Chitosan-based amphiphilic self-assembling nano carrier and preparation method and application thereof

A nano-carrier and chitosan technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of chitosan's unideal solubility and achieve good biological Safety, good dispersibility, and uniform particle size

Active Publication Date: 2019-08-16
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent decades, chitosan has been widely used in the field of biopharmaceuticals due to its superior biocompatibility, degradability, bacteriostasis, mucoadhesion, non-toxic and environmental protection, but chitosan is not ideal Solubility greatly limits its application

Method used

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  • Chitosan-based amphiphilic self-assembling nano carrier and preparation method and application thereof
  • Chitosan-based amphiphilic self-assembling nano carrier and preparation method and application thereof
  • Chitosan-based amphiphilic self-assembling nano carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Accurately weigh 0.24g of low-molecular-weight chitosan and dissolve it in 30mL of 1% hydrochloric acid solution, stir rapidly with a glass rod for 10min at room temperature, and then dissolve it completely by magnetic stirring, and set aside. Accurately weigh 0.79g VES and place it in a three-necked flask, use a graduated cylinder to measure 40mL DMF and pour it into the three-necked flask, stir to dissolve it completely, then accurately weigh 0.32g EDC and 0.19g NHS and add them to the above solution, and stir magnetically for 2 hours , the dissolved chitosan solution was added dropwise into a three-neck flask through a constant pressure titration funnel at a rate of 1 drop / second, and mechanically stirred for 48 hours at room temperature. Pour the reacted mixed solution into 5 times the volume of absolute ethanol to precipitate, stir for 8 hours, centrifuge at room temperature at 8000rpm for 20 minutes, discard the supernatant, collect the precipitate, wash the precip...

Embodiment 2

[0056] Digest L929 cells in the logarithmic growth phase with 0.25% trypsin, add DMEM medium containing 10% FBS to stop the digestion, resuspend the cells, and dilute the concentration to 2×10 with DMEM medium after centrifugation 4 per mL, the diluted cells were planted in a 96-well plate, with 200 μL of cell suspension per well. After the 96-well plate was placed in the cell incubator for 24 h, the culture medium in the cell plate was discarded, and 200 μL of fresh medium containing VCH blank nanoparticles with different concentrations was added, and the concentration of VCH blank nanoparticles was set to 10, 50, 100, 200 μg / mL, and the cells cultured in normal DMEM medium were set as the control group, and the cells only containing DMEM medium without planting were set as the blank control group, and 6 replicates were set for each group. Gently shake, culture in the cell incubator for 24 and 48 hours, observe the cell morphology under an inverted microscope and take picture...

Embodiment 3

[0062] 24 KM male mice were randomly divided into 2 groups, the experimental group and the control group, 12 in each group, and the experimental group injected 0.2mL VCH nanoparticles into the mice every day according to the dose of 10mg / Kg through the tail vein injection method. Saline solution, the control group injected 0.2mL physiological salt injection into the tail vein of the mice every day for seven consecutive days, and observed the daily activity status of the mice and whether there were symptoms of poisoning reaction. After the end of the administration, on the eighth day, blood was taken from each mouse by taking blood from the eye socket, and the blood taken out was collected separately to contain sodium citrate and EDTAK 2 The four blood coagulation items and blood routine tests were carried out in the blood vessels; the mice were sacrificed after the blood collection was completed, the heart, liver, spleen, lung and kidney were taken out, the fascia was peeled of...

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Abstract

The invention discloses a chitosan-based amphiphilic self-assembling nano carrier and a preparation method and an application thereof. The nano carrier is mainly chitosan, and an amino group of chitosan is respectively connected with histidine (His) and vitamin E succinate (VES); and the chitosan-based amphiphilic self-assembling nano carrier can be used for the preparation of a hydrophobic drug carrier. The average particle diameter of the nano carrier prepared by the invention is 172.1+ / -44.17 nm, PDI is 0.349, and the surface zeta potential is +49.5+ / -5.96 mV; the encapsulation efficiency of drug-loaded nanoparticle DOX / VCH drug doxorubicin after drug loading is 66.64%, and the drug loading is as high as 21.04%; the nano carrier has good anti-tumor effect in functional experiments in vitro and in vivo: the tumor inhibition rate in vitro is 56.27% at 24 h, and the tumor inhibition rate is 45.81% in 12 days.

Description

technical field [0001] The invention relates to a chitosan-modified nanometer material, in particular to a chitosan-based amphiphilic self-assembled nanometer carrier, which belongs to the field of biological material preparation. Background technique [0002] Chitosan is the only alkaline polysaccharide existing in nature. It was discovered by Frenchman C. Rouget in 1859 and was discussed as a deacetylated form of chitin. In recent decades, chitosan has been widely used in the field of biopharmaceuticals due to its superior biocompatibility, degradability, bacteriostasis, mucoadhesion, non-toxic and environmental protection, but chitosan is not ideal Solubility greatly limits its application. Chemical modification of chitosan is a way for people to develop the application prospect of chitosan. Chitosan contains a large number of active groups such as amino groups and hydroxyl groups, and various side chain groups can be introduced into the macromolecular chain to meet the...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K47/18A61K47/22A61K9/51A61K31/704A61P35/00
CPCA61K9/5123A61K9/5161A61K31/704A61P35/00
Inventor 常菁陈晓彤张旺旺张海斌张艳韩宝芹
Owner OCEAN UNIV OF CHINA
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