M cell targeting and pH responding starch based carrier material and preparation method and applications thereof

A technology of cell targeting and carrier materials, which is applied in the direction of medical preparations, pharmaceutical formulas, and capsule delivery of non-active ingredients. Strong resistance, the effect of improving the transfer efficiency

Active Publication Date: 2019-09-20
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, most of the carrier materials are artificially synthesized polymer materials, which have potential hazards. Natural polymer carrier materials are mainly concentrated in chitosan, but due to the solubility of the material itself, it is not conducive to the immune active substances. Controlled release in the gastrointestinal tract

Method used

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  • M cell targeting and pH responding starch based carrier material and preparation method and applications thereof
  • M cell targeting and pH responding starch based carrier material and preparation method and applications thereof
  • M cell targeting and pH responding starch based carrier material and preparation method and applications thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] (1) According to monochloroacetic acid: native starch (molecular weight is 2.0×10 6 g / mol)=0.4 molar ratio to carry out etherification reaction, reaction temperature 50 ℃, reaction time 4h, the obtained carboxymethyl starch (CMS1) that carboxymethyl substitution degree is 0.27;

[0058] (2) According to molar ratio, carboxymethyl group: catalyst: GRGDS short peptide=1:1:1 ratio carries out acylation reaction, and reaction temperature is 35 ℃, and the reaction time is 24h, and wherein catalyzer is EDC and NHS (mole The ratio is 1:1), the concentration of carboxymethyl starch in the reaction system is 1% (w / v, g / mL), and the solvent is phosphate buffer (0.1M, pH=7.5). After the reaction was completed, it was dialyzed and freeze-dried to obtain a molecular weight of 2.11×10 6 g / mol, a starch-based carrier material (RGD-CMS1) with a carboxymethyl substitution degree of 0.27 and a targeting peptide GRGDS grafting amount of 1.12% (calculated based on N element content).

[...

Embodiment 2

[0065] (1) According to monochloroacetic acid: native starch (molecular weight is 1.0×10 6 g / mol)=0.1 molar ratio to carry out etherification reaction, reaction temperature 40 ℃, reaction time 2h, the carboxymethyl starch that makes carboxymethyl substitution degree is 0.04;

[0066] (2) The carboxymethyl starch with a carboxymethyl substitution degree of 0.04 prepared in step (1) was first enzymolyzed by pullulanase (unit enzyme activity 15U / g (carboxymethyl starch dry basis)) at 50°C for 24h Finally, use high temperature-resistant α-amylase (unit enzyme activity 100U / g (carboxymethyl starch dry basis)) to enzymolyze at 80°C for 30min to obtain a molecular weight of 6.99×10 4 Carboxymethyl starch (CMS2) of g / mol;

[0067] (3) carry out acylation reaction according to the molar ratio carboxymethyl group: catalyst: GRGDS short peptide=4:1:1 ratio, reaction temperature is 25 ℃, and the reaction time is 12h, and wherein catalyzer is EDC and NHS (molar ratio 1:1), the concentrat...

Embodiment 3

[0074] (1) According to monochloroacetic acid: native starch (molecular weight is 1.0×10 7 g / mol)=0.3 molar ratio to carry out etherification reaction, reaction temperature 45 ℃, reaction time 3h, the carboxymethyl starch that makes carboxymethyl substitution degree is 0.24;

[0075] (2) The carboxymethyl starch obtained in step (1) with a carboxymethyl substitution degree of 0.24 is enzymatically hydrolyzed at 50°C for 16 hours by pullulanase (unit enzyme activity 15U / g (carboxymethyl starch dry basis)) Finally, use high temperature resistant α-amylase (unit enzyme activity 15U / g (carboxymethyl starch dry basis)) to enzymolyze at 80°C for 10min to obtain a molecular weight of 4.56×10 5 Carboxymethyl starch (CMS3) of g / mol;

[0076] (3) The acylation reaction was carried out according to the molar ratio of carboxymethyl group:catalyst:GRGDS short peptide=2:1:1, the reaction temperature was 30°C, and the reaction time was 18h. Wherein the catalyst is EDC and NHS (the molar ra...

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Abstract

The invention discloses an M cell targeting and pH responding starch based carrier material and a preparation method and applications thereof. The molecular structure of the starch based carrier material is represented in the description. The molecular weight of the starch based carrier material is 7.04*10<4> to 2.11*10<6> g / mol. The substitution degree of carboxymethyl groups is 0.04 to 0.28. The grafting amount of targeted peptide (GRGDS) is 0.01 to 1.12% (calculated by N element). Under a stomach pH value of 1.2, the carrier material is protonized and is undissolved in water, and under a small intestine pH of 6.8, the carrier material is de-protonized and can be dissolved by water slowly. The carrier material has good gastrointestinal tract pH responsiveness. Through electrostatic interaction, an active substance with positive charges can be efficiently embedded. The active substance is protected and will not be deactivated in gastrointestinal tracts. At the same time, the active substance can be targeted to M cells, the transfer efficiency of the active substance carried by M cells is improved, and the bioavailability of the active substance is enhanced therefore.

Description

technical field [0001] The invention relates to a starch-based carrier material, in particular to an M cell-targeting and pH-responsive starch-based carrier material and a preparation method and application thereof. Background technique [0002] The mucosal immune system is the largest component of the entire immune system and is the first line of defense for human immunity, including about three-quarters of immune cells, among which M cells are the main entrance for mucosal uptake and capture of antigens. M cells are mainly distributed in the lymph node epithelium (FAE) of Peyer's pathway, and they are closely arranged with intestinal epithelial cells. The intestinal epithelium forms irregular microvilli, which helps it to take up antigenic substances from the intestinal lumen of the upper gastrointestinal tract. There are abundant pinocytic vesicles and mitochondria in the cytoplasm of M cells, but less lysozyme. There are membranous folds on the top of M cells, and a dee...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B31/12A61K47/36
CPCC08B31/125A61K47/36A61K47/62A61K47/6925A61K47/61
Inventor 李晓玺张义平陈玲李琳
Owner SOUTH CHINA UNIV OF TECH
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