Polyethylene glycol chitosan self-assembled nanoparticles and preparation method thereof

A technology of self-assembled nanoparticles and polyethylene glycol, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of harsh preparation conditions and affecting the release of macromolecular substances, and achieve good biocompatibility, The effect of uniform size and stable water dispersion system

Inactive Publication Date: 2014-01-22
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The covalent cross-linking method will affect the release of macromolecular substances; the precipitation method is a heterogeneous reaction, and the preparation conditions are harsh

Method used

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  • Polyethylene glycol chitosan self-assembled nanoparticles and preparation method thereof
  • Polyethylene glycol chitosan self-assembled nanoparticles and preparation method thereof
  • Polyethylene glycol chitosan self-assembled nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] One, embodiment 1: prepare the polyethylene glycol chitosan self-assembled nanoparticle of PEG:CS=5:1:

[0028] 1. Synthesis of mPEG-COOH:

[0029] Weigh 5g of mPEG into a round-bottomed flask, dissolve with 25ml of dry pyridine, add 0.3g of succinic anhydride, react at 60°C for 2 hours, and remove most of the pyridine with a rotary evaporator at 45°C under reduced pressure. The obtained solid was dissolved in 30ml of toluene, stirred continuously on a magnetic heating stirrer, and 40ml of n-hexane precipitant was slowly added until the product was precipitated. The crude product was dialyzed with a dialysis bag for four days, and then the dialyzed material was freeze-dried to obtain the product, and mPEG-COOH with a molecular weight of 2000 could be obtained.

[0030] 2. Preparation of PEGylated Chitosan PEG-CS (PEG:CS=5:1):

[0031] Weigh 1 g of CS (500KDa) and dissolve it in 6 ml of acetic acid (2%, w / v), dilute it with 20 ml of TEMED·HCL with a pH of 4.7, add it t...

Embodiment 2

[0043] Two, embodiment 2: prepare the polyethylene glycol chitosan self-assembled nanoparticle of mPEG:CS=1:10:

[0044] 1. Synthesis of mPEG-COOH:

[0045] Weigh 5g of mPEG into a round-bottomed flask, dissolve with 25ml of dry pyridine, add 0.3g of succinic anhydride, react at 60°C for 2 hours, and remove most of the pyridine with a rotary evaporator at 45°C under reduced pressure. The obtained solid was dissolved in 30ml of toluene, stirred continuously on a magnetic heating stirrer, and 40ml of n-hexane precipitant was slowly added until the product was precipitated. The crude product was dialyzed with a dialysis bag for four days, and then the dialyzed material was freeze-dried to obtain the product, and mPEG-COOH with a molecular weight of 2000 could be obtained.

[0046] 2. Preparation of PEGylated chitosan PEG-CS (PEG:CS=1:10):

[0047] Weigh 1g CS (500KDa) and dissolve it in 6 ml acetic acid (2%, w / v), dilute it with 20 ml TEMED·HCL (pH 4.7), add it into a three-neck ...

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Abstract

The invention discloses polyethylene glycol-chitosan self-assembled nanoparticles and a preparation method thereof, belonging to the technical field of preparation of a functional material. Chitosan derivative with water solubility and biocompatibility is obtained by modifying chitosan by polyethylene glycol, so as to prepare the polyethylene glycol-chitosan self-assembled nanoparticles. The polyethylene glycol-chitosan self-assembled nanoparticles have the advantages that TEMED (tetramethylethylenediamine).HCL is taken as a diluent; EDC (dichloroethane) and NHS are taken as activating agents under a mild condition; the polyethylene glycol chitosan derivative with water solubility and biocompatibility is prepared by grafting mPEG-COOH on CS in a covalent coupling manner and modifying the chitosan by PEG (polyethylene glycol), so that the nanoparticles can be formed in a water solution in a self-assembling manner.

Description

technical field [0001] The invention belongs to the technical field of functional material preparation. Background technique [0002] Chitosan is the only alkaline polysaccharide in nature. It is the product of N-deacetylation of chitin, and it exists in large quantities in shells, shrimp shells, crab shells, arthropods, annelids, and mollusks. Chitosan has the advantages of non-toxic, biocompatible, biodegradable and antibacterial, and is widely used in biology, medicine and other fields. However, due to the existence of strong intramolecular and intermolecular hydrogen bonds, chitosan is insoluble in water and physiological environments, which greatly limits its application. Therefore, the development of chitosan derivatives with specific properties has attracted much attention. [0003] In the fields of biology and medicine, the preparation methods of chitosan nanoparticles that can be used as macromolecular drugs and bioactive macromolecular carriers mainly include: cov...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08G65/00C08B37/08C08J3/12A61K47/36
Inventor 宋晓丽王娟尤娟朱爱萍郭荣
Owner YANGZHOU UNIV
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