Preparation method and application of mannose grafted trimethyl chitosan

A technology of trimethyl chitosan and mannose, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulas, block delivery, etc., can solve the problems of low absorption rate and poor immunogenicity, and achieve simple processing and improved Drug activity, effect of improving reaction efficiency

Active Publication Date: 2018-07-20
ZHEJIANG PHARMA COLLEGE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In order to solve the above-mentioned problems of poor immunogenicity, degradation and low absorption rate of vaccines with recombinant DNA technology and chemically synthesized antigens and polypeptides under the action of low pH and enzymes, the present invention provides a mannose-grafted trimethyl shell The preparation method and application of the polysaccharide carrier have the advantages of mild preparation conditions, the preparation of mannose-grafted trimethyl chitosan drug-loaded microspheres has high targeting ability to dendritic cells, and can overcome the mucosal barrier

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  • Preparation method and application of mannose grafted trimethyl chitosan
  • Preparation method and application of mannose grafted trimethyl chitosan
  • Preparation method and application of mannose grafted trimethyl chitosan

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Embodiment 1

[0041] see figure 1 , a flow chart of the preparation method of the mannose-grafted trimethyl chitosan carrier provided by the invention. The preparation method of described mannose grafting trimethyl chitosan carrier, comprises the following steps:

[0042] Step S1, adding N,N,N-trimethyl chitosan into the organic solvent, stirring and making it into a swollen state;

[0043] Specifically, see figure 2 , is the synthetic route map of N,N,N-trimethyl chitosan. Put 2g of chitosan (chitosan, CS) with a molecular weight of 20kDa-1000kDa and 80mL of N-methyl-2-pyrrolidone (N-methyl-2-pyrrolidone, NMP) into a round bottom flask, or use dimethylformamide and N -Any one or more combinations of organic solvents such as methylpyrrolidone, stirred overnight at room temperature to swell chitosan, added 4.8g of sodium iodide and 11mL of 15% NaOH solution, stirred at 60°C for 20 minutes, added 12mL of iodine methane, continue to react for 2 hours; add 11mL of 15% NaOH solution and 6mL o...

Embodiment 2

[0061] Weigh 10 mg Manno-TMCS and 5 mg ovalbumin (Ovalbumin, OVA), dissolve in 5 mL deionized water, and prepare a Manno-TMCS-OVA solution. Weigh 2 mg of sodium alginate (Sodium alginate, SL), dissolve it in 10 mL of deionized water, and prepare a 0.2 mg / mL SL solution. Under magnetic stirring, add 2 mL of SL solution dropwise to Manno-TMCS-OVA solution at a rate of 6 mL / h, continue stirring for 30 min after the addition is complete, refrigerate and centrifuge to collect the precipitate, wash, and dry to obtain mannose-grafted trimethyl Chitosan-loaded ovalbumin microspheres.

Embodiment 3

[0063] Weigh 10 mg Manno-TMCS and 5 mg ovalbumin (OVA), dissolve in 5 mL deionized water, and prepare Manno-TMCS-OVA solution. Weigh 4 mg of sodium alginate, dissolve it in 10 mL of deionized water, and prepare a 0.4 mg / mL SL solution. Under magnetic stirring, add 2 mL of SL solution dropwise to Manno-TMCS-OVA solution at a rate of 6 mL / h, continue stirring for 30 min after the addition is complete, refrigerate and centrifuge to collect the precipitate, wash, and dry to obtain mannose-grafted trimethyl Chitosan-loaded ovalbumin microspheres.

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Abstract

The invention relates to a preparation method and application of mannose-grafted trimethyl chitosan.The preparation method comprises: adding N,N,N-trimethyl chitosan into an organic solvent so that the organic solvent wells, adding mannopyran phenyl isothiocyanate for full reacting, and preparing N-mannose-N,N,N-trimethyl chitosan by ethanol washing, suction filtering and vacuum drying.The invention also provides application of the preparation method of the mannose-grafted trimethyl chitosan in the preparation of drug-carrying microspheres.The preparation method of a mannose-grafted trimethyl chitosan carrier has mild conditions, and a prepared mannose-grafted trimethyl chitosan drug-carrying microsphere preparation can target dendritic cells, overcoming mucosal barriers.

Description

technical field [0001] The invention relates to the technical field of drug-loaded microspheres, in particular to a preparation method and application of mannose-grafted trimethyl chitosan. Background technique [0002] Vaccines are autoimmune preparations made from pathogenic microorganisms (such as bacteria, rickettsia, viruses, etc.) and their metabolites, which are artificially attenuated, inactivated, or genetically modified, and used to prevent infectious diseases. The vaccines currently used in the market are mainly live attenuated vaccines, which have problems such as virulence reversal, adverse reactions, and the need for refrigerator storage and transportation. However, this new generation of vaccines, which use recombinant DNA technology and chemically synthesized antigens and peptides, limits and avoids the common side effects of traditional vaccines, but their immunogenicity is poor, and they will degrade under the action of low pH and enzymes. The absorption r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/08A61K9/16A61K47/36
CPCA61K9/1652C08B37/003
Inventor 徐蓓华胡英
Owner ZHEJIANG PHARMA COLLEGE
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