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Nano-carrier capable of realizing co-delivery of genes and medicines and preparation method of nano-carrier

A nanocarrier and co-delivery technology, applied in drug delivery, gene therapy, drug combination, etc., can solve the problems of troublesome operation, low drug loading, and inability to release the prototype drug well, and achieve accelerated release and high therapeutic effect. Effect

Active Publication Date: 2016-04-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In recent years, some literatures have reported the research on the co-delivery of drugs and genes. These drugs are basically grafted onto polymers or encapsulated in polymers. This method has low drug loading and is cumbersome to operate.
There are also some literatures that synthesize drugs into polymers for post-loading drugs, but they cannot release the original drug well. Therefore, norcantharidins synthesize cationic polymers in the form of ester bonds and transfer genes to achieve co-delivery of drugs and genes.

Method used

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  • Nano-carrier capable of realizing co-delivery of genes and medicines and preparation method of nano-carrier
  • Nano-carrier capable of realizing co-delivery of genes and medicines and preparation method of nano-carrier
  • Nano-carrier capable of realizing co-delivery of genes and medicines and preparation method of nano-carrier

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Experimental program
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Effect test

Embodiment 1

[0037] Synthesis of norcantharidin diacrylate: norcantharidin, 4-dimethylaminopyridine, hydroxyethyl acrylate and dicyclohexylcarbodiimide feed in a certain molar ratio (1.0:0.02:2.0:2.1), Dissolved in dichloromethane, reacted for 36h, passed through a silica gel column to obtain norcantharidin diacrylate; polymer PEI-alt-DAN synthesis: take an appropriate amount of norcantharidin diacrylate, dissolve it with ethanol, add PEI423, to a certain Ratio molar ratio (1.0:1.0) feeding, stirring reaction at 60°C for 5 days under nitrogen protection, dialysis (MWCO=3500), and freeze-drying the solution to obtain the final polymer product;

Embodiment 2

[0039] Synthesis of cantharidin diacrylate: cantharidin, 4-dimethylaminopyridine, hydroxyethyl acrylate and dicyclohexylcarbodiimide are fed in a certain molar ratio (1.0:0.02:2.0:2.1), dissolved in dichloro In methane, react for 36 hours, pass through a silica gel column to obtain norcantharidin diacrylate; polymer synthesis: take an appropriate amount of cantharidin diacrylate, dissolve in ethanol, add PEI300, feed with a certain molar ratio (1.0:1.0), and protect with nitrogen The reaction was stirred at 60°C for 5 days, dialyzed (MWCO=3500), and the solution was freeze-dried to obtain the final polymer product;

Embodiment 3

[0041] Synthesis of PEI-alt-PEG polymer: take an appropriate amount of polyethylene glycol acrylate, dissolve in ethanol, add PEI423, feed in a certain molar ratio (1.0:1.0), stir and react at 60°C for 5 days under nitrogen protection, and dialyze (MWCO=3500 ), the solution was freeze-dried to obtain a control polymer material.

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Abstract

The invention discloses a nano-carrier capable of realizing co-delivery of genes and medicines and a preparation method of the nano-carrier, and in particular relates to a nano-carrier capable of realizing co-loading and co-delivery of genes and medicines. The medicine delivery system is formed through self-assembly of a cation prodrug polymer and the genes through the electrostatic interaction between the cation prodrug polymer and the genes, wherein the cation prodrug polymer can release active medicines through the hydrolysis by esterases in the cells, after entering into the cells under the phagocytosis, the nano-composition escapes from an endosome under the effect of the buffer capacity of polyamines on a polymer, and releases the medicines ad the genes in the cytoplasm, so that the medicines and the genes can inhibit the tumor proliferation together.

Description

technical field [0001] The present invention relates to a nanocarrier for co-delivery of drugs and genes, in particular to a targeted drug delivery system simultaneously loaded with gene drugs and therapeutic drugs. The co-delivery system of the present invention can simultaneously release drugs through hydrolysis in tumor cells The gene is produced, and the two synergistically inhibit the proliferation of tumor cells and the migration of tumor cells together, which belongs to the technical field of nano-pharmaceutical preparations. Background technique [0002] Tumor has become one of the diseases that seriously threaten people's lives. At present, the preferred treatment for tumors is surgical treatment, but not all patients are suitable for surgery. Only patients with good tissue physiological functions, concentrated tumors, and no metastasis are suitable for surgery. The vast majority of patients are inoperable for various reasons. Therefore, chemotherapy is still one...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K48/00A61K47/34A61K9/19A61K31/365A61P35/00C08G73/02
CPCA61K9/0019A61K9/0073A61K9/19A61K31/365A61K47/34A61K48/0041A61K48/0075C08G73/0273
Inventor 姜虎林邢磊
Owner CHINA PHARM UNIV
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