Brain tumor targeted drug delivery system and preparation method thereof

A drug delivery system, a technology for brain tumors, applied in antitumor drugs, pharmaceutical formulations, drug combinations, etc., can solve brain diseases epilepsy, schizophrenia difficult to achieve effective treatment, lack of tumor tissue selectivity, dose-dependent acute Toxicity and other issues, to achieve the effect of improving brain entry efficiency, good solubilization effect, and improved uptake and transport rates

Active Publication Date: 2015-05-06
黄山市屯溪区昱城产业投资控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, like other cytotoxic antitumor drugs, this type of drug lacks selectivity to tumor tissue, and has serious dose-dependent acute toxicity. Long-term use can cause dose-dependent irreversible cardiomyopathy, thus causing severe cardiotoxicity. and liver damage, at the same time, due to the existence of multidrug resistance, the clinical application is limited
[0003] The blood-brain barrier (BBB) ​​is a special physiological barrier between the brain and the blood, which is composed of brain capillary endothelial cells, intercellular tight junctions, as...

Method used

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  • Brain tumor targeted drug delivery system and preparation method thereof
  • Brain tumor targeted drug delivery system and preparation method thereof
  • Brain tumor targeted drug delivery system and preparation method thereof

Examples

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Effect test

Embodiment 1

[0050] Dissolve adriamycin in absolute ethanol, dissolve the glucose-modified amphiphilic chitosan derivative, which is the drug delivery carrier, in water, and slowly add the adriamycin solution to the drug delivery carrier solution under rapid stirring. After the solution is mixed, ultrasonic for 0.5h, ultrasonic power 360w, ultrasonic frequency 28KHz, deionized water dialysis, 0.22μm microporous filter membrane to filter out unencapsulated doxorubicin, then glucose-modified brain tumor targeting nanomicelle delivery system.

[0051] The concentration of the doxorubicin in absolute ethanol is 10 mg / mL; the concentration of the drug delivery vehicle in water is 15 mg / mL; the weight ratio of the doxorubicin to the drug delivery vehicle is 1:5;

[0052] The weight ratio of doxorubicin to drug delivery carrier in the prepared drug delivery system is 1:6;

[0053] The drug delivery carrier is synthesized by the following method:

[0054] Dissolve chitosan in a 1% acetic acid aqueous sol...

Embodiment 2

[0068] Dissolve doxorubicin in dimethyl sulfoxide, dissolve the glucose-modified amphiphilic chitosan derivative that is the drug delivery carrier in water, slowly add the doxorubicin solution to the drug delivery carrier solution under rapid stirring. After mixing the two solutions, ultrasonic 0.25h, ultrasonic power 250w, ultrasonic frequency 30KHz, deionized water dialysis, 0.22μm microporous filter membrane to filter out unencapsulated doxorubicin, that is, glucose-modified brain tumor targeting nanomicelle delivery Medicine system.

[0069] The concentration of the doxorubicin in dimethyl sulfoxide is 8 mg / mL; the concentration of the drug delivery vehicle in water is 20 mg / mL; the weight ratio of the doxorubicin to the drug delivery vehicle is 1:7;

[0070] The weight ratio of the drug to the drug delivery carrier in the prepared drug delivery system is 1:8;

[0071] The drug delivery carrier is synthesized by the following method:

[0072] Disperse chitosan in methanol, stir m...

Embodiment 3

[0086] Dissolve gambogic acid in dichloromethane, dissolve the glucose-modified amphiphilic chitosan derivative, which is the drug delivery carrier, in water, and slowly add the gambogic acid solution to the drug delivery carrier solution under rapid stirring. After the solution is mixed, ultrasonic for 0.3h, ultrasonic power 400w, ultrasonic frequency 25KHz, deionized water dialysis, 0.22μm microporous filter membrane to filter out unencapsulated gambogic acid, then glucose-modified brain tumor targeting nanomicelle delivery system.

[0087] The concentration of the gambogic acid in methylene chloride is 20 mg / mL; the concentration of the drug delivery vehicle in water is 35 mg / mL; the weight ratio of the gambogic acid to the drug delivery vehicle is 1:6;

[0088] The weight ratio of the drug to the drug delivery carrier in the prepared drug delivery system is 1:7;

[0089] The drug delivery carrier is synthesized by the following method:

[0090] Disperse chitosan in methanol, stir...

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Abstract

The invention relates to a brain tumor targeted drug delivery system and a preparation method thereof. The brain tumor targeted drug delivery system comprises a mediated molecule, a basic carrier and a drug, wherein the mediated molecule refers to glucose; the basic carrier refers to an amphipathic chitosan derivative; the mediated molecule and the basic carrier are covalently bound to form a drug delivery carrier; and the drug delivery carrier forms nano-micelles so as to encapsulate the drug. According to the drug delivery system, the accumulated amount and brain entry efficiency of the encapsulated hydrophobic antitumor drugs in the brain can be obviously improved, and the damage of the drug on other normal tissues is reduced.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a brain tumor targeted drug delivery system and a preparation method thereof. Background technique [0002] Anthracycline anti-tumor drugs are an important class of anti-tumor drugs commonly used in clinical practice. Their structure includes both fat-soluble anthraquinone cyclic ligands and water-soluble daunorubicin amines, acidic phenolic hydroxyl groups and basic amino groups. Enter tumor cells through the cell membrane and act on DNA to achieve the purpose of anti-tumor. It has a wide anti-tumor spectrum and good curative effect. It is widely used in the treatment of various cancers, such as lung cancer, leukemia, breast cancer, liver cancer, brain cancer and others Solid tumors. However, like other cytotoxic anti-tumor drugs, this type of drug lacks selectivity to tumor tissues and has severe dose-dependent acute toxicity. Long-term use can cause dose-depen...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/36A61P35/00
Inventor 牛江秀史建俊郑祖彪柯仲成程子洋李伟伟狄蕊
Owner 黄山市屯溪区昱城产业投资控股有限公司
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