Antharcycline antitumor antibiotics loaded nano-micelle preparation and preparation method thereof

A nanomicelle, anti-tumor technology, applied in the field of biomedical materials, can solve the problems of low drug loading, dissociation, etc., achieve uniform particle size, improve stability, and increase loading capacity

Inactive Publication Date: 2013-03-20
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the problems of low drug loading, sudden release of drugs and drug dissociation in polymer bonded drugs in the existing micellar preparations, and provide a nano-sized drug loaded with anthracycline antitumor antibiotics Micellar formulation and preparation method

Method used

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  • Antharcycline antitumor antibiotics loaded nano-micelle preparation and preparation method thereof
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  • Antharcycline antitumor antibiotics loaded nano-micelle preparation and preparation method thereof

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preparation example Construction

[0034] The preparation method of the A-B-C type triblock polymer of the present invention is a known technology, and the specific preparation steps are as follows:

[0035] Step 1: Under the protection of nitrogen, put PEGs of different molecular weights into the reaction vessel, add the solvent toluene for azeotropic water removal, after 2-5 hours, add cerium hydroxide into the reaction vessel, and stir the reaction at 40°C-70°C After 2-4 hours, remove the solvent, continue to add allyl glycidyl ether, react at 20°C-50°C for 12-24 hours, cool to room temperature, settle with 200-500mL ether, filter, and vacuum dry to obtain solid powder PEG-PAGE , the molar ratio of PEG, cerium hydroxide and allyl glycidyl ether is 1:1:4-20;

[0036] The second step: Take the above PEG-PAGE and dissolve it in 10-50 mL of THF. After stirring and dissolving, add the catalyst Zn[N(SiMe 3 ) 2 ] 2 After reacting with polyester monomer and stirring at room temperature for 2-10 hours, settle with...

Embodiment 1

[0051] Example 1: Preparation of nanomicelles encapsulating doxorubicin with A-B-C type triblock polymers of different molecular weights

[0052] Table 1

[0053]

[0054] According to the formula in Table 1, 100 mg of A-B-C triblock polymer was weighed and dissolved in acetonitrile, and placed in a round-bottomed flask. The concentration of the A-B-C triblock polymer was 1 mg / mL. , evaporated the organic solvent to form a thin and uniform polymer film on the surface of the round bottom flask, dissolved 10 mg doxorubicin (ADM) in water to obtain an aqueous solution of doxorubicin, the concentration of ADM was 0.1 mg / mL, Add the aqueous solution of doxorubicin to the round bottom flask, 60 o Hydrate at C for 1 min, filter and sterilize with a 0.22 um microporous membrane to obtain a nanomicelle solution, and freeze-dry to obtain a nanomicelle lyophilized powder loaded with anthracycline antitumor antibiotics. The obtained samples P1-P6 have a spherical structure with a pa...

Embodiment 2

[0055] Embodiment 2: Prepare the nano-micelle of wrapping daunorubicin with the A-B-C type triblock polymer of different molecular weights

[0056] Table 2

[0057]

[0058] According to the formula in Table 2, 100 mg of the A-B-C type triblock polymer was weighed and dissolved in acetone, and placed in a round bottom flask. The concentration of the A-B-C type triblock polymer was 10 mg / mL. , evaporate the organic solvent to form a thin and uniform polymer film on the surface of the round bottom flask, and dissolve 5 mg daunorubicin (DNR) in sodium chloride injection to obtain an aqueous solution of daunorubicin. The concentration of ADM is 0.5 mg / mL, the aqueous solution of daunorubicin is added in the round bottom flask, 70 o Hydrate at C for 5 min, filter and sterilize with a 0.22 um microporous membrane to obtain a nanomicelle solution, and freeze-dry to obtain a nanomicelle lyophilized powder loaded with anthracycline antitumor antibiotics. The obtained samples P7-P...

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Abstract

The invention discloses an antharcycline antitumor antibiotics loaded nano-micelle preparation, which comprises antharcycline antitumor antibiotics, A-B-C type triblock polymer and assisting agents, wherein the antharcycline antitumor antibiotics is one or more of adriamycin, daunorubicin, pharmorubicin, perarubicin or lacinomycin; and the A-B-C type triblock polymer is polyethylene glycol-polyethylene glycol containing carboxyl on side chain-polyester. According to the preparation, drugs are coated in the nano-micelle by virtue of the coaction of self-assembly of segmented copolymer and electrostatic adsorption, the nano-micelle has uniform and stable grain diameter, the encapsulation efficiency reaches 99 percent, and the prepared nano-micelle preparation is of a spherical structure with grain diameter between 20 and 300nm; and the shell of the micelle is made from polyethylene glycol molecules, so that drugs are prevented from being contacted with enzyme and other protein molecules in blood or identified and swallowed by a reticuloendothelial system in the body, so that the circulating period of micelle in the body can be prolonged.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a nanomicelle preparation loaded with anthracycline antitumor antibiotics and a preparation method. Background technique [0002] Anthracycline antitumor antibiotics are a class of effective broad-spectrum antitumor drugs, which are widely used clinically to treat various cancers, such as leukemia, lymphoma, breast cancer, lung cancer, liver cancer and many other solid tumors. Such antineoplastic drugs mainly include: Doxorubicin (ADM), Daunorubicin (DNR), Epirubicin (Epirubicin, EPI), Pirarubicin (Pirarubicin, THP-ADM), Aclacinomycin (ACM). At present, clinical administration is mostly intravenous infusion, but anthracycline antineoplastic drugs cannot pass through the blood-brain barrier, and they are rapidly distributed throughout the body after intravenous injection, and have relatively serious side effects on bone marrow and heart. Simultaneously, the dose o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/704A61K47/34A61P35/00
Inventor 景遐斌胡秀丽张文静王瑞郑勇辉谢志刚黄宇彬
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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