel and flavonoid compounds, thereby realizing slow-release of drugs in vivo, reducing drug resistance of tumors, and reducing the dosage of the drugs. The invention further provides a method for preparing the polymer nanoparticles double-loaded with docetaxel and flavonoid compounds, and the method has the characteristics of simple process and relatively high yield. The polymer nanoparticles have considerableprospects in the application of antitumor drugs.

Description

technical field [0001] The invention relates to the field of drug research and development, in particular to an antitumor drug with nanomaterials as carriers. Background technique [0002] Docetaxel (DTX) is a taxane broad-spectrum antineoplastic drug further synthesized from the extract from the leaves of Taxus chinensis. In recent years, a large number of research reports have confirmed that DTX has a good effect on malignant tumors such as breast cancer, lung cancer, head and neck cancer, sarcoma, non-small cell carcinoma, and prostate cancer. [0003] Due to the low water solubility and instability of DTX, the current mainstream approach is to carry it on nanomaterials with amphiphilic affinity. The hydrophobic side of the nanomaterial binds and wraps DTX; In contact with body fluids, it has good biocompatibility and realizes its transportation function. Nanomaterials can also reduce the non-target release of drugs in the systemic circulation, thereby ensuring high dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/59A61K47/60A61K47/69A61K31/337A61K31/352A61P35/00
CPCA61K31/337A61K31/352A61K47/593A61K47/60A61K47/6935A61P35/00A61K2300/00
Inventor 杨倩彭锦荣谭睿谭立伟吴敏李忆言
Owner CHENGDU MEDICAL COLLEGE
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