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PH-response anti-cancer medicinal preparation and preparation method thereof

A technology of anti-cancer drugs and anti-cancer active substances, which is applied in the field of pH-responsive anti-cancer drug preparations and its preparation, can solve the problems of practical application limitations, high metal content, and threat to drug safety, and achieve high safety and particle size. Uniform diameter and low toxicity

Inactive Publication Date: 2013-11-20
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the carrier of this system is not a biodegradable material, which limits its practical application
Patent applications CN201010283898.X and CN201010283937.6 disclose the technical solution of the drug-metal-polymer pH-responsive drug delivery system based on the coordination bond, which solves the problem of degradability of the carrier, but the metal content is too high ( More than 10%), threatening the safety of medication

Method used

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  • PH-response anti-cancer medicinal preparation and preparation method thereof
  • PH-response anti-cancer medicinal preparation and preparation method thereof
  • PH-response anti-cancer medicinal preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] The pH-responsive anticancer pharmaceutical preparations involved in this embodiment include that the anticancer pharmaceutical preparations contain mitoxantrone, albumin and Zn ions. The preparation method comprises the following steps:

[0033] Dissolve 100 mg of BSA in 1 mL of NaCl (10 mM) solution, adjust the pH to 8.0, add 4 mL of ethanol at a rate of 1 mL / min under stirring, and centrifuge to obtain albumin particles.

[0034] Put the albumin particles in a 0.1M ethanol solution of zinc nitrate to load zinc, and centrifuge to obtain albumin-zinc particles;

[0035] The obtained albumin-zinc granule is placed in a mitoxantrone solution, loaded with mitoxantrone, and centrifuged to obtain the drug-loaded albumin-zinc granule, which is a pH-responsive anticancer drug preparation.

[0036] Scanning electron microscope images of albumin-zinc particles and drug-loaded albumin-zinc particles figure 1 shown. The particle size of the obtained nanoparticles was measured ...

Embodiment 2

[0038] The pH-responsive anticancer pharmaceutical preparations involved in this embodiment include that the anticancer pharmaceutical preparations include doxorubicin hydrochloride, albumin and Zn ions. The preparation method comprises the following steps:

[0039] Dissolve 30 mg of BSA in 1 mL of NaCl (5 mM) solution, adjust the pH to 7.0, add 2 mL of ethanol at a rate of 1.2 mL / min under stirring, and centrifuge to obtain albumin particles;

[0040]placing the albumin particles in a 0.2M zinc chloride ethanol solution to load zinc, and centrifuging to obtain albumin-zinc particles;

[0041] The obtained albumin-zinc granules are placed in a doxorubicin hydrochloride solution, loaded with doxorubicin hydrochloride, and then filtered to obtain the drug-loaded albumin-zinc granules. The particle size of the obtained nanoparticles was measured, and the average particle size was less than 200nm. The mass percentage of zinc in the sample was tested by plasma mass spectrometry t...

Embodiment 3

[0043] The pH-responsive anticancer pharmaceutical preparations involved in this embodiment include that the anticancer pharmaceutical preparations include daunorubicin hydrochloride, albumin and Zn ions. The preparation method comprises the following steps:

[0044] Dissolve 200 mg of BSA in 1 mL of NaCl (20 mM) solution, adjust the pH to 9.0, add 10 mL of ethanol at a rate of 0.8 mL / min under stirring, and centrifuge to obtain albumin particles;

[0045] placing the albumin particles in a 0.05M zinc acetate ethanol solution to load zinc, and centrifuging to obtain albumin-zinc particles;

[0046] The obtained albumin-zinc particles are placed in a daunorubicin hydrochloride solution, loaded with daunorubicin hydrochloride, and freeze-dried to obtain the drug-loaded albumin-zinc particles. The particle size of the obtained nanoparticles was measured, and the average particle size was less than 200nm. The mass percentage of zinc in the sample was tested by plasma mass spectr...

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Abstract

The invention relates to a pH-response anti-cancer medicinal preparation and a preparation method of the pH-response anti-cancer medicinal preparation, relating to the technical field of medicines. The anti-cancer medicinal preparation comprises an anti-cancer active drug, albumin and Zn ions, wherein a coordinate bond is formed between the Zn ions and the anti-cancer active substances, and the preparation method of the anti-cancer medicinal preparation comprises the steps of: (a) preparing albumin grains by a conventional method, (b) adding the albumin grains to ethanol solution of zinc salt, centrifuging or filtering, obtaining albumin-zinc grains, and (c) adding the albumin-zinc grains into solution containing anti-cancer active drug, centrifuging, filtering or directly freezing and drying the solution, and obtaining the pH-response anti-cancer medicinal preparation. The pH-response anti-cancer medicinal preparation, disclosed by the invention, is sensitive to pH response, ensures the anti-cancer drug not to be released basically in blood circulation, and abundantly released at an anti-cancer part, has less toxicity while improving the targeting of the anti-cancer drug, selects the albumin as high polymer material, and has the advantages of low toxicity, good biocompatibility and high safety.

Description

technical field [0001] The invention relates to an anticancer drug preparation in the technical field of medicine and a preparation method thereof, in particular to a pH-responsive anticancer drug preparation and a preparation method thereof. Background technique [0002] Cancer is a disease caused by a malfunction in the mechanisms that control cell growth and proliferation. In addition to growing out of control, cancer cells can also locally invade surrounding normal tissues, and even transfer to other parts of the body through the circulatory system or lymphatic system. According to statistics, 12 million people worldwide are diagnosed with cancer every year, and 7.6 million people die of cancer. Moreover, the incidence of cancer is still increasing. It is estimated that there will be 26 million new cases and 17 million deaths worldwide in 2030, most of which will occur in low- and middle-income developing countries. In some western countries, such as the United States,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K47/42A61K47/02A61P35/00
Inventor 车顺爱李晨光
Owner SHANGHAI JIAO TONG UNIV
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