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Use of chitosan oligosaccharide and its chitosan oligosaccharide iron complex as anti HIV-1 polypeptide drug carrier

An iron complex, HIV-1 technology, applied in the intersection of biomaterials and pharmacology, can solve the problems of polypeptide medicinal chemistry and conformation instability, affecting absorption, difficult to penetrate semipermeable membrane, etc., to increase bioavailability. Effect

Inactive Publication Date: 2009-09-30
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of administering polypeptide and protein drugs in the gastrointestinal tract, there are generally the following difficulties that have not been overcome: catalytic degradation by gastric acid, enzymatic hydrolysis in the gastrointestinal tract, and poor permeability of the gastrointestinal mucosa; and peptide drugs have a large relative molecular weight and poor fat solubility , it is difficult to pass through the semi-permeable membrane, which affects the absorption; peptide drugs also have chemical and conformational instability, etc.

Method used

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  • Use of chitosan oligosaccharide and its chitosan oligosaccharide iron complex as anti HIV-1 polypeptide drug carrier
  • Use of chitosan oligosaccharide and its chitosan oligosaccharide iron complex as anti HIV-1 polypeptide drug carrier
  • Use of chitosan oligosaccharide and its chitosan oligosaccharide iron complex as anti HIV-1 polypeptide drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Purification of Chitooligosaccharides and Preparation of Nanoparticles:

[0033] Purification: Since chitosan oligosaccharide contains some impurities such as ash, it should be purified before the experiment. Dissolve chitosan oligosaccharides with a deacetylation degree of 85% and a molecular weight of 5000 in 1% acetic acid and filter to remove insoluble impurities, rinse the filtrate with a large amount of ultrapure water to neutrality, then filter with a 0.22 μm nylon membrane, and freeze-dry to obtain Purified chitosan.

[0034] Preparation of nanoparticles: Water-soluble chitosan oligosaccharides can undergo molecular self-assembly in aqueous solution to form nanoparticles due to the amino groups in the molecule. Use 2% sodium phosphotungstate as the negative staining solution, take a small amount of chitosan oligosaccharide nanoparticle solution and drop it on the copper grid covered with carbon film, let it stand for 10min, dry the suspension with filter paper,...

Embodiment 2

[0036] Get the chitosan oligosaccharide and polypeptide C22 prepared in Example 1, keep stirring at a pH of about 6.0 and carry out blending and compounding at room temperature, and use an ultrafiltration membrane to filter and separate to obtain chitosan / polypeptide C22 composite nanoparticles, and Freeze dried.

Embodiment 3

[0038] Accurately take 1.25g according to the deacetylation degree after the purification of the method in Example 1 and be 70% molecular weight and be dissolved in 25ml ultrapure water, add the there-necked flask, adjust pH=3.0 with 1% HAC, Slowly add an equal volume of 0.01M FeCl under constant stirring at 500rpm 3 Solution, after reacting at room temperature for 12 hours, wash with ultrapure water on an ultrafiltration membrane with a molecular weight of 2000 until the solution is neutral, and remove unreacted FeCl 3 , freeze-dry to obtain light yellow chitosan oligosaccharide-iron complex powder, freeze-dry.

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Abstract

The invention provides the application of chitosan oligosaccharide and its derivatives as anti-HIV-1 polypeptide drug carrier. Chitosan and its derivatives as anti-HIV-1 peptide drug carriers can increase the bioavailability of peptide drugs with low absorption rate; control the release of peptide drugs; reduce the stimulation of peptide drugs to gastrointestinal mucosa; keep peptide drugs in vivo stability; improve the targeting of peptide drugs.

Description

technical field [0001] The invention belongs to the cross field of biomaterials and pharmacy, and relates to the application of chitosan oligosaccharide and its derivatives, especially the application of chitosan oligosaccharide and its derivatives as anti-IIIV-1 polypeptide drug carrier. Background technique [0002] AIDS is acquired immunodeficiency syndrome (acquured immunodeficiency syndrome, AIDS), which is caused by human immunodeficiency virus (human immunodeficiency virus, HIV or AIDS virus) infection, resulting in partial or complete loss of the immune function of the infected person. The number of CD4 cells decreases, followed by opportunistic infections, tumors, etc., and the clinical manifestations are various. The disease spreads rapidly, has a high mortality rate, and currently has no cure. [0003] Aiming at the mechanism of HIV-1 invasion, infection and other mechanisms that may inhibit IIIV-1, various types of inhibitory drugs have been researched and desig...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K38/16A61P31/18
Inventor 汪世龙孙晓宇张蕤黄进姚思德
Owner TONGJI UNIV