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Magnet composite drug-carrying microspheres and preparation method thereof

A technology of drug-loaded microspheres and magnetism, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, non-effective ingredients of polymer compounds, etc., can solve the problems of few functional groups, difficult multi-functional modification, poor hydrophilicity, etc. It achieves the effect of simple preparation process, strong function of crossing the biofilm barrier, and good stability

Active Publication Date: 2013-05-22
JIANGSU ZODIAC MARINE BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a drug carrier, PLGA has certain defects: (1) poor hydrophilicity; (2) the surface of PLGA microspheres has few functional groups, making it difficult to carry out multifunctional modification; (3) the surface of PLGA microspheres is negatively charged, making it difficult to be used in gene carrier

Method used

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  • Magnet composite drug-carrying microspheres and preparation method thereof
  • Magnet composite drug-carrying microspheres and preparation method thereof
  • Magnet composite drug-carrying microspheres and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Preparation process of composite drug-loaded microspheres. The drug used is a water-soluble drug doxorubicin, and the magnetic nanoparticles used are ferric oxide nanoparticles with a particle diameter of 7 nanometers and a saturation magnetization of 64.2 emu / g. The mass proportioning of raw materials is as follows:

[0030] PLGA:PVA=1:1.5;

[0031] PLGA: doxorubicin: magnetic nanoparticles = 100:10:3;

[0032] TAT-OQLCS:Chol=3:1;

[0033] Polymer lipid film: PLGA drug-loaded microspheres = 2.5:1.

[0034] (1) Weigh 5 mg of doxorubicin and dissolve it in 1 mL of distilled water, and set aside; weigh 50 mg of PLGA and place it in a small beaker, add 3 mL of dichloromethane to dissolve it completely, add 1.5 mg of magnetic nanoparticles, and use an ultrasonic cell pulverizer to Ultrasound was performed at 200W power. Add adriamycin aqueous solution to the small beaker during ultrasonication, and continue ultrasonication until a uniform water-in-oil emulsion is forme...

Embodiment 2

[0041] Preparation process of composite drug-loaded microspheres. The medicine used is bovine serum albumin, a water-soluble protein model medicine, and the magnetic nanoparticles used are iron ferric oxide nanoparticles with a particle diameter of 6 nanometers and a saturation magnetization of 73.7emu / g. The mass proportioning of raw materials is as follows:

[0042] PLGA:PVA=1:2;

[0043] PLGA: bovine serum albumin: magnetic nanoparticles = 60:5:5;

[0044] TAT-OQLCS:Chol=2:1;

[0045] Polymer lipid film: PLGA drug-loaded microspheres = 1:1.

[0046] (1) Weigh 5 mg of bovine serum albumin and dissolve it in 1 mL of distilled water for use; weigh 60 mg of PLGA and place it in a small beaker, add 3 mL of dichloromethane to dissolve it completely, add 5 mg of magnetic nanoparticles, and use an ultrasonic cell pulverizer at 50W Ultrasound at high power. Add bovine serum albumin aqueous solution to the small beaker during the ultrasonication process, and continue ultrasonica...

Embodiment 3

[0053] Preparation process of composite drug-loaded microspheres. The drug used is paclitaxel, an oil-soluble drug, and the magnetic nanoparticles used are iron ferric oxide nanoparticles with a particle diameter of 10 nm and a saturation magnetization of 79.3 emu / g. The mass proportioning of raw materials is as follows:

[0054] PLGA:PVA=1:1;

[0055] PLGA: paclitaxel: magnetic nanoparticles = 30:8:2;

[0056] TAT-OQLCS:Chol=4:1;

[0057] Polymer lipid film: PLGA drug-loaded microspheres = 4:1.

[0058] (1) Weigh 30mg of PLGA and place it in a small beaker, add 3mL of dichloromethane to dissolve it completely, add 2mg of magnetic nanoparticles and 8mg of paclitaxel, so that the magnetic nanoparticles are evenly dispersed, and the paclitaxel is completely dissolved;

[0059] (2) Pour the solution in the small beaker into a beaker filled with 10 mL of PVA solution with a concentration of 3 mg / mL, and use an ultrasonic cell pulverizer to perform ultrasound at a power of 100 ...

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Abstract

The invention relates to magnet composite drug-carrying microspheres and a preparation method thereof. Magnetic nanoparticles and drugs are loaded inside poly lactic-co-glycolic acid copolymer microspheres and a cation high polymer liposome prepared from lysine chitosan octadecyl quaternary ammonium salt modified by transactivator TAT and cholesterol coats the poly lactic-co-glycolic acid copolymer microspheres, so that a core-shell drug-carrying microsphere system is formed; after the magnetic nanoparticles and the drugs are loaded into the composite drug-carrying microsphere system, the composite drug-carrying microsphere system has the particle size in the range of 300 to 400 mum, positive surface Zeta potential and high stability and can be stored for at least two months after being freeze-dried; and the slow-release composite drug-carrying system loaded with the magnetic nanoparticles and the drugs, which is provided by the invention, has the characteristics of uniform and controllable particle size, high stability, surface modified by the transactivator TAT, simple preparation process and the like and is suitable for mass production.

Description

technical field [0001] The invention relates to a composite drug-loaded microsphere carrying magnetic nanoparticles and drugs and a preparation method thereof, belonging to the technical field of drugs. Background technique [0002] The special properties of magnetic nanoparticles, such as superparamagnetism and high coercive force, make them widely used in magnetic recording materials, magnetic liquids, biomedicine, sensors, catalysis, permanent magnetic materials, pigments, radar wave absorbing materials and other fields Has a wide range of applications. Among them, in the field of biomedicine, the carrier can be used to simultaneously encapsulate magnetic nanoparticles and drugs, so that the drug carrier can be targeted, improve the utilization efficiency of drugs and reduce toxic and side effects. [0003] Poly(lactic-co-glycolic acid) (PLGA) is formed by random polymerization of lactic acid and glycolic acid. It is a degradable functional polymer organic compound with ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/42A61K47/34A61K47/36A61K47/28A61K48/00
Inventor 常津王亮亮王生康世胤苏文雅
Owner JIANGSU ZODIAC MARINE BIOTECH