Hydrophobized polysaccharide, and preparation method and application thereof

A technology for hydrophobizing and converting polysaccharides, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of harsh storage requirements, inconvenient transportation and storage, etc.

Inactive Publication Date: 2017-07-28
BENGBU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, many protein drugs used as drugs, such as vaccines, have been inactivated, but the storage requirements are harsh, which brings inconvenience to transportation and storage.

Method used

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  • Hydrophobized polysaccharide, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The preparation method of embodiment 1 polysaccharide

[0020] A method for preparing a polysaccharide, the preparation method specifically comprising: dissolving 20 g of dextran (molecular weight 2-500,000 Daltons) in 200 ml of dimethyl sulfoxide, adding 10 g of butyric anhydride and 2 ml of pyridine to react at room temperature for 4 hours, Add deionized water to stop the reaction. Add 2.54L of ethanol. After standing still for 3 hours, a precipitate was precipitated, which was re-purified with ethanol and dried under reduced pressure to obtain butylated polysaccharide.

Embodiment 2

[0021] Example 2 The method of preparing hydrophobized polysaccharide with polysaccharide as raw material

[0022] Dissolve 200 mg of the butylated polysaccharide prepared in Example 1 in dimethyl sulfoxide, add 50 mg of dicyclohexylcarbodiimide, and react at 10° C. for 1 hour. After the reaction is complete, add 20 ml of aqueous solution to the reaction solution, The DCU solids were removed by filtration, and 1000 ml of deionized water was used for dialysis to remove impurities to obtain a dialysate, and then 500 ml of ethanol was added to the dialysate, and the precipitated substance was the hydrophobized polysaccharide.

Embodiment 3

[0023] Example 3 Preparation of drug-loaded particles

[0024] This example provides a method for preparing drug-loaded particles using the hydrophobized polysaccharide prepared in Example 2 as a carrier, and the method is as follows:

[0025] Dissolve 40 mg of tetanus vaccine in 18 mL of NaOH aqueous solution at pH 9, add 80 mg of hydrophobized polysaccharide, and emulsify at room temperature for 10 minutes to obtain a mixed solution, which is to obtain vaccine-loaded nanoparticles. The hydrophobized polysaccharide drug-loaded nanoparticles are circular in alkaline aqueous solution and in a polydisperse state. Figure 1 is a photo taken under an inverted microscope of the hydrophobized polysaccharide-loaded tetanus vaccine nanoparticles.

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Abstract

The invention especially relates to a hydrophobized polysaccharide, and a preparation method and application thereof, belonging to the technical field of organic synthesis. The hydrophobized polysaccharide is prepared by reacting the hydroxyl group of glucan with succinic anhydride to prepare glucan butyrate with a butyric acid group at first and then reacting glucan butyrate with dicyclohexylcarbodiimide (DCC) so as to allow a carboxyl group to be modified by dicyclohexylurea (DCU); so the terminal group of the hydrophobized polysaccharide is modified by DCU, and butyric acid is used as a linking arm for connection with glucan via an ester bond. According to the preparation method, glucan or other polysaccharide is used as a raw material and reacts butyric anhydride and DCC to prepare the hydrophobized polysaccharide. The prepared hydrophobized polysaccharide has a molecular weight in a range of 20 to 500 K, has self-emulsifying performance and is applicable as a proteinic drug, especially as a carrier for amino acid and vaccine drugs.

Description

technical field [0001] The invention relates to the technical field of organic synthesis, in particular to a hydrophobized polysaccharide and its preparation method and application. Background technique [0002] Proteins in biological cells maintain their biological activity under glycoproteins, water, and a certain temperature. When they leave the environment of the human body, they are easily inactivated and condensed and deteriorated. However, many protein drugs used as drugs, such as vaccines, have been inactivated, but the storage requirements are harsh, which brings inconvenience to transportation and storage. The present invention replaces traditional vaccine protective agents with hydrophobized polysaccharides, encapsulates protein drugs in the center of the polysaccharide shell, and bridges the protein and hydrophobized polysaccharides under the action of hydrogen bonds and hydrophobicity. When the pH condition changes, this The bridge joint disintegrates, and the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/02A61K9/51A61K47/36A61K31/4745A61K39/08A61P31/04
CPCA61K9/5161A61K31/4745A61K39/08A61K47/36A61K2039/6087C08B37/0006
Inventor 梁颖段贵新刘浩
Owner BENGBU MEDICAL COLLEGE
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