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Oxymatrine hepatic targeting nano drug delivery system and preparation method thereof

A technology of oxymatrine and drug delivery system, which is applied in the field of nano-targeted drug delivery system and preparation containing oxymatrine, can solve the problems of increased dose, less liver distribution, short half-life of oxymatrine, and the like, Achieving the effect of delaying clearance, improving efficacy, and increasing access to the liver

Active Publication Date: 2013-03-13
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, oxymatrine has a short half-life and less liver distribution. In order to ensure the curative effect in clinical practice, increasing the dose and prolonging the course of treatment increases the frequency of adverse drug reactions.

Method used

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  • Oxymatrine hepatic targeting nano drug delivery system and preparation method thereof
  • Oxymatrine hepatic targeting nano drug delivery system and preparation method thereof
  • Oxymatrine hepatic targeting nano drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 film dispersion method

[0034]Put MALPEG3500-PCL9000 and MPEG3000-PCL4000 in a molar ratio of 1:10~15 into a 50ml round bottom flask, add 1~3ml of chloroform to dissolve, heat in a water bath at 32~38°C to remove the organic solvent, and then pass it into Nitrogen for 2 to 5 minutes to remove residual solvent to form a dry polymer film; add 2ml of citric acid buffer (pH: 3.5 to 4.5) with a concentration of 150mM / L, transfer the suspension to a 5ml beaker, seal it, and stir at 45 to 70°C Hydrate for 4-8 hours, then ultrasonically disperse for 5-15 minutes with a power of 70-150w, and obtain blank polymer nanoparticles with a particle size of about 80-120nm; after adjusting the pH to 3.5-5 with 1M / L sodium hydroxide, press oxidation The mass ratio of matrine: polyethylene glycol-polycaprolactone is 1:3~8. Add the stock solution of oxymatrine to the system obtained in the step, stir and incubate in a water bath at 25~65°C for 1~3h, and then use Sodium hydrox...

Embodiment 2

[0035] Embodiment 2 film dispersion method

[0036] Put MALPEG4500-PCL1000 and MPEG5000-PCL9000 in a molar ratio of 1:10~15 into a 50ml round bottom flask, add 1~3ml of chloroform to dissolve, heat in a water bath at 32~38°C to remove the organic solvent, and then pass it into Nitrogen for 2 to 5 minutes to remove residual solvent to form a dry polymer film; add 2ml of citric acid buffer (pH: 3.5 to 4.5) with a concentration of 150mM / L, transfer the suspension to a 5ml beaker, seal it, and stir at 55 to 75°C Hydrate for 6-12 hours, and then ultrasonically disperse with 200-400w power for 8-20 minutes to obtain blank polymer nanoparticles with a particle size of about 100-160nm; after adjusting the pH to 3.5-5 with 1M / L sodium hydroxide, press oxidation The mass ratio of matrine: polyethylene glycol-polycaprolactone is 1:3~8. Add the oxymatrine stock solution to the system obtained in the step, stir and incubate in a water bath at 25~65°C for 2~5h, and then use Sodium hydroxid...

Embodiment 3

[0037] Embodiment 3 reverse evaporation method

[0038] Dissolve MALPEG3.5K-PCL7K and MPEG3K-PCL4K in a molar ratio of 1:10-15 in 2-3 mL of chloroform to form an organic phase; Dilute the oxymatrine stock solution into 3-5 mL of 0.05 M / L phosphate buffer solution to form an aqueous phase. Ultrasonic the organic phase at a power of 100-150W, add the water phase to the organic phase, ultrasonically form a uniform dispersion system of water and oil, and remove the organic solvent by rotary evaporation under reduced pressure in a water bath at 40-60°C to obtain Shake the colloidal solution and continue to evaporate under reduced pressure to obtain drug-loaded polymer nanoparticles with a particle size of about 100-180°C and uniform size distribution. Use 1M / L sodium hydroxide to adjust the pH to 7.35-7.45; Peptide RGD was added to the drug-loaded nanoparticles according to the molar ratio of RGD:MALPEG-PCL 1:5~15, and after 10~12 hours of magnetic stirring reaction at 25~37°C, th...

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Abstract

The invention relates to an oxymatrine hepatic targeting nano drug delivery system and a preparation method thereof. The oxymatrine hepatic targeting nano drug delivery system is prepared by the following steps of: with polyethylene glycol-polycaprolactone block polymer as a carrier, preparing polymer nanoparticles by adopting a film dispersion method, a reverse evaporation method or an organic solvent injection method, encapsulating oxymatrine into the polymer nanoparticles, then modifying a new glycoprotein or cyclic octapeptide ligand to be taken as a ligand on the surfaces of the nanoparticles, and constructing an anti-hepatic fibrosis nano targeting drug delivery system for hepatic stellate cells (HSCs). The nano drug delivery system has the advantages that particle size is 50-260nm, encapsulation efficiency is 18-42%, drug loading capacity is 2-12% and the surface of the nano drug delivery system is rich in new glycoprotein M6PHSA (mannose-6-phosphate human serum albumin) or cyclic octapeptide RGD (arg gly asp). The oxymatrine hepatic targeting nano drug delivery system provided by the invention can increase opportunities that nanoparticles enter the liver through blood circulation, is beneficial to targeting distribution of drugs at focus parts of the liver and is beneficial to absorption of drug-carrying nanoparticles at lesion parts of the liver and ingestion of HSCs, so that hepatic fibrosis treatment is enhanced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a nano-targeted drug delivery system containing oxymatrine and a preparation method. More precisely, the present invention relates to a ligand-modified polymer nanoparticle-loaded oxymatrine liver-targeted nano drug delivery system and a preparation method thereof. Background technique [0002] Hepatic fibrosis (HF) and cirrhosis represent the ultimate common outcome of various chronic liver diseases, and currently there is no effective treatment. Oxymatrine, namely matrine, is easily soluble in water. It is one of the alkaloids extracted from Sophoraal opecuraidesl, a characteristic Chinese medicinal material in Ningxia. It has anti-hepatitis virus and anti-arrhythmia. and antitumor effects. Studies in recent years have shown that oxymatrine has a clear anti-hepatic fibrosis effect, and has been widely used in clinical practice. However, oxymatrine has a short half-li...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/4375A61K47/42A61K47/34A61P1/16
Inventor 杨建宏刘艳华戴贵东侯延辉张亚军陈建海
Owner NINGXIA MEDICAL UNIV
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