Docetaxel nanometer micelle, and preparation method and application thereof

A technology of docetaxel and nano micelles, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations containing active ingredients. To solve the problems of drug application, carrier materials without medicinal specifications, etc., to achieve the effect of improving tissue distribution and pharmacokinetic characteristics, improving anti-tumor efficacy, and the preparation method is simple and easy to control

Active Publication Date: 2014-12-24
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent applications CN102264396A and CN102626521A respectively disclose HPMA-docetaxel conjugates and docetaxel-pluronic conjugates, both of which can improve the water solubility of docetaxel, but docetaxel in the tumor site Difficult to release quickly and efficiently from the conjugate
Chinese patent application CN102379849A discloses a docetaxel pH-sensitive liposome. Its preparation method is difficult to achieve industrial production, and the liposome particle size is relatively large, so it is difficult to target the tumor site through passive targeting
Chinese patent application CN102357075A discloses a docetaxel nano-preparation, most of the carrier materials used have no medicinal specifications, and there are potential safety hazards
Chinese patent application CN101653414A discloses a solid lipid nanoparticle of docetaxel, which uses a variety of excipients and complicated preparation methods
Chinese patent application CN101732234A discloses a docetaxel-loaded block polymer micelle, but the micelle does not mention the application in overcoming tumor drug resistance
Chinese patent application CN101773480A discloses a nanocrystalline preparation containing docetaxel, which has problems such as poor stability and easy precipitation of the drug
Compared with amphiphilic polymer micelles, surfactant micelles have received less attention from scholars due to their disadvantages such as small drug loading and unstable micelles, and little research has been done on the use of surfactant micelles in the study of tumor multidrug resistance. see literature report

Method used

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  • Docetaxel nanometer micelle, and preparation method and application thereof
  • Docetaxel nanometer micelle, and preparation method and application thereof
  • Docetaxel nanometer micelle, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Weigh 20 mg of docetaxel (purchased from Shanghai Sanwei Pharmaceutical Co., Ltd.), 200 mg of Pluronic L61, 200 mg of PEG-DSPE, and 50 mg of soybean oil, add 0.5 ml of absolute ethanol to dissolve it ultrasonically, and inject it into 5 ml of water (by millipore pure water instrument). (prepared) was stirred at 20,000 rpm at high speed for 1 min, and homogenized under high pressure at 20,000 psi for 5 times to obtain translucent and uniform docetaxel nanomicelles.

Embodiment 2

[0051] Weigh 20 mg of docetaxel, 300 mg of soybean lecithin, 200 mg of Pluronic P85, 200 mg of Pluronic F127, and 50 mg of corn oil, add 0.5 ml of absolute ethanol to dissolve and ultrasonically dissolve them, inject them into 5 ml of pure water and stir at a high speed of 20,000 rpm for 5 min , at 20,000 psi high-pressure homogenization 4 times to obtain translucent and uniform docetaxel nanomicelles.

Embodiment 3

[0053] Weigh 20 mg of docetaxel, HS15800 mg, 400 mg of egg yolk phospholipids, and add 0.2 ml of absolute ethanol to dissolve them, inject them into 5 ml of pure water, stir at a high speed of 15000 rpm for 10 min, and ultrasonicate through the probe (ultrasonic power: 400w , ultrasound time: 10s, ultrasound frequency: 10 times) to obtain docetaxel nanomicelles with translucency and opalescence.

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Abstract

The invention discloses a docetaxel nanometer micelle, a preparation method and application of the micelle to prepare medicines for treating tumor or drug-resistant tumor. The docetaxel nanometer micelle comprises 1 part by weight of docetaxel, 10-100 parts by weight of a carrier material and 0-10 parts of oil, wherein the average particle size of the docetaxel nanometer micelle is 10-200 nm. According to the preparation, the water solubility of docetaxel is substantially improved, the stability of the preparation is improved, the cycling time of docetaxel in blood is prolonged, the toxic and side effects of conventional preparations are reduced, docetaxel nanometer micelle can be driven to be targeted to tumor tissue through EPR effect, so that the anti-tumor curative effect of docetaxel is improved, and the docetaxel nanometer micelle overcomes the multidrug resistance of tumor.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a docetaxel nano-micelle, a preparation method and its application in the preparation of drugs for treating tumors or drug-resistant tumors. Background technique [0002] Docetaxel (DOCETAXEL) is a second-generation semi-synthetic taxane derivative, its mechanism of action is to enhance tubulin polymerization and inhibit microtubule depolymerization, resulting in the formation of stable non-functional microtubule bundles, thus destroying Mitosis of tumor cells. The pharmacological effect of docetaxel is stronger than that of paclitaxel. The concentration of docetaxel in the cell is 3 times higher than that of paclitaxel, and the residence time in the cell is longer. Its affinity for microtubules is 2 times that of paclitaxel; as a stable microtubule As an agent and assembly promoter, its activity is 2 times greater than that of paclitaxel; as a microtubule depolymerizati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/24A61K47/34A61P35/00
Inventor 李亚平陈伶俐樊继涛张志文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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