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Folacin receptor mediated targeted acetyl pullulan polysaccharide nano granule and preparation thereof

A technology of pullulan and folate receptors, which is applied in the field of folate receptor-mediated targeting of acetyl pullulan and its nanoparticles and its preparation, can solve the problems that have not been seen in any literature or patent reports, and achieve improved Bioavailability, small particle size distribution range, and the effect of reducing drug side effects

Inactive Publication Date: 2008-09-03
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, folic acid and acetyl pullulan conjugates, preparation of nanoparticles by solvent diffusion method as anti-tumor drug carrier research has not seen any literature or patent reports

Method used

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  • Folacin receptor mediated targeted acetyl pullulan polysaccharide nano granule and preparation thereof
  • Folacin receptor mediated targeted acetyl pullulan polysaccharide nano granule and preparation thereof
  • Folacin receptor mediated targeted acetyl pullulan polysaccharide nano granule and preparation thereof

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Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1: the chemical synthesis of acetylated pullulan (PA)

[0045] Add 20ml of formamide to 2g of pullulan with a molecular weight of 200,000, stir it at 54°C to completely dissolve it, then add 6ml of pyridine and 7.5ml of acetic anhydride, and react the mixture at 54°C for 48h. Add 500ml of distilled water to form a black-brown precipitate, wash repeatedly with water and anhydrous methanol until the precipitate turns white, and dry in vacuum to obtain a white powder. According to the NMR method, the degree of acetyl substitution was 90.3%.

[0046] Proton NMR spectra of acetyl pullulan derivatives ( 1 H-NMR) see figure 1 . figure 1 for acetylated pullulan 1 H-NMR spectrum (solvent: deuterated dimethyl sulfoxide: DMSO-d 6 ); Compared with pullulan, PA showed methyl proton signal at 1.8-2.2ppm, indicating the presence of acetyl group.

Embodiment 2

[0047] Embodiment 2: the chemical synthesis of folic acid coupling acetylated pullulan (FPA)

[0048] Dissolve 1g (2.27mmol) of folic acid in 15ml of dimethyl sulfoxide (DMSO), dropwise add 5 drops of triethylamine, stir to dissolve completely, add 0.9g (4.4mmol) of N,N'-dicyclohexylcarbodiethylene Amine (DCC), 0.25g (2.05mmol) 4-dimethylaminopyridine (DMAP), stirred for 1 hour, then added 1.5g of acetyl pullulan dissolved in 25ml of DMSO, and reacted for 5 days under electromagnetic stirring. Remove the DCU precipitate by filtration, let stand at room temperature for 24 hours, filter again, add the filtrate dropwise to 400ml methanol solution, stir evenly, and centrifuge to collect the yellow precipitate. The precipitate was repeatedly washed with anhydrous methanol until there was no yellow in the supernatant, and then freeze-dried to obtain a yellow powder, which was a folic acid-coupled acetyl pullulan derivative. The degree of substitution of folic acid was determined to...

Embodiment 3

[0050] Embodiment 3: Preparation of loaded epidoxorubicin nanoparticles

[0051] Weigh 50 mg of folic acid-coupled acetyl pullulan and dissolve it in 5 ml of dimethylformamide to make the concentration 10 mg / ml. Dissolve 10 mg of epirubicin in 2 ml of dimethylformamide to make the concentration of epirubicin 5 mg / ml, add 5 μl of triethylamine (2 times the molar amount), and stir at 25 ° C for 12 hours in the dark to dehydrochloride the epirubicin . The drug / material solution was mixed at a volume ratio of 1:0.2, and the drug-loaded nanospheres were prepared by an automatic emulsification solvent diffusion method. That is, under electromagnetic stirring, slowly inject 1ml of the material / drug mixed solution into 10ml of 0.5% PVA solution with a syringe (the needle of the syringe is No. liquid. The nanosuspension was centrifuged at 18000 rpm at 4°C for 25 minutes to remove organic solvents, surfactants and free drugs. Add 10ml of distilled water to the precipitate to dispers...

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Abstract

The invention discloses a method for preparing folic acid coupled acetyl pullulan polysaccharide and the nanoparticles thereof, a preparation of drug-loaded nanoparticles which take the compound as the carrier and the role of the drug-loaded nanoparticles on the tumor cells. Firstly, the water soluble pullulan polysaccharide is converted to hydrophobic polymers by acetylation, so as to be conductive to the preparation of the nanoparticles and the loading of a hydrophobic drug, and the tumor cells with the high expression of the folate receptor can be targeted after the coupling of the folic acid by esterification. The drug-loaded nanoparticles are prepared by taking epirubicin as a model drug and adopting the solvent dispersion method, and the role of the drug-loaded nanoparticles on the tumor cells are evaluated by the in vitro cell uptake test. The results show that the method for preparing the folic acid-acetyl pullulan polysaccharide nanoparticles by the solvent dispersion method is simple, the reproducibility is good, the expanded production is easy, the drug-loading ratio is high, and the drug-loaded nanoparticles can be taken into the tumor cells by the route of the folate receptor.

Description

Technical field: [0001] The invention relates to a folic acid receptor-mediated targeting acetyl pullulan polysaccharide and its nanoparticle and a preparation method, that is, the hydrophilic pullulan polysaccharide is acetylated and hydrophobically modified, and then cross-linked with folic acid to form folic acid-acetyl pullulan Lulan polysaccharide conjugates, drug-loaded nanoparticles with the polymer as a carrier, a preparation method and their effects on tumor cells in vitro. Background technique: [0002] Drug delivery system (drug delivery system, DDS) is an important research direction in the field of medicine at home and abroad, especially the nano-controlled sustained-release system composed of anticancer drugs, which converts drugs into stable nanoparticles, and its outstanding advantage is that the volume of nanoparticles It is small, can run freely in the blood, has the ability to pass through the endothelial cells of the target tissue, can be taken up by tumo...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K47/48A61K45/06A61P35/00A61K47/61
Inventor 张其清张慧珠刘玲蓉李学敏
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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