A res macrophage blocking material, a series of drugs for tumor multi-step therapy and its application

A technology of macrophages and drugs, applied in multidisciplinary fields, can solve the problems of poor tumor treatment effect, low drug concentration, body damage, etc., achieve good biocompatibility and biodegradability, small body damage, reduce Toxic effects

Active Publication Date: 2019-06-18
HUAZHONG UNIV OF SCI & TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Aiming at the above deficiencies or improvement needs of the prior art, the present invention provides a RES macrophage blocking material, a series of drugs for tumor multi-step therapy and their applications, the purpose of which is to synthesize hydroxyethyl starch-polysaccharides with different grafting ratios. Lactic acid nanoparticles are used as RES blockade materials and drug carrier materials for temporary blocking of the RES system respectively. The RES blockade strategy combined with the hydroxyethyl starch-polylactic acid drug-loaded nanoparticle drug-loading system is applied to tumor treatment, thereby solving the problem of the existing technology. The non-specific uptake of drug-loaded nanoparticles by the reshaped endothelial system (RES) eventually leads to low concentration of the drug enriched in the tumor site, poor tumor treatment effect, and the existing RES macrophage blocking material caused by excessive dosage of the body. Damaged technical issues

Method used

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  • A res macrophage blocking material, a series of drugs for tumor multi-step therapy and its application
  • A res macrophage blocking material, a series of drugs for tumor multi-step therapy and its application
  • A res macrophage blocking material, a series of drugs for tumor multi-step therapy and its application

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preparation example Construction

[0041] The preparation method of the reticuloendothelial system macrophage blocking material comprises the following steps:

[0042] (1) Dissolving polylactic acid and activating its terminal carboxyl group: Add catalyst N-N'-dicyclohexylcarbodiimide and 4-dimethylaminopyridine to 0.2-0.7 g of carboxyl-terminated polylactic acid, and use anhydrous dimethylaminopyridine Sulfoxide is used as a solvent, and the quality of the polylactic acid is preferably 0.3-0.4 g, and it is reacted at 50-70°C for 25-45 minutes to completely dissolve it to obtain polylactic acid activated by the carboxyl group; the polylactic acid, N-N' -The molar ratio of dicyclohexylcarbodiimide and 4-dimethylaminopyridine is 1:4:2;

[0043](2) Dissolving hydroxyethyl starch: under the condition of nitrogen protection, fully dissolve 0.5 g of hydroxyethyl starch in anhydrous dimethyl sulfoxide at 50-70 ° C to obtain a dimethyl sulfoxide solution of hydroxyethyl starch;

[0044] (3) Esterification reaction: th...

Embodiment 1

[0062] Prepare a kind of tumor two-step therapy series medicine, comprise medicine A and medicine B, the preparation steps of medicine A RES blockade hydroxyethyl starch-polylactic acid block polymer are as follows:

[0063] 0.323g carboxyl-terminated polylactic acid (PLA-COOH), N-N'-dicyclohexylcarbodiimide (DCC), 4-dimethylaminopyridine (DMAP), (where PLA, DCC, and DMAP are fed The molar ratio is 1:4:2) placed in a 100mL dry round bottom flask. At the same time, 15 mL of anhydrous dimethyl sulfoxide (DMSO) solvent under nitrogen protection was added, and stirred at 60° C. for 30 min to completely dissolve the reactant and activate its terminal carboxyl group.

[0064] At the same time, 0.5 g of hydroxyethyl starch HES was dissolved in 10 mL of anhydrous DMSO solvent, and the reaction time at 60 ° C was 30 min. Add the DMSO solution of PLA, DCC, and DMAP to the fully dissolved HES solution, and add 5ml of anhydrous DMSO to rinse the flask in which the PLA was dissolved, and ...

Embodiment 2

[0072] Prepare a kind of tumor two-step therapy series medicine, comprise medicine A and medicine B, the preparation steps of medicine A RES blockade hydroxyethyl starch-polylactic acid block polymer are as follows:

[0073] 0.404g carboxyl-terminated polylactic acid (PLA-COOH), N-N'-dicyclohexylcarbodiimide (DCC), 4-dimethylaminopyridine (DMAP), (wherein PLA, DCC, DMAP three feed The molar ratio is 1:4:2) in a dry 100mL round bottom flask. At the same time, 15 mL of anhydrous dimethyl sulfoxide (DMSO) solvent under nitrogen protection was added, and stirred at 60° C. for 30 min to completely dissolve the reactant and activate its terminal carboxyl group.

[0074] At the same time, 0.5g of hydroxyethyl starch HES was dissolved in 10mL of anhydrous DMSO solvent, and the reaction time was 30min at 60°C. Add the DMSO solution of PLA, DCC, and DMAP to the fully dissolved HES solution, and add 5ml of anhydrous DMSO to rinse the flask in which the PLA was dissolved, and then add th...

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Abstract

The invention provides a novel reticuloendothelial system macrophage blocking material, in order to solve the problem that a reticuloendothelial system can achieve non-specific uptake on tumor therapy drug loaded nanoparticles while an existing RES (reticuloendothelial system) macrophage blocking material, which is excessive in using dose, can cause body injury. The novel reticuloendothelial system macrophage blocking material is a hydroxyethyl starch-polylactic acid segmented polymer which is about 700nm in size. The invention also provides tumor multi-step therapy series medicines, wherein the series medicines include a medicine A and a medicine B; the medicine A consists of the reticuloendothelial system (RES) macrophage blocking material and the medicine B includes drug-loaded nanoparticles of an anti-tumor medicine, namely hydroxyethyl starch-polylactic acid, and the particle size of the drug-loaded nanoparticles is about 140nm. By applying the combination of an RES blockade strategy and a hydroxyethyl starch-polylactic acid drug-loaded nano-system to the preparation of the tumor treating medicines, the aggregation of the anti-tumor medicines in a tumor site can be significantly improved, cardiotoxicity and hepatotoxicity of the medicines can be relieved and a tumor treatment efficiency can be improved.

Description

technical field [0001] The invention belongs to the interdisciplinary fields of chemistry, pharmacy, medicine, etc., and more specifically relates to a RESblockade strategy combined with hydroxyethyl starch-polylactic acid nanoparticle drug delivery system and its application. Background technique [0002] Chemotherapy is currently one of the most effective means of treating cancer. Chemotherapy drugs will spread throughout most of the organs and tissues of the body along with the blood circulation. As a systemic treatment, chemotherapy is currently the most important treatment for some tumors that tend to spread throughout the body and advanced tumors that have metastasized. However, current chemotherapeutic drugs have great defects: the non-specific targeting of chemotherapeutic drugs leads to the killing of normal cells as well as tumor cells by chemotherapeutic drugs, and the treatment process often causes irreversible damage to normal tissues of the body. Lowering the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K47/34A61K31/704A61K31/765A61P35/00C08G81/00
CPCA61K31/704A61K31/765A61K47/34A61K47/36C08G81/00A61K2300/00
Inventor 杨祥良李子福万影徐辉碧余婵周庆
Owner HUAZHONG UNIV OF SCI & TECH
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