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Chitosan/polylysine dendritic macromolecular core-shell nanoparticles and preparation method thereof

A technology of dendritic macromolecule and polylysine, which is applied in the direction of nanotechnology, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve the problems of low bioavailability and high cytotoxicity of drugs, and improve bioavailability The effect of high degree, simple preparation method and easy control

Inactive Publication Date: 2017-04-26
TIANJIN UNIV OF COMMERCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, peptide dendrimers have the following defects when used alone as drug carriers: the small size of low-generation dendrimers makes them easy to be quickly cleared during blood circulation, and the bioavailability of drugs is low; high-generation dendrimers Can overcome the size defect to a certain extent, but it will bring high cytotoxicity

Method used

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  • Chitosan/polylysine dendritic macromolecular core-shell nanoparticles and preparation method thereof
  • Chitosan/polylysine dendritic macromolecular core-shell nanoparticles and preparation method thereof
  • Chitosan/polylysine dendritic macromolecular core-shell nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] At 25°C, under nitrogen protection and stirring at 600 rpm, 5 g of methyl ester-protected lysine, 18.5 g of Boc-protected lysine, 16.4 g of EDC and 6.3 g of HOBt were dissolved in 20 ml of dichloromethane. While continuing to stir, slowly add 7ml of N-ethyldiisopropylamine. After that, the reaction was carried out for 48 hours at 25° C. under nitrogen protection and stirring at 600 rpm. After the reaction was finished, the solvent dichloromethane was removed by rotary evaporation. The residue was dissolved in about 400ml of chloroform, washed once with about 350ml of saturated NaCl solution, washed once with about 350ml of saturated NaHCO 3 Solution washed 3 times, 350ml 1mol / l dilute hydrochloric acid solution washed 1 time and 350ml saturated NaCl solution washed 1 time. The obtained oil phase was treated with anhydrous MgSO 4 Dry overnight, filter, and rotary evaporate, and then use silica gel column chromatography (eluent is a mixed solvent of dichloromethane / eth...

Embodiment 2

[0033] The preparation process of Boc-protected 2nd generation polylysine dendrimer (G2-Boc) is the same as that in Example 1.

[0034] Under nitrogen protection at 25°C and stirring at 600 rpm, 5 g of the obtained Boc-protected 2nd-generation polylysine dendrimer (G2-Boc) was dissolved in 10 ml of redistilled dichloromethane. After that, 18.8 ml of trifluoroacetic acid was slowly added in an ice-water bath at 2° C. while stirring was continued. After that, the reaction was stirred for 5 h at 25° C. under the protection of nitrogen. After the reaction, dichloromethane and trifluoroacetic acid were removed by rotary evaporation. The residue was precipitated with about 80ml of anhydrous ether and stirred overnight, and the anhydrous ether was removed by rotary evaporation to obtain a 2nd generation polylysine dendrimer (G2-NH 2 ).

[0035] 25 DEG C, under nitrogen protection, under the condition of 600 rpm stirring, the 2.55g de-Boc-protected 2nd generation polylysine dendrim...

Embodiment 3

[0039] The preparation process of Boc-protected third-generation polylysine dendrimer (G3-Boc) is the same as that in Example 2.

[0040] 5 g of the obtained Boc-protected third-generation polylysine dendrimer (G3-Boc) was dissolved in 10 ml of N,N-dimethylformamide at 25° C. under nitrogen protection and stirring at 600 rpm. Afterwards, in an ice-water bath at 2°C, 9 ml of trifluoroacetic acid was slowly added under continuous stirring. Then, at 25°C, under the protection of nitrogen, the reaction was stirred for 5 h. After the reaction, N,N-dimethylformamide and trifluoroacetic acid were removed by rotary evaporation. The residue was precipitated with about 50ml of anhydrous ether and stirred overnight, and the anhydrous ether was removed by rotary evaporation to obtain a third-generation polylysine dendrimer (G3-NH 2 ).

[0041] 25 DEG C, under nitrogen protection, under the condition of 600 rpm stirring, the 2.68g de-Boc-protected 3rd generation polylysine dendrimer (G3...

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Abstract

The invention discloses chitosan / polylysine dendritic macromolecular core-shell nanoparticles and a preparation method thereof. The chitosan / polylysine dendritic macromolecular core-shell nanoparticles are characterized in that the chitosan / polylysine dendritic macromolecular core-shell nanoparticles are of a chitosan derivative formed by carrying out an amidation reaction on an amino on chitosan with the weight average molecular weight of 5*10<4> to 2*10<5> and the deacetylation degree of 85 percent to 100 percent, and carboxyl on a polylysine dendritic macromolecule. The method disclosed by the invention comprises the following steps: preparing the chitosan into a chitosan water solution with the concentration of 0.5mg / ml to 5mg / ml and marking the chitosan water solution as a solution A; stirring at the speed of 500rpm to 1000rpm at 20 DEG C to 35 DEG C under the protection of nitrogen gas, and dropwise adding the solution A into a DMF (Dimethyl Formamide) solution of the polylysine dendritic macromolecule, EDC (Dichloroethane) and HOBt (Hydroxybenzotriazole); continually stirring and reacting for 2 days to 5 days; dialyzing for 2 days to 4 days, and freezing and drying to obtain a product. The praparation method is simple, has moderate reaction conditions and is easy to control.

Description

technical field [0001] The invention relates to the field of functional polymer materials, and more specifically relates to a chitosan / polylysine dendrimer core-shell nanoparticle and a preparation method thereof. Background technique [0002] Peptide dendrimers are a new class of highly branched macromolecules with amino acids as structural units. Peptide dendrimers have a protein-like spherical structure, good biocompatibility and water solubility, and can be biodegraded and the degradation products are non-toxic. In addition to having a unique open topology, easy modification to obtain controllable physicochemical properties, and nanometer size (maximum molecular size of 10–20 nm with low dispersion), the high surface functional group density of peptide dendrimers endows them with The function amplification effect makes it easy to bind multiple bioactive molecules such as chemotherapy drugs, drug-sensitizers, siRNA, etc. through electrostatic interaction or covalent bond...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08G83/00C08B37/08B82Y40/00A61K9/51A61K47/36A61K47/34A61K48/00
CPCA61K9/5161A61K47/34A61K48/0041B82Y40/00C08B37/003C08G81/00C08G83/003
Inventor 闻燕王禹晨牛阳阳雷虎军
Owner TIANJIN UNIV OF COMMERCE
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