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Adriamycin nano drug delivery system as well as preparation method and application thereof

A nano-loaded drug and doxorubicin technology, which is applied in the direction of pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of inability to deliver two active ingredients at the same time, inconsistent pharmacokinetic behavior, and low bioavailability of drugs , achieve good market development prospects, enhance anti-cancer effects, and have no obvious toxic and side effects

Active Publication Date: 2014-08-13
HUAZHONG UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned combined drug uses different preparations of the two active ingredients in combination, and does not use the same carrier for drug co-delivery, so there are two different active ingredients (different chemotherapeutic drugs, sensitizers and chemotherapeutic drugs) in vivo pharmacokinetics However, due to the inconsistency of biological behavior, the inability of the two active ingredients to be delivered to tumor cells at the same time, and the low bioavailability of the drug, its therapeutic effect is still limited.

Method used

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  • Adriamycin nano drug delivery system as well as preparation method and application thereof
  • Adriamycin nano drug delivery system as well as preparation method and application thereof
  • Adriamycin nano drug delivery system as well as preparation method and application thereof

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preparation example Construction

[0052] The preparation method of the doxorubicin nano-loading system provided by the invention comprises the following steps:

[0053] (1) Uniformly disperse the doxorubicin-containing active ingredient, solid lipid, liquid lipid and fat-soluble emulsifier in the organic solvent in the formula ratio, evaporate the organic solvent to dryness at 65°C to 80°C to obtain an oil phase, and maintain the temperature.

[0054] The fat-soluble emulsifier, such as phospholipids and the like.

[0055] The doxorubicin is fat-soluble doxorubicin, which can be obtained as follows: dissolve the water-soluble doxorubicin hydrochloride in an organic solvent, and add triethylamine 2 to 5 times the molar mass of doxorubicin hydrochloride for neutralization , stirred overnight in the dark, and the solvent was spun to dryness to obtain fat-soluble doxorubicin.

[0056] The organic solvent is dichloromethane, chloroform or ethanol, preferably absolute ethanol.

[0057] (2) Uniformly disperse other...

Embodiment 1

[0068] Doxorubicin nano-loading system, according to the mass ratio, includes 1.5% active ingredient containing doxorubicin, 20% solid lipid, 20% liquid lipid, 5% emulsifier and 5% isotonic regulator, and the balance is injection use water.

[0069] The active ingredient containing doxorubicin is a 1:10 mixture of doxorubicin and a sensitizer, and the sensitizer is curcumin.

[0070] The emulsifier contains polyethylene glycol 5000 vitamin E succinate with 10% total mass of emulsifier, and the emulsifier also contains polyoxyethylene-polyoxypropylene block copolymer with 90% total mass of emulsifier

[0071] The solid lipid comprises glyceryl monostearate with 100% of the total mass of the solid lipid.

[0072] The liquid lipid comprises 50% glyceryl linoleate and 50% isopropyl myristate of the total mass of the liquid lipid.

[0073] The isotonic regulator includes 100% glucose in the total mass of the isotonic regulator.

[0074] The solid lipid and the liquid lipid form ...

Embodiment 2

[0076] Doxorubicin nano-loading system, according to the mass ratio, includes 0.02% active ingredient containing doxorubicin, 1% solid lipid, 0.2% liquid lipid, 10% emulsifier and 0.5% isotonic regulator, and the balance is injection use water.

[0077] The active ingredient containing doxorubicin is a 1:1 mixture of doxorubicin and a sensitizer, and the sensitizer is curcumin.

[0078] The emulsifier contains polyethylene glycol 2000 vitamin E succinate with 5% of the total mass of the emulsifier, and the emulsifier also contains polysorbate with 95% of the total mass of the emulsifier.

[0079] The solid lipid comprises 100% stearic acid of the total mass of the solid lipid.

[0080] The liquid lipid comprises 100% propylene glycol monocaprylate of the total mass of the liquid lipid.

[0081] The isotonic regulator includes 100% glycerol in the total mass of the isotonic regulator.

[0082] The solid lipid and the liquid lipid form nanoparticles under the action of the em...

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Abstract

The invention discloses an adriamycin nano drug delivery system as well as a preparation method and application thereof. The drug delivery system comprises the following components in percentage by weight: 0.02%-1.5% of active ingredient containing adriamycin, 1%-20% of solid lipid, 0.1%-20% of liquid lipid, 0.5%-20% of emulsifier and 0.1%-5% of isoosmotic adjusting agent, wherein the solid lipid and the liquid lipid form nanoparticles to cover the active ingredient containing the adriamycin. The preparation method comprises the following steps: (1), uniformly dispersing the active ingredient containing the adriamycin, the solid lipid, the liquid lipid and fat-soluble emulsifier in an organic solvent, evaporating the organic solvent to obtain an oil phase; (2), uniformly dispersing other emulsifiers and the isoosmotic adjusting agent in water to obtain a water phase; (3), adding the water phase into the oil phase for emulsifying drop by drop; (4), homogenizing under high pressure; (5), cooling and degerming. The adriamycin nano drug delivery system disclosed by the invention can be used for realizing co-transporting of the adriamycin and a chemosensitizer, so that the killability of the adriamycin on liver cancer cells is strengthened.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and more specifically relates to a nano drug-carrying system, its preparation method and application. Background technique [0002] Primary hepatocellular carcinoma is a major disease that seriously endangers human health. It is highly malignant, invades and grows rapidly, and is easy to relapse after treatment. The 5-year survival rate is less than 5%. It is called "the king of cancers". At present, chemotherapy drugs for the treatment of primary liver cancer include doxorubicin, 5-fluorouracil, cisplatin, mitomycin, camptothecin, gemcitabine, sorafenib, etc. Clinical standard medication. However, liver cancer cells usually have primary drug resistance, and most liver cancers occur on the basis of existing liver diseases, which affect the absorption and metabolism of drugs, making the therapeutic effect of single chemotherapy drugs limited. Therefore, the current focus of research on anti-liv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/704A61K47/08A61K47/34A61P35/00A61K47/14A61K47/22A61K47/26
Inventor 刘卫赵小静唐和斌杨祥良李玉桑万江陵
Owner HUAZHONG UNIV OF SCI & TECH
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