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Degradable polymer supported nanometer Daunorubicin microsphere and its prepn process

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

Inactive Publication Date: 2007-06-06
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 prepn process
  • Degradable polymer supported nanometer Daunorubicin microsphere and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The polylactic acid is dissolved in an organic solvent with a volume ratio of methylene chloride: 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 is 5 mg / ml. : 1 mixed, emulsified into a primary emulsion by ultrasonic, added this primary emulsion to 30 ml of a 1% gelatin aqueous solution, sonicated again to form a double emulsion, and slowly added the double emulsion to 150 ml of a 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, washe...

Embodiment 2

[0023] The polylactic acid is dissolved in an organic solvent with a volume ratio of methylene chloride: acetone=4: 1 to form an organic solution with a concentration of 10 mg / ml, and then with an aqueous solution containing daunorubicin 5 mg / ml by volume to be 10 : 1 mixed, emulsified into a primary emulsion by ultrasonic, added this primary emulsion to 30 ml of a 1% gelatin aqueous solution, sonicated again to form a double emulsion, and slowly added the double emulsion to 150 ml of a 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 centrifugation, washed...

Embodiment 3

[0026] The polylactic acid is dissolved in an organic solvent with a volume ratio of methylene chloride: acetone=5: 1 to form an organic solution with a concentration of 20 mg / ml, and then with an aqueous solution containing daunorubicin 10 mg / ml by volume to be 20 : 1 mixed, emulsified into a primary emulsion by ultrasonic, added this primary emulsion to 30 ml of a 1% gelatin aqueous solution, sonicated again to form a double emulsion, and slowly added the double emulsion to 150 ml of a 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 centrifugation, wash...

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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 free radicals ( OH-), causing lipid peroxidation of mitochondrial membrane and endoplasmic reticulum, resulting in cytotoxicity; but DNR can also specifically bind to mitochondrial DNA, especially cardiolipin DNA, to generate compl...

Claims

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Application Information

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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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