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A kind of method adopting chitosan and β-cyclodextrin to prepare hydrophobic drug magnetic targeting sustained and controlled release carrier

A technology of controlled release carrier and cyclodextrin, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems affecting the clinical therapeutic value of drugs, low bioavailability and short half-life. and other problems, to achieve the effect of excellent loading and slow release

Active Publication Date: 2017-07-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Considering that the current anti-inflammatory and anti-cancer drugs are mostly hydrophobic drugs, and their half-life is often short, resulting in low bioavailability of such drugs; in order to maintain effective blood drug concentrations, frequent administration is required, not only for patients It brings inconvenience, but also increases the probability of adverse reactions, which seriously affects the clinical value of this class of drugs

Method used

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  • A kind of method adopting chitosan and β-cyclodextrin to prepare hydrophobic drug magnetic targeting sustained and controlled release carrier
  • A kind of method adopting chitosan and β-cyclodextrin to prepare hydrophobic drug magnetic targeting sustained and controlled release carrier
  • A kind of method adopting chitosan and β-cyclodextrin to prepare hydrophobic drug magnetic targeting sustained and controlled release carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Implementation Example 1: Preparation of Chitosan / Cyclodextrin-modified Magnetic Microspheres

[0025] (1) Accurately weigh 3.98 g FeCl 2 4H 2 O and 10.82 g FeCl 3 ·6H 2 O, dissolved in 95 mL pure water, in N 2 Under the protection of , the temperature of the above solution was raised to 60°C, and under vigorous stirring (1200rpm), 56 mL of 25% ammonia solution was added, and the system quickly turned black. Then the temperature of the system was raised to 90°C, 1.5 g of trisodium citrate was added, and after stirring for 30 min, the obtained product was washed three times with deionized water and absolute ethanol in turn, and the supernatant was removed with the assistance of an external magnetic field. the above Fe 3 o 4 Nanoparticles, dispersed in the mixed solution of ethanol and water (the volume ratio of ethanol and water is 4:1), and made into a suspension with a concentration of 50 mg / mL, take 100 mL of the above suspension, and then add 10 mL of 25% Ammo...

Embodiment 2

[0029] Implementation example 2: preparation of magnetic microspheres modified by chitosan / cyclodextrin

[0030] (1) Accurately weigh 3.98 g FeCl 2 4H 2 O and 6.76 g FeCl 3 ·6H 2 O, dissolved in 95 mL pure water, in N 2 Under the protection of , the temperature of the above solution was raised to 60°C, and under vigorous stirring (1200 rpm), 56 mL of ammonia solution with a mass fraction of 10% was added, and the system quickly turned black. Then the temperature of the system was raised to 70°C, 0.5 g of trisodium citrate was added, and after stirring for 30 min, the obtained product was washed three times with deionized water and absolute ethanol successively, and the supernatant liquid was removed with the assistance of an external magnetic field. the above Fe 3 o 4 Nanoparticles, dispersed in a mixed solution of ethanol and water (volume ratio of ethanol and water: 4:1), made into a suspension with a concentration of 10 mg / mL, took 100 mL of the above suspension, and ...

Embodiment 3

[0034] Implementation example 3: the cyclodextrin immobilization capacity determination of the magnetic microspheres modified by chitosan / cyclodextrin

[0035] Accurately weigh 0.1 g of glucose standard substance dried to constant weight, add an appropriate amount of water to dissolve, transfer to a 100 mL volumetric flask, add distilled water to the mark and shake well to prepare a glucose solution with a concentration of 1 mg / mL, and then accurately pipette 10 mL, dilute to 100 mL with distilled water to obtain 0.1 mg / mL glucose standard solution. Pipette 0.05, 0.1, 0.2, 0.4, 0.6, 0.8, 1.0 mL of the stock solution and dilute to 2 mL with water, add 1 mL of 5% phenol reagent, and mix well. Add 5 mL of concentrated sulfuric acid along the tube wall, let it stand for 5 min, shake it, heat it in a boiling water bath for 15 min, and immediately transfer it to a cold water bath to cool to room temperature. Using distilled water as a blank, the absorbance was measured at a wavelen...

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Abstract

The invention discloses a method for preparing a magnetic-targeted sustained / controlled release carrier of a hydrophobic drug by adopting chitosan and beta-cyclodextrin. The method comprises the following steps: (1) obtaining Fe3O4 magnetic nanoparticles by adopting a chemical coprecipitation method, and adding tetraethoxysilane into a magnetic fluid to obtain Fe3O4@SiO2 magnetic microspheres; (2) obtaining epoxy group modified Fe3O4@SiO2 magnetic microspheres by adopting gamma-(2,3-epoxypropoxy)-propyltrimethoxysilicane as a coupling agent; (3) adding the epoxy group modified Fe3O4@SiO2 magnetic microspheres into an alkalized beta-cyclodextrin solution, so as to obtain cyclodextrin modified magnetic microspheres; (4) crosslinking chitosan with the cyclodextrin modified magnetic microspheres, so as to prepare chitosan / cyclodextrin modified magnetic microspheres, wherein the grain size of the magnetic polymeric microspheres is 0.085-8.046 [mu]m, and have good magnetic responsibility, and the maximum drug loading capacity of the magnetic microspheres to ibuprofen as a hydrophobic drug can reach 233.08 mg / g, and the sustained release time is as long as 24h. The invention provides the new method for preparing the magnetic-targeted sustained / controlled release carrier with biocompatibility.

Description

technical field [0001] The invention relates to a preparation method of a drug carrier, in particular to a method for preparing a hydrophobic drug magnetically targeted sustained and controlled release carrier by using chitosan and β-cyclodextrin, and belongs to the field of pharmaceutical preparations. Background technique [0002] Magnetic polymer microspheres are a new type of functional microspheres composed of magnetic materials and non-magnetic polymer materials. On the one hand, like many organic polymer microspheres, it can be endowed with a variety of active groups (such as amino, hydroxyl, carboxyl, etc.) on its surface by means of copolymerization and surface modification. On the other hand, due to its superparamagnetism, it can move to the lesion area in a directional manner to exert a therapeutic effect by simply applying an external magnetic field. [0003] The magnetic substances in magnetic polymer microspheres are mainly iron, cobalt, nickel or their oxides...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K41/00A61K47/40A61K47/36A61K47/04A61K31/192
Inventor 姚舜陈鹏飞宋航杨畅陈军
Owner SICHUAN UNIV