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Glutathione response-type dual-drug carrier as well as preparation method and application thereof

A glutathione and dual technology, applied in the field of biomedical engineering materials, can solve the problem that the application of glutathione-responsive hyperbranched polyamidoamine dual drug carrier has not yet been reported, and achieves the promotion of drug synergy and convenient operation. , good water solubility

Active Publication Date: 2017-12-26
广州元合生物科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, glutathione-responsive hyperbranched polyamidoamine dual drug carriers prepared by Michael addition and amidation reactions and their applications have not been reported

Method used

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  • Glutathione response-type dual-drug carrier as well as preparation method and application thereof
  • Glutathione response-type dual-drug carrier as well as preparation method and application thereof
  • Glutathione response-type dual-drug carrier as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Synthesis of N,N'-bis(acryloyl)cystamine (CBA)

[0060] Dissolve cystamine dihydrochloride and solid sodium hydroxide in pure water respectively, dissolve acryloyl chloride in dichloromethane, and then slowly alternate sodium hydroxide aqueous solution and acryloyl chloride in dichloromethane under ice bath conditions for 20 minutes Add dropwise to the aqueous solution of cystamine dihydrochloride, react at room temperature for 6 hours after the dropwise addition, magnetically stir during the reaction, and the rotation speed is 300rpm; Vacuum-dried at 40°C for 12 hours to obtain N,N'-bis(acryloyl)cystamine (CBA).

[0061] The mol ratio of described cystamine dihydrochloride, sodium hydroxide, acryloyl chloride is 1:2.7:2.5; The volume ratio of dichloromethane and reaction system solution used during the extraction is 20:1; The amount is 4 times by mass of cystamine dihydrochloride, 2.5 times by mass of sodium hydroxide, and the amount of dichloromethane used...

Embodiment 2

[0062] Example 2: Synthesis of N,N'-bis(acryloyl)cystamine (CBA)

[0063] Dissolve cystamine dihydrochloride and solid sodium hydroxide in pure water respectively, dissolve acryloyl chloride in dichloromethane, and then slowly alternate sodium hydroxide aqueous solution and acryloyl chloride in dichloromethane under ice bath conditions for 100 minutes Add dropwise to the aqueous solution of cystamine dihydrochloride, react at room temperature for 12 hours after the dropwise addition, magnetically stir during the reaction, and the rotation speed is 600rpm; Vacuum-dried at 40°C for 24 hours to obtain N,N'-bis(acryloyl)cystamine (CBA).

[0064] The mol ratio of described cystamine dihydrochloride, sodium hydroxide, acryloyl chloride is 1:1.5:1.5; The volume ratio of dichloromethane and reaction system solution used during the extraction is 50:1; The amount is 10 times by mass of cystamine dihydrochloride, 5 times by mass of sodium hydroxide, and the amount of dichloromethane use...

Embodiment 3

[0065] Example 3: NMR characterization of N,N'-bis(acryloyl)cystamine (CBA)

[0066] The N,N'-bis(acryloyl)cystamine (CBA) obtained in Example 1 was dissolved in deuterated chloroform for H NMR characterization. Such as figure 1 As shown, the peaks at 2.92, 3.60, and 6.65 ppm of chemical shifts correspond to the proton peaks of methylene on cystamine dihydrochloride; the peaks at 5.62, 6.25 ppm of chemical shifts correspond to proton peak. figure 1 The results proved that N,N'-bis(acryloyl)cystamine (CBA) was successfully synthesized in this step.

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Abstract

The invention discloses a glutathione response-type dual-drug carrier as well as a preparation method and application thereof, and belongs to the field of biomedical engineering materials. The preparation method comprise the following steps: performing Michael addition reaction to obtain hyperbranched poly(amide amine)s; then connecting a hydrophobic drug onto an end group amino of a high polymer by amidation reaction, so as to form a prodrug micelle molecule; then loading another hydrophobic drug by subject-object assembly of the prodrug micelle molecule, thus effectively increasing drug loading capacity and promoting an synergistic effect of the drugs; preparing to obtain the glutathione response-type dual-drug carrier. The method is mile, the operation is convenient, byproducts are fewer, and a product is easy to separate and purify, thus facilitating the material biocompatibility. The glutathione response-type dual-drug carrier has the advantages of simple material components, easy-to-get raw materials and good biocompatibility, and is hopefully widely applied to the field of the biomedical engineering materials as a great amount of surface functional groups capable of being modified provide support for the application of the carrier in preparing the biomedical engineering materials.

Description

technical field [0001] The invention belongs to the field of biomedical engineering materials, in particular to a glutathione-responsive dual drug carrier and its preparation method and application. Background technique [0002] Polymer prodrugs refer to compounds formed by bonding polymers and drugs. Compared with general drug carriers, prodrugs can effectively improve the water solubility of hydrophobic drugs, prolong the half-life of drugs in the body, and improve How the drug is distributed in the body, protecting the drug from degradation. The concentration of glutathione with reduced mercapto groups in tumor tissues is much higher than that in normal tissues. In recent years, glutathione-responsive drug carriers have attracted extensive attention in drug carriers. [0003] Li et al. designed a disulfide-bonded polyethylene glycol / camptothecin (CPT) prodrug molecule, which could release 80% of CPT slowly under reducing conditions due to the breakage of the disulfide bo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/59A61K31/519A61K31/4745A61P35/00A61K31/12A61K9/107
CPCA61K9/1075A61K31/12A61K31/4745A61K31/519A61K2300/00
Inventor 马栋唐侨薛巍曾小龙
Owner 广州元合生物科技有限公司
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