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Degradable polymer supported nanometer daunorubicin microsphere and its preparation process

A technology of loading daunorubicin and degrading polymers, which is applied in the field of biomedical materials, can solve problems such as damage to normal cells, adverse reactions, and problems with surgical thoroughness, and achieve good therapeutic effects, good stability, and avoid magnetic distribution. uneven effect

Inactive Publication Date: 2009-06-24
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, general radiotherapy and chemotherapy lack selectivity. While inhibiting tumors, they also damage normal cells and cause adverse reactions. Surgical treatment brings various traumas and complications to patients, and there are also problems in the thoroughness of surgery.

Method used

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  • Degradable polymer supported nanometer daunorubicin microsphere and its preparation process
  • Degradable polymer supported nanometer daunorubicin microsphere and its preparation process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The polylactic acid was dissolved in an organic solvent with a volume ratio of dichloromethane:acetone=3:1 to form an organic solution with a concentration of 5 mg / ml, and then with an aqueous solution containing daunorubicin 2.5 mg / ml by volume in a ratio of 5. : 1 Mixing, emulsification into primary emulsion by ultrasonic method, add this primary emulsion to 30 ml of 1% gelatin aqueous solution, sonicate again to form a double emulsion, slowly drop the double emulsion into 150 ml of 0.5% gelatin aqueous solution, Keep stirring at a high speed during dropwise addition, and maintain stirring for 1 hour after the end of dropping, to partially solidify the surface of the nano-microspheres, and then maintain stirring under negative pressure to accelerate the volatilization of the organic solvent in the emulsion system to completeness through the action of negative pressure. Finally, the solid nano-microspheres are collected by low-temperature high-speed centrifugation, wash...

Embodiment 2

[0023] The polylactic acid was dissolved in an organic solvent with a volume ratio of dichloromethane:acetone=4:1 to form an organic solution with a concentration of 10 mg / ml, and then mixed with an aqueous solution containing daunorubicin 5 mg / ml by volume to a ratio of 10. : 1 Mixing, emulsification into primary emulsion by ultrasonic method, add this primary emulsion to 30 ml of 1% gelatin aqueous solution, sonicate again to form a double emulsion, slowly drop the double emulsion into 150 ml of 0.5% gelatin aqueous solution, Keep stirring at a high speed during dropwise addition, and maintain stirring for 2 hours after the dropwise addition, to partially solidify the surface of the nano-microspheres, and then maintain stirring under negative pressure to accelerate the volatilization of the organic solvent in the emulsion system to completeness through the action of negative pressure. Finally, the solid nano-microspheres are collected by low-temperature high-speed centrifugat...

Embodiment 3

[0026] The polylactic acid was dissolved in an organic solvent with a volume ratio of dichloromethane:acetone=5:1 to form an organic solution with a concentration of 20 mg / ml, and then mixed with an aqueous solution containing daunorubicin 10 mg / ml by volume in a ratio of 20. : 1 Mixing, emulsification into primary emulsion by ultrasonic method, add this primary emulsion to 30 ml of 1% gelatin aqueous solution, sonicate again to form a double emulsion, slowly drop the double emulsion into 150 ml of 0.5% gelatin aqueous solution, Keep stirring at a high speed during dropwise addition, and maintain stirring for 1.5 hours after the dropwise addition to partially solidify the surface of the nano-microspheres, and then maintain stirring under negative pressure to accelerate the volatilization of the organic solvent in the emulsion system to completeness through the action of negative pressure. Finally, the solid nano-microspheres are collected by low-temperature high-speed centrifug...

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Abstract

The present invention is degradable polymer supported nanometer Daunorubicin microsphere and its preparation process. The microsphere has size of 200-800 nm, Daunorubicin carrying rate of 3.05-18.4 %, encapsulating rate of 53.2-88.3 %, and degradable polymer polylactic acid or polylactic acid-polyglycolic acid copolymer. Experiment shows that the nanometer Daunorubicin microsphere may be released continuously in buffering phosphate solution for 2-8 weeks and the releasing rate and period may be controlled through changing the sort and molecular weight of the polymer. The nanometer Daunorubicin microsphere is superior to conventional Daunorubicin preparation, and has higher acute promyelocytic leukemia cell ingesting efficiency, higher tumor cell inhibiting rate and long effective period.

Description

technical field [0001] The invention belongs to the field of biomedical materials, in particular to a degradable polymer-loaded daunorubicin nano-microsphere and a preparation method thereof. Background technique [0002] Daunorubicin (DNR) is a class of anthracycline antibiotics with broad-spectrum and high-efficiency anticancer activity that has been widely used in clinic for more than 30 years. It is mainly used for the treatment of acute myeloid leukemia. Solid tumors also have significant efficacy. DNR can embed the aromatic ring on its structure into the DNA chain, change the DNA molecular conformation, inhibit DNA replication and RNA synthesis, and mediate active free radicals, such as superoxide anion free radicals (· O 2 —) and hydroxyl radicals ( OH—), which cause lipid peroxidation in the mitochondrial membrane and endoplasmic reticulum of cells, resulting in cytotoxicity; but DNR can also specifically bind to mitochondrial DNA, especially cardiolipin DNA, to ge...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/704A61K9/14A61K47/34A61P35/00A61P35/02
Inventor 张胜民刘杰王一帆
Owner HUAZHONG UNIV OF SCI & TECH
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