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Galactosamine and polydopamine modified liver cancer targeting nanoparticles as well as preparation method and application thereof

A technology targeting nanoparticles and polydopamine, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problem of inability to effectively distinguish cancer cells from normal cells, high cytotoxicity, The problem of normal body organ damage and other problems, to achieve the effect of good liver targeting and simple preparation method

Inactive Publication Date: 2015-06-03
SHENZHEN BAINUO KANTAI BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy and radiotherapy are the earliest developed and widely used treatment methods. Their main disadvantages are: the treatment methods are not highly targeted to cancer cells, and cannot effectively distinguish cancer cells from normal cells, especially chemotherapy and some protein drugs. Very high cytotoxicity, it also causes great damage to normal body organs during treatment
But this kind of nanomedicine does not have the function of active targeting

Method used

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  • Galactosamine and polydopamine modified liver cancer targeting nanoparticles as well as preparation method and application thereof
  • Galactosamine and polydopamine modified liver cancer targeting nanoparticles as well as preparation method and application thereof
  • Galactosamine and polydopamine modified liver cancer targeting nanoparticles as well as preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0041] A method for preparing liver cancer targeting nanoparticles modified by galactosamine and polydopamine, comprising the steps of:

[0042] (1) Weigh 100mg polymer TPGS-PLA and 10mg docetaxel powder, dissolve in 8ml acetone, add dropwise to 100ml 0.3mg / L polyethylene glycol 1000 vitamin E succinate under stirring condition (TPGS) aqueous solution, stirred for 6 hours, evaporated under reduced pressure to remove acetone, centrifuged at 20000rpm for 15min, discarded the supernatant, washed three times with deionized water, to remove the emulsifier TPGS and free docetaxel, precipitated as docetaxel The initial nanoparticles TPGS-PLA / NPs;

[0043] (2) Resuspend the initial nanoparticle TPGS-PLA / NPs in a 10mM Tris buffer with pH=8.5 at a ratio of 5mg:1mL, add dopamine hydrochloride to make the concentration 0.5mg / mL, and react for 3 hours , centrifuged at 10,000rpm for 30min, collected the precipitate, washed three times with deionized water to remove unreacted dopamine hydro...

Embodiment 2

[0056] A method for preparing liver cancer targeting nanoparticles modified by galactosamine and polydopamine, comprising the steps of:

[0057] (1) Weigh 100mg of polymer TPGS-PLA and 2mg of coumarin-6, dissolve in 8ml of dichloromethane, add dropwise to 100ml of 0.3mg / L TPGS aqueous solution under stirring condition, stir for 24 hours, Remove dichloromethane by evaporation under reduced pressure, centrifuge at 20000rpm for 15min, discard the supernatant, wash three times with deionized water to remove emulsifier TPGS and free coumarin-6, and precipitate as the initial nanoparticle TPGS loaded with coumarin-6 -PLA / NPs;

[0058] (2) Resuspend the initial nanoparticle TPGS-PLA / NPs in a 10 mM, pH=8.5 PBS buffer solution at a ratio of 1 mg:1 mL, add dopamine hydrochloride to make the concentration 0.2 mg / mL, and react for 5 hours , centrifuged at 20000rpm for 15min, collected the precipitate, washed three times with deionized water to remove unreacted dopamine hydrochloride, and...

Embodiment 3

[0064] A method for preparing liver cancer targeting nanoparticles modified by galactosamine and polydopamine, comprising the steps of:

[0065] (1) Weigh 100 mg of polymer PLGA and 20 mg of paclitaxel powder, dissolve in 10 ml of dioxane, add dropwise to 100 ml of 10 mg / L TPGS aqueous solution under stirring, stir for 12 hours, evaporate under reduced pressure to remove dioxane Oxycycline, centrifuged at 15000rpm for 15min, discarded the supernatant, washed three times with deionized water to remove the emulsifier TPGS and free paclitaxel, and precipitated as the initial nanoparticle PLGA / NPs loaded with paclitaxel;

[0066] (2) Resuspend the initial nanoparticle PLGA / NPs in a 10mM, pH=8.5 Tris buffer at a ratio of 10mg:1mL, add dopamine hydrochloride to make the concentration 1.0mg / mL, react for 12 hours, 15000rpm After centrifugation for 20 min, the precipitate was collected and washed three times with deionized water to remove unreacted dopamine hydrochloride to obtain pol...

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Abstract

The invention discloses galactosamine and polydopamine modified liver cancer targeting nanoparticles as well as a preparation method and application thereof. The preparation method of the galactosamine and polydopamine modified liver cancer targeting nanoparticles comprises the following steps: taking polymer and a hydrophobic medicine, dissolving the polymer and the hydrophobic medicine into an organic solvent, stirring, dropwise adding the obtained solution into TPGS aqueous solution, stirring, carrying out reduced pressure volatilization, centrifuging, and abandoning supernate, so that polymer initial nanoparticles carrying the hydrophobic medicine are obtained; resuspending the initial nanoparticles in Tris buffer solution, adding dopamine hydrochloride for reacting, and centrifuging, so that hydrophobic-medicine-carrying nanoparticles wrapped by polydopamine are obtained; dispersing the hydrophobic-medicine-carrying nanoparticles wrapped by polydopamine into weakly alkaline aqueous solution, adding a liver cancer targeting ligand galactosamine, reacting, centrifuging, and carrying out freeze drying, so that the galactosamine and polydopamine modified liver cancer targeting nanoparticles are obtained. The preparation method of the galactosamine and polydopamine modified liver cancer targeting nanoparticles is simple and pollution-free; and the galactosamine and polydopamine modified liver cancer targeting nanoparticles have good liver targeting property, biological compatibility and biological degradability, can be used for targeting liver cancer and has treatment effect.

Description

technical field [0001] The invention relates to a liver cancer targeting nanoparticle modified by galactosamine and polydopamine, a preparation method and application thereof. Background technique [0002] The liver is one of the most critical organs in the human body. It is involved in multiple processes such as digestion, excretion, detoxification and immune regulation in the body. Therefore, the liver is also one of the most vulnerable organs in the human body. However, diseases such as liver cancer have caused a large number of deaths and seriously threatened human health. So far, more than a dozen methods of liver cancer treatment have been developed, such as chemotherapy, radiotherapy, surgery, biological therapy, gene therapy, photodynamic therapy, cancer vaccines, etc. Chemotherapy and radiation therapy are the earliest developed and widely used treatment methods. Their main disadvantages are: the treatment methods are not highly targeted to cancer cells, and cannot...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/34A61K47/26A61P35/00A61K31/337
Inventor 梅林曾小伟刘赣张明明
Owner SHENZHEN BAINUO KANTAI BIOTECH CO LTD
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