Preparation method and application of low-molecular-weight heparin-antitumor drug electrostatic complex nano system

An anti-tumor drug and low-molecular-weight heparin technology, which is applied in the field of self-assembled nanosystems of low-molecular-weight heparin-anti-tumor drug electrostatic complexes and its preparation, can solve problems such as bleeding and side effects, and achieve high drug loading and high Effects of safety, good biocompatibility and biosafety

Inactive Publication Date: 2019-12-10
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the toxic and side effects of hemorrhage when low molecular weight heparin is used as an antitumor drug is an important factor that limits its clinical use in tumor suppression

Method used

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  • Preparation method and application of low-molecular-weight heparin-antitumor drug electrostatic complex nano system
  • Preparation method and application of low-molecular-weight heparin-antitumor drug electrostatic complex nano system
  • Preparation method and application of low-molecular-weight heparin-antitumor drug electrostatic complex nano system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1: Preparation of Low Molecular Weight Heparin-Adriamycin Electrostatic Complex

[0065] Dissolve low molecular weight heparin (100 mg) in an appropriate amount of deionized water, dissolve adriamycin hydrochloride (10 mg, calculated as adriamycin hydrochloride) in an appropriate amount of deionized water, and dissolve adriamycin hydrochloride The saline solution was quickly added to the low-molecular-weight heparin solution, and stirring was continued at room temperature for 12 hours. The precipitate is separated by centrifugation, and the obtained precipitate is dispersed in dimethyl sulfoxide to obtain a dimethyl sulfoxide solution of the low-molecular-weight heparin-doxorubicin electrostatic complex.

Embodiment 2

[0066] Example 2: Preparation of Low Molecular Weight Heparin-Adriamycin Electrostatic Complex

[0067] Dissolve low molecular weight heparin (100 mg) in an appropriate amount of deionized water, dissolve adriamycin hydrochloride (20 mg, calculated as adriamycin hydrochloride) in an appropriate amount of deionized water, and dissolve adriamycin hydrochloride The saline solution was quickly added to the low-molecular-weight heparin solution, and stirring was continued at room temperature for 12 hours. The precipitate is separated by centrifugation, and the obtained precipitate is dispersed in dimethyl sulfoxide to obtain a dimethyl sulfoxide solution of the low-molecular-weight heparin-doxorubicin electrostatic complex.

Embodiment 3

[0068] Example 3: Preparation of Low Molecular Weight Heparin-Adriamycin Electrostatic Complex

[0069] Low-molecular-weight heparin (100 mg, calculated as doxorubicin hydrochloride) was dissolved in an appropriate amount of deionized water, and adriamycin hydrochloride (50 mg) was dissolved in an appropriate amount of deionized water, and the doxorubicin hydrochloride was dissolved under stirring. The saline solution was quickly added to the low-molecular-weight heparin solution, and stirring was continued at room temperature for 12 hours. The precipitate is separated by centrifugation, and the obtained precipitate is dispersed in dimethyl sulfoxide to obtain a dimethyl sulfoxide solution of the low-molecular-weight heparin-doxorubicin electrostatic complex.

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Abstract

The invention relates to a preparation method and application of a low-molecular-weight heparin-antitumor drug electrostatic complex nano system. (1) A low-molecular-weight heparin-antitumor drug electrostatic complex is prepared by using the electrostatic interaction between low-molecular-weight heparin with extremely high negative electricity and a positively charged amphoteric antitumor drug. (2) The prepared electrostatic complex can self-assemble in water to form spherical nanoparticles with a uniform particle size. The low-molecular-weight heparin-antitumor drug electrostatic complex nano system of the invention has the advantages of simple preparation method and high drug loading capacity. Meanwhile, the low-molecular-weight heparin-antitumor drug electrostatic complex nano system has the functions of reducing the anticoagulant and hemolytic toxic and side effects of the low-molecular-weight heparin carrier, achieving targeted delivery of antitumor drugs, and improving the efficacy of antitumor drugs. In vivo and in vitro tumor cell growth inhibition results prove that the system has excellent anti-tumor effects and has good application prospects.

Description

technical field [0001] The invention relates to the technical field of nano-pharmaceutical preparations, in particular to a self-assembled nano-system of low-molecular-weight heparin-anti-tumor drug electrostatic complexes and a preparation method and application thereof. Background technique [0002] Chemotherapy drugs are one of the commonly used methods for clinical treatment of tumor diseases, but the non-selective distribution of free drugs in the whole body and the killing of cells are important reasons for the serious side effects of chemotherapy drugs. For example, doxorubicin hydrochloride can be distributed in the heart and thus Cardiotoxicity is caused, and heart failure may occur in severe cases, which greatly restricts its application and development. [0003] The nano-delivery system has the advantages of sustained release, passive targeting, improved bioavailability, prolonged circulation time in the body, improved pharmacokinetics, and reduced toxic and side ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/727A61K45/06A61P35/00A61P35/02A61K31/138A61K31/704
CPCA61K31/727A61K45/06A61P35/00A61P35/02A61K31/138A61K31/704
Inventor 张烜张爽
Owner PEKING UNIV
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