Reducible and degradable nano medicine-carrying micelle and preparation method thereof

A nano-drug-loading and micelle technology, applied in the field of biomedical technology and nano-medicine, can solve problems such as the concentration difference of glutathione, improve clinical efficacy and bioavailability, efficient delivery and localized release, and efficient method. Effect

Inactive Publication Date: 2011-06-08
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Interestingly, there are significant differences in the concentration of glutathione in different tissues of the human body as well as intracellular and extracellular

Method used

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  • Reducible and degradable nano medicine-carrying micelle and preparation method thereof
  • Reducible and degradable nano medicine-carrying micelle and preparation method thereof
  • Reducible and degradable nano medicine-carrying micelle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] A method for preparing reductively degradable nano drug-loaded micelles, comprising the steps of:

[0032] The first step: use the Michael addition of N,N'-bis(acryloyl)cystamine and ethanolamine to obtain polycystamine with a disulfide bond with a hydroxyl group, and then use the hydroxyl group to perform a ring-opening reaction on caprolactone to obtain CA -PCL polymer; can be divided into three steps for above reaction:

[0033](1): Substitution reaction of cystamine dihydrochloride and acryloyl chloride to obtain N, N'-bis(acryloyl) cystamine (CBA): 10mmol cystamine dihydrochloride (cysteamine hydrochloride) dissolved in In a mixed solution containing 10mL chloroform and 15mL, 3.5M NaOH, heat to 50°C, add 5mL chloroform containing 20mmol acryloyl chloride dropwise, react for 15min, and keep the temperature of the reaction solution at 50°C; then filter and extract while hot, and take Cool the organic phase to room temperature to obtain a white crystalline solid, fil...

Embodiment 2

[0041] With the experimental method of embodiment 1, fix the amount of polycystamine containing disulfide bond with hydroxyl and the amount of catalyst stannous octoate, change the add-on of caprolactone monomer, make the polycystamine containing disulfide bond with hydroxyl The molar ratios of cystamine and caprolactone monomers were 1:15, 1:30, and 1:60, respectively. The remaining steps are the same as in Example 1.

Embodiment 3

[0043] With the experimental method of embodiment 1, fix the amount of the polycystamine containing the disulfide bond of band hydroxyl and the add-on of caprolactone monomer, change the add-on of catalyzer stannous octoate, catalyzer stannous octoate and caprolactone monomer The molar ratio of the body is 1:1000, 1:5000, 1:10000. The remaining steps are the same as in Example 1.

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Abstract

The invention relates to a reducible and degradable nano medicine-carrying micelle and a preparation method thereof, belonging to the fields of biomedical technology and nano medical technology. The reducible and degradable nano medicine-carrying micelle is characterized by having the following structural general formula: MPEG-CA-PCL, wherein the CA is poly-cystamine containing disulfide bonds, the MPEG is methoxy polyethylene glycol the molecular weight of which is 475-5000DA, and the PCL is polycaprolactone. The preparation method of the reducible and degradable nano medicine-carrying micelle comprises the following steps: (1) carrying out Michael addition to N,N'-bis (acrylic) cystamine and ethanolamine to obtain hydroxy poly-cystamine containing disulfide bonds, and then, carrying out ring opening reaction on caprolactone by utilizing a hydroxy group to obtain a CA-PCL polymer; and (2) mixing the CA-PCL polymer obtained in the step (1) and carboxyl-terminated MPEG, and adding paclitaxel (PTX) to prepare the nano medicine-carrying micelle through a dialysis method. The method is efficient and simple.

Description

technical field [0001] The invention relates to a reductively degradable nano drug-loaded micelle and a preparation method thereof, belonging to the technical fields of biomedicine technology and nanomedicine. Background technique [0002] The research on polymer drug-loaded micelles in drug delivery and gene delivery is developing rapidly. When polymer micelles are used as drug carriers, drugs can be loaded into polymer micelles by simple physical embedding, electrostatic interaction or covalent bonding methods. Polymer micelle has a perfect core-shell structure, its nano-scale particle size and the hydrophilic effect of the micelle shell make it difficult to be phagocytized by the reticuloendothelial system and prevent the adsorption of proteins and cells. The particle size of polymer micelles is very similar to natural structures such as viruses and lipoproteins, and the shell has hydrophilic segments such as PEG to avoid phagocytosis by phagocytic cells. Therefore, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K47/48C08G73/00C08G63/688C08G63/08C08G65/48A61P35/00A61K47/59A61K47/60A61K47/69
Inventor 黄进余家会张晓兰李俊丽任红轩黄行九
Owner WUHAN UNIV OF TECH
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