Multifunctional high molecular micelle drug delivering system and preparation method and application thereof

A technology of polymer micelles and delivery systems, applied in the field of design targets, to increase the variety, enhance stability, and facilitate research and development

Active Publication Date: 2019-01-04
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the therapeutic effect of mercaptododecaborane disodium salt on tumors needs to be improved, and there is still a lack of a multifunctional polymer micelle nano-drug delivery system for efficient delivery of mercaptododecaborane disodium salt to improve tumor cells' ability to respond to sulfhydryl groups. Endocytosis of dodecaborane disodium salt, targeted drug delivery and boron neutron capture therapeutic efficacy

Method used

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  • Multifunctional high molecular micelle drug delivering system and preparation method and application thereof
  • Multifunctional high molecular micelle drug delivering system and preparation method and application thereof
  • Multifunctional high molecular micelle drug delivering system and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] In this example, polyethylene glycol-polylysine block copolymer and 3,3'-dithiobispropioimidate dimethyl dihydrochloride were used as raw materials to construct a polymer micellar drug carrier system. The drug molecule is mercaptododecaborane disodium salt, and the process steps are as follows:

[0045] (1) Synthesis of polymer materials

[0046] Dissolve 50 mg of 3,3'-dithiobispropioimidate dimethyl dihydrochloride side chain modified polyethylene glycol-polylysine block copolymer in 15 ml of HEPES buffer solution (10 mM , pH 7.4), 34 mg of medicinal mercaptododecaborane disodium was dissolved in 4 ml of HEPES buffer solution (10 mM, pH 7.4), then the two solutions were mixed, stirred and reacted for 6 hours, and then the products were washed with HEPES respectively The buffer solution and pure water were dialyzed for 24 hours to form polymer micelles dissolved in disodium mercaptododecaborane through self-assembly.

[0047] (2) Cross-linking of drugs and polymer mat...

Embodiment 2

[0051] In this example, polyethylene glycol-polylysine block copolymer and 3,3'-dithiobispropioimidate dimethyl dihydrochloride were used as raw materials to construct a polymer micellar drug carrier system. The drug molecule is mercaptododecaborane disodium salt, and the process steps are as follows:

[0052] (1) Synthesis of polymer materials

[0053] At 25°C, 100 mg of polyethylene glycol-polylysine block copolymer was dissolved in 10 mL of borate buffer with a concentration of 100 mM and a pH value of 9.0, while 50 mg of 3,3'-bis Thiobispropionimidate dimethyl dihydrochloride was dissolved in 12mL concentration of 100mM, pH value of 9.0 borate buffer, the two solutions were mixed at room temperature for 60 minutes, and then the reaction product in 10mM, pH7 .4 Dithiothreitol was dialyzed three times, then added 70mg dithiothreitol to react for 50 minutes, then dialyzed three times with phosphate buffer solution and pure water, and finally obtained 3,3'-dithiobispropionimi...

Embodiment 3

[0057] In this example, polyethylene glycol-polylysine block copolymer and 3,3'-dithiobispropioimidate dimethyl dihydrochloride were used as raw materials to construct a polymer micellar drug carrier system. The drug molecule is mercaptododecaborane disodium salt, and the process steps are as follows:

[0058] (1) Synthesis of polymer materials

[0059] At 25°C, 100 mg of polyethylene glycol-polylysine block copolymer was dissolved in 10 mL of borate buffer with a concentration of 100 mM and a pH value of 9.0, while 150 mg of 3,3'-bis Thiobispropionimidate dimethyl dihydrochloride was dissolved in 15mL concentration of 100mM, pH value of 9.0 borate buffer, the two solutions were mixed at room temperature for 120 minutes, and then the reaction product in 10mM, pH7 .4 Dithiothreitol was dialyzed three times, then added 200 mg dithiothreitol to react for 60 minutes, then dialyzed three times with phosphate buffer solution and pure water, and finally obtained 3,3'-dithiobispropio...

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Abstract

The invention belongs to the technical field of targeted drug delivery, and relates to a multifunctional high molecular micelle drug delivering system and a preparation method and application thereof.Some side chains of a polyethylene glycol-polylysine block copolymer are chemically modified by dimethyl 3,3'-dithiobispropionimidate dihydrochloride to obtain thiol-containing groups, and then a thiol-containing boron neutron capturing therapeutic drug disodium thiol dodecaborane reacts with the side chains through disulfide bonds to form stable multifunctional high molecular micelles in a watersolution through self-assembly and the crosslinkinging action of some free disulfide bonds; the prepared high molecular micelles can deliver the thiol-containing drug disodium thiol dodecaborane or other thiol-containing drugs or prodrugs, so that the content of the drug delivered to tumor cells is increased and a targeted therapeutic effect on tumors is enhanced.

Description

technical field [0001] The present invention designs the technical field of targeted drug delivery, and relates to a multifunctional polymer micellar drug delivery system and its preparation method and application. It has the ability to improve the stability of the drug delivery system through disulfide bond crosslinking, and realize the escape of endosomes into tumor cells. New applications of highly efficient drug delivery and drug release in response to glutathione, also particularly related to the application of radiotherapy and / or neutron capture therapy / chemotherapy drugs in the preparation of therapeutic tumors or malignancies. Background technique [0002] The drug delivery system is a kind of drug delivery system and a way of drug preparation. The drug delivery system is mainly constructed with drug carrier materials (such as polymer materials) to load biologically active substances / drugs and deliver them to the lesion site Play a medicinal effect. The drug deliver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K41/00A61P35/00
CPCA61K41/0095A61K47/60A61K47/6907A61P35/00
Inventor 米鹏刘静
Owner SICHUAN UNIV
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