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Cholesteryl-carboxymethyl Curdlan nanometer particle and preparing method

A technology of carboxymethyl-codlan polysaccharide and carboxymethyl-codlan, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., to achieve prolonged circulation time, stable structure, mild conditions

Inactive Publication Date: 2010-06-09
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, there has not been any literature or patent reports on the preparation of nanoparticles as anti-tumor drug carriers by dialysis and probe ultrasonication of cholesterol and carboxymethylcotran polysaccharide conjugates.

Method used

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  • Cholesteryl-carboxymethyl Curdlan nanometer particle and preparing method
  • Cholesteryl-carboxymethyl Curdlan nanometer particle and preparing method
  • Cholesteryl-carboxymethyl Curdlan nanometer particle and preparing method

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Embodiment 1

[0031] Embodiment 1: the chemical synthesis of carboxymethyl cotran (CMC)

[0032] Add 3 g of polysaccharide with a molecular weight of 81,000 to 80 mL of isopropanol, stir at room temperature for 30 min, then add 8 mL of 30% sodium hydroxide to the above reaction solution, and continue stirring at room temperature for 90 min. Add 3.6g of chloroacetic acid into the above reaction solution, and continue to stir the mixture at 50-60°C for 5h. The product is collected by filtration, and mixed with methanol-acetic acid (7:3, v / v) solvent, methanol-water (4:1 , v / v) mixed solvent, methanol, acetone washing to remove unreacted chloroacetic acid, finally the precipitate was dissolved in water, dialyzed with distilled water for three days, and lyophilized to obtain a white powder. The substitution degree of carboxymethyl was 75% as measured by NMR and potentiometric titration.

[0033] The proton magnetic spectrum of carboxymethyl cortlan ( 1 H-NMR) see figure 1 (solvent: deuterate...

Embodiment 2

[0034] Embodiment 2: the synthesis of cholesteryl-carboxymethyl codran polysaccharide conjugate (CCMC)

[0035] Dissolve 0.8g of fluffy carboxymethylcortlan (CMC) (carboxyl content: 3mmoL) in 40mL of anhydrous dimethyl sulfoxide (DMSO) by ultrasonication in a water bath, and add 0.57g (3mmoL) of carbodiimide (EDC) and 0.17g (1.5mmoL) of N-hydroxysuccinimide (NHS) and stirred at room temperature for 30min. Then, 10 mL of tetrahydrofuran solution dissolved with 0.35 g (0.9 mmoL) of cholesterol was added to the above carboxymethylcotran polysaccharide solution, and the reaction was continued at 45 ° C. After 48 hours, the reaction mixture was poured into 200 mL of acetone to precipitate, filtered and collected. The precipitate was washed with water-tetrahydrofuran (1:5, V / V) and tetrahydrofuran three times respectively, and finally the product was dissolved in water, dialyzed with distilled water for three days and then freeze-dried to obtain a white flocculent substance, namely ...

Embodiment 3

[0037] Embodiment 3: Preparation of CCMC nanoparticles loaded with epirubicin

[0038] Dissolve cholesteryl-carboxymethylketranan in dimethyl sulfoxide-water (1:1, V / V), dialyze in normal saline for 24 hours, and then use a probe ultrasonic instrument at 40W for 2 minutes. Ultrasound is also used In the pulse working mode, the ultrasonic wave is repeated twice, and then filtered through a microporous membrane to obtain CCMC self-aggregating nanoparticles. The morphology of CCMC self-aggregated nanoparticles is uniform spherical, see image 3 ; the particle size distribution is unimodal, see Figure 4 .

[0039] Disperse 20mg of cholesteryl-carboxymethylcodran polysaccharide in 8mL of ammonium sulfate solution (0.15mol / L), vibrate at 37°C and 50rpm for 24h, use a probe ultrasonic instrument at 40W for 2min, and then place it in a dialysis bag , dialyzed in normal saline for 4 hours to obtain blank cholesteryl-carboxymethylketranan self-aggregating nanoparticles, and adjusted...

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Abstract

The invention relates to a cholesteryl-carboxymethyl Curdlan nanometer particle and a preparing method. Cholesterol and carboxymethyl Curdlan are used as raw materials. The carboxyl of the carboxymethyl Curdlan is activated by 1-(3-dimethylaminopropyl)-3-ethylcarbodimide hydrochloride (EDC.HCl) and N-hydroxysuccinimide (NHS) firstly, and then reacts with the cholesterol to be synthesized. The mole proportion of the carboxymethyl Curdlan to the cholesterol to EDC to NHS is 1:(0.2-5):1:5. The prepared amphipathic polymer is beneficial to preparing nanometer particles and entrapping hydrophobic drugs. The invention has the advantages of simple preparing method, good reproducibility, high drug entrapping efficiency and easy industrial production, the drug entrapping particle can greatly prolong the action time of the drugs in human bodies, obviously change the distribution of the drugs in different organs, and achieve the functions on reducing toxic or side effect, prolong the circulation time in the human bodies and enhances the biological availability of the drugs.

Description

Technical field: [0001] The invention relates to a cholesteryl-carboxymethylcortlan polysaccharide nanoparticle and a preparation method thereof. The water-insoluble cotlan polysaccharide is hydrophilically modified with chloroacetic acid, and then cross-linked with cholesterol and carboxymethylcortlan Formation of cholesteryl-carboxymethylcodran polysaccharide conjugate, and the preparation method of the polymer polysaccharide as an anti-tumor drug carrier to carry drugs and its effect in animals. 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 uses a special carrier to transform drugs into stable nanoparticles. Its outstanding advantages Nanoparticles are small in size, can run freely in the blood, have the ability to pass through the endothelial cells of the target tissue...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K45/00A61P35/00
Inventor 张其清李磊白永刚张彤唐洪波刘玲蓉李学敏周志敏
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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