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Nanometer capsule of anthracene nucleus anticancer antibiotic with polyethylene glycol-phospholipid

A technology of PEGylated phospholipids and nanomicelles, which can be used in antitumor drugs, medical preparations containing active ingredients, powder delivery, etc., can solve the problems of complex liposome preparation process and easy flocculation.

Active Publication Date: 2010-05-12
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, anthracycline antitumor antibiotic liposomes also have many shortcomings.
For example, the drug is encapsulated in the inner water phase, and the drug can only be effective when it is released from the liposome; the minimum particle size of the liposome is 50nm, and the liposome enters the cell through the mechanism of fusion and endocytosis. Therefore, the cytotoxicity of the drug encapsulated by liposomes is weaker than that of free drugs; the preparation process of liposomes is complicated, requiring the compounding of various lipid components (at least two lipid components), and particle size control requires special Equipment and devices; easy to flocculate during storage, etc.

Method used

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  • Nanometer capsule of anthracene nucleus anticancer antibiotic with polyethylene glycol-phospholipid
  • Nanometer capsule of anthracene nucleus anticancer antibiotic with polyethylene glycol-phospholipid

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preparation example Construction

[0032] The preparation method of the nanomicelle preparation of anthracycline antitumor antibiotics according to the present invention specifically comprises the following steps:

[0033] (1) Anthracycline antitumor antibiotics and pegylated phospholipids are dissolved in an organic solvent;

[0034] (2) removing the organic solvent to obtain a polymer lipid film containing anthracycline antitumor antibiotics;

[0035] (3) adding water or a buffer solution to the polymer lipid film obtained in the above (2), and hydrating at 25° C. to 60° C.;

[0036] (4) Vortex shaking or ultrasonication to obtain PEGylated phospholipid nanomicelles loaded with anthracycline antitumor antibiotics.

[0037] The organic solvent in the method step (1) of the present invention is methanol, ethanol, chloroform, or a mixture thereof.

[0038] In step (2) of the process according to the invention, the organic solvent is removed by reducing pressure and / or removing the organic solvent under vacuum....

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Abstract

This invention provides an intravenous injection approvable anthracene-nucleus antineoplastic-antibiotic nanomicelle drug, which comprises anthracene-nucleus antineoplastic antibiotic, macrogol derivelized phosphatide those have therapy dose, and findings acceptable in medicine. In the nanomicelle, the macrogol wraps around the drug hydrophobilic nucleuses and forms hydrophilic protective layer, this can provide the drugs from contacting with proteins in blood and identifying and licking up by esoderma system in body, so the drug cycle time in body will be prolonged.

Description

technical field [0001] The invention relates to a nanomicelle preparation of intravenously injectable anthracycline antitumor antibiotics and a preparation method thereof. Background technique [0002] Anthracycline anti-tumor antibiotics are a class of effective broad-spectrum anti-tumor drugs, which are widely used in clinical treatment of 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 (THP-ADM), Aclacinomycin (ACM). However, like other cytotoxic antineoplastic drugs, it lacks selectivity to tumor tissue and has severe dose-dependent acute toxicity, which is clinically manifested as nausea, vomiting, hair loss, and bone marrow suppression. What's more serious: repeated medication, drug accumulation in the heart tissue leads to serious irreversible heart damage. The toxic and side ef...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/704A61K9/00A61K9/19A61P35/00
CPCA61K9/1075A61K9/0019A61P35/00A61P35/02
Inventor 梁伟唐宁张春玲饶子和
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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