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Method for preparing amphiphilic chitosan nanometer medicament carrier

A nano- and amphiphilic technology of chitosan, applied in pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve problems such as unfavorable controlled release, poor stability of polymer micelles, and influence on the properties of chitosan, and achieve The effect of good particle size distribution, controllable yield and easy operation

Active Publication Date: 2010-05-26
ZHANGJIAGANG IND TECH RES INST CO LTD DALIAN INST OF CHEM PHYSICS CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Above two kinds of methods, the former operation is simpler, but only limited in the patent (Chinese patent: CN1883708): the fatty acid of grafting C8-C22 on the chitosan chain that molecular weight is 1.5-51KDa, low molecular weight chitosan degrades relatively Fast, not conducive to the controlled release of experimental drugs for a long time
In addition, the fatty acid used in this patent is a flexible linear chain, and the stability of the polymer micelles is poor after dilution. Therefore, in order to improve its stability, it is necessary to chemically modify the surface of the nanomicelles with bifunctional small molecules. Intermolecular chemical bond bridging on the surface of polymer micelles to improve the stability of polymer micelles
Moreover, existing studies have shown that as the grafting rate of lipophilic small molecules increases, the formed nanomicelles are more stable, and the increase in the grafting rate will also affect the properties of chitosan itself.

Method used

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  • Method for preparing amphiphilic chitosan nanometer medicament carrier
  • Method for preparing amphiphilic chitosan nanometer medicament carrier
  • Method for preparing amphiphilic chitosan nanometer medicament carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0030] 1) At room temperature, 1g chitosan M v64KDa was dissolved in 100 mL of aqueous hydrochloric acid with a molar concentration of 0.05, and then the pH of the solution was adjusted to 4 with 1N NaOH to form a transparent 1% (w / v) chitosan solution.

[0031] 2) Get a certain amount of lithocholic acid, make the ratio of the amount of substance of lithocholic acid to the amount of substance of glucosamine residue in chitosan be 0.14: 1, add it in the DMSO solution of 100mL, add to lithocholic acid subsequently EDC and NHS are added into the solution in equal quantities, and the ratio of EDC to lithocholic acid is kept constant at 1.2:1. Lithocholic acid, EDC and NHS were reacted at room temperature at 500rpm for 90min.

[0032] 3) A mixed solution of lithocholic acid, EDC and NHS reacted in 100 mL of DMSO for 90 min was slowly added dropwise to a 1% (w / v) chitosan solution within 30 min, and reacted for 24 h at a stirring speed of 1000 rpm.

[0033] 4) Add the above 200mL...

Embodiment 2

[0037] Except that the molar ratio of lithocholic acid and glucosamine residues in chitosan is 0.24:1, other conditions are the same as in Example 1.

[0038] The FTIR characterization spectrum of the synthesized product under this condition is shown in figure 1 -c.

[0039] The particle size intensity distribution diagram of the nanoparticles prepared under this condition is shown in Figure 4 (Z-average=249.2±27.4 nm).

[0040] The TME morphology characterization diagram of the nanoparticles prepared under this condition is shown in Figure 5 .

Embodiment 3

[0042] Except that the molar ratio of lithocholic acid and glucosamine residue in chitosan is 0.34: 1, other conditions are the same as specific example 1.

[0043] The FTIR characterization spectrum of the synthesized product under this condition is shown in figure 1 -d.

[0044] When the synthetic product under this condition is characterized by pyrene molecular fluorescent probe to characterize the critical micelle concentration, the obtained pyrene emission spectrum is shown in figure 2 .

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Abstract

The invention relates to an amphiphilic chitosan material prepared by grafting lipophilic micro-molecular lithocholic acid on chitosan molecules and having good biocompatibility and degradability. Under catalysis of catalysts EDC and NHS, Mv64-230KDa amphiphilic macromolecular chitosan and lipophilic micro-molecular lithocholic acid are subjected to amidation reaction to form the amphiphilic chitosan material with good biocompatibility and degradability; in acidic solution with pH of less than 6.5, the amphiphilic chitosan material can rapidly form uniformly-distributed nanometer micelle with granularity of between 200 and 400 nm based on a molecule self-assembling principle under the ultrasonic condition; and an internal amphiphilic structure of the amphiphilic chitosan material is favorable for improving solubility of fat-soluble medicaments and further the bioavailability of the medicament in human body is expected to be improved..

Description

technical field [0001] The invention relates to a fat-soluble drug nano-carrier material, specifically a method for preparing nanoparticles with hydrophilic surfaces and lipophilic interiors through molecular self-assembly under ultrasonic conditions. Background technique [0002] Amphiphilic polymers composed of hydrophilic and lipophilic segments form nanomicelles in aqueous solution through the principle of molecular self-assembly. Because the surface of the micelles is hydrophilic and the interior is lipophilic, this type of micelles has many advantages in the field of fat-soluble drug delivery and controlled release, such as improving the solubility of fat-soluble drugs in solution and avoiding easy degradation of drugs in the future. Degradation occurs in the process of reaching the target, improving the bioavailability of the drug, prolonging the circulation time of the drug in the body, improving the distribution of the drug in the body, and at the same time chemical...

Claims

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Application Information

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IPC IPC(8): A61K47/36C08B37/08
Inventor 马小军周火飞刘袖洞
Owner ZHANGJIAGANG IND TECH RES INST CO LTD DALIAN INST OF CHEM PHYSICS CHINESE ACADEMY OF SCI
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