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Preparation method and application of redox-sensitive targeting polymer and drug-loaded micelles thereof

A polymer, sensitive technology, applied in the field of chemical medicine, can solve the problem of non-specific targeting of tumor sites and other problems

Active Publication Date: 2020-04-14
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although this polymer drug-loaded micelle can reduce the leakage of drugs in the blood, it cannot specifically target the tumor site.

Method used

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  • Preparation method and application of redox-sensitive targeting polymer and drug-loaded micelles thereof
  • Preparation method and application of redox-sensitive targeting polymer and drug-loaded micelles thereof
  • Preparation method and application of redox-sensitive targeting polymer and drug-loaded micelles thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Synthesis of embodiment 1folate (folic acid)-PEG-PLG (SH)-Pphe polymer

[0060] (1) Synthesis of folate-SH: Weigh 0.44g (1mM) of folic acid, 0.3g (1.5mM) of DCC (1.5mM) and 0.14g (1.2mM) of NHS and dissolve them in 30mL of dry DMSO, react at room temperature for 24 hours; add 28mg of aminoethanol (0.36mM) and 0.0730mL triethylamine, continue to react at room temperature for 2 days. After the reaction, the reaction solution was poured into a dialysis bag (MWCO=3500), dialyzed for 48 hours, and the water was changed every 12 hours, and then the reaction solution was lyophilized to obtain folate-SH as a yellow solid. Yield 80%.

[0061]

[0062] (2) Synthesis of Mal-PEG-NH 2 : PEG 5g (1mM), Fmoc-Phe 0.74g (2mM), EDCI 0.22g (1.2mM) and DMAP 0.15g (1.2mM) were dissolved in 100mL dry DCM, and reacted at room temperature for 48 hours. After the reaction, the reaction solution was extracted with 1mM hydrochloric acid (100mL×3), washed with a saturated aqueous sodium chlor...

Embodiment 2

[0073] The preparation of embodiment 2 polymer critical micelles

[0074] Folate-PEG-PLG(SH)-PPhe micelles (fPGPM) were prepared by dialysis. Weigh 100 mg of polymer folate-PEG-PLG(SH)-PPhe and dissolve it in 4 mL of DMSO. After it is completely dissolved, add 10 times the equivalent of sodium borohydride to break the disulfide bond. After stirring for 30 min, 5 mL of PBS (pH 7.4) was added and stirred at 50° C. for 1 h. Then pour the mixed solution into a dialysis bag with a molecular weight cut-off of 1000 Da, dialyze at room temperature for 36 hours, and change the water (PBS) every 12 hours. After dialysis, the micellar solution was passed through a 0.45 μm injection microporous membrane, and sealed and stored at 4° C. for future use.

[0075] Prepare 6×10 -7 For the methanol solution of Piperium M, add 1mL of pyrene solution into the brown cillin bottle, and after the methanol volatilizes, dilute the original micellar solution, and prepare it in the cilin bottle from 2...

Embodiment 3

[0077] Example 3 Preparation of DOX-loaded folate-PEG-PLG(HS)-PPhe(DOX-fPGPM) micelles

[0078] Folate-PEG-PLG(SH)-PPhe micelles (DOX-fPGPM) loaded with DOX were prepared by dialysis. Weigh 50 mg polymer folate-PEG-PLG(SH)-PPhe and 5.4 mg DOX·HCl and dissolve in 2 mL DMSO. After complete dissolution, add 5 μL triethylamine to deprotonate DOX, and add 10 times the equivalent of boron Sodium hydride, breaks disulfide bonds. After stirring for half an hour, 4 mL of PBS (pH 7.4) was added, oxygen was continuously introduced into it, and stirred at 50° C. for 1 hour. Then pour the mixed solution into a dialysis bag with a molecular weight cut-off of 1000Da, dialyze at room temperature for 36 hours, change the water (PBS) every 12 hours, and pass oxygen into it for a certain period of time. After dialysis, the micellar solution was passed through a 0.45 μm injection microporous membrane, and sealed and stored at 4° C. for future use. Another part of the micelles was freeze-dried ...

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Abstract

The invention belongs to the field of a chemical medicine, and more specifically relates to a targeting polymer having oxidation-reduction sensitivity and a preparation method of drug-loaded micelle and a purpose thereof. The invention provides the targeting polymer having oxidation-reduction sensitivity with a structure shown as a formula I. The invention provides the targeting polymer having oxidation-reduction sensitivity and the preparation method of the drug-loaded micelle and the purpose thereof. The Drug-R-PGPM of the provided targeting polymer having oxidation-reduction sensitivity andcarried with a hydrophobic antineoplastic small molecular drug has a large application prospect for tumor targeting treatment.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to a redox-sensitive targeting polymer and a preparation method and application of drug-loaded micelles thereof. Background technique [0002] With the deepening of our research on tumor biology, there are new diagnosis and treatment methods for cancer, but cancer is still one of the main reasons that threaten human life and health. This is due to the lack of therapeutic drugs or formulations that can selectively target tumor cells without causing damage to normal tissues. The current treatment for most cancers is a combination of surgical resection, radiotherapy, and chemotherapy. However, these therapies have non-specific damage to normal cells, which makes the morbidity and mortality of patients very high. Therefore, it is necessary to develop agents that can selectively target tumor tissues, overcome biological barriers, and have intelligent response mechanisms acco...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/46C08G69/40C08G65/48A61K9/107A61K47/34A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/34C08G65/48C08G69/40C08G69/46
Inventor 陈俐娟汪周峰
Owner SICHUAN UNIV
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