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New preparation for chemotherapy on tumor vascular thrombosis mediated by biological effect of ultrasound

A technology of biological effects and tumor blood vessels, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, anti-tumor drugs, etc. The effect of avoiding radioactive contamination, convenient operation, and preventing multidrug resistance

Inactive Publication Date: 2012-02-01
FUJIAN MEDICAL UNIV UNION HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the lack of corresponding receptors, endocrine and biological therapy cannot be performed. At present, the systemic treatment of this special type of breast cancer is limited to chemotherapy, but the effect of chemotherapy alone is not good, and tumor cells are prone to multidrug resistance.

Method used

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  • New preparation for chemotherapy on tumor vascular thrombosis mediated by biological effect of ultrasound
  • New preparation for chemotherapy on tumor vascular thrombosis mediated by biological effect of ultrasound
  • New preparation for chemotherapy on tumor vascular thrombosis mediated by biological effect of ultrasound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The synthesis of embodiment 1 PLGA-PEG-PLGA

[0024]PLGA-PEG-PLGA triblock copolymers were synthesized by ring-opening polymerization. Weigh 1.5 g of PEG with a relative molecular mass of 1500 and 2000, and dry in a vacuum environment at 95 °C for 3 h, add 3.6 g of lactide and 2 g of glycolide, continue to dry in vacuum for 30 min, add the catalyst ethylene chloride 50 mg of tin was filled with nitrogen, reacted at 140°C for 8 h, vacuumed for 30 min, and cooled naturally to obtain a light yellow PLGA-PEG-PLGA copolymer.

Embodiment 2

[0025] Example 2 Preparation of docetaxel nanomicelles

[0026] The drug-loaded copolymer nanomicelles were prepared by direct dissolution method. Prepare 1 mL of the PLGA-PEG-PLGA triblock copolymer solution prepared in Example 1 with a mass fraction of 5% in double distilled water, add 25 ul of docetaxel absolute ethanol solution (mass concentration 100 mg / mL), Vortex for 3 minutes, ultrasonically disperse for 10 minutes, and centrifuge at 10 000 r / min for 5 minutes, and the supernatant is the docetaxel-loaded copolymer nanomicelle. Docetaxel-loaded copolymer nanomicelles were vacuum freeze-dried, 60 After Co irradiation sterilization, they were stored at 4°C for later use. The mass percentage of docetaxel and PLGA-PEG-PLGA polymer is 1:20. The docetaxel-loaded copolymer nanomicelles are hereinafter referred to as docetaxel nanomicelles or nanomicelles or drug-loaded nanomicelles.

Embodiment 3

[0027] Example 3 Characterization of docetaxel nanomicelles

[0028] Prepare the aqueous solution of docetaxel copolymer nano micelles, after fully ultrasonically dispersed, drop it on the copper grid covered with carbon film, after drying, use the ion plating device to splash gold, observe under the scanning electron microscope, it can be seen that the nano micelles are well dispersed, showing Spherical (see figure 1 ), when the temperature of the docetaxel nanomicelle solution was increased to 38.5°C, the nanomicelles transformed into micron-sized embolic agents (see figure 2 ). 3 mL of the aqueous solution of docetaxel copolymer nanomicelles prepared in Preparation Example 2 was fully ultrasonically dispersed, and the average particle size of the docetaxel-loaded nanomicelles was measured by a laser particle size analyzer to be 30.8 nm, and the multivariate dispersion coefficient was 30.8 nm. 0.42. .

[0029] High performance liquid chromatography was used to detect t...

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Abstract

The invention discloses a new preparation for chemotherapy on tumor vascular thrombosis mediated by biological effect of ultrasound. The new preparation comprises a high molecular polymer and docetaxel, wherein the high molecular polymer adopts a polyethylene glycol / poly-(D,L-lactic-CO-glycollic acid) copolymer system, and the copolymer system adopts a polyethylene glycol-poly(lactic-co-glycolic acid)-polyethylene glycol, polyethylene glycol-polylactic acid-polyethylene glycol, poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic-co-glycolic acid) or polyethylene glycol / poly(lactic-co-glycolic acid) (PEG / PLGA) graft polymer. The new preparation is characterized in that the mass percent of the docetaxel to the copolymer system is (1:20)-(1:5), and docetaxel carried copolymer nano-micelle is prepared by a direct dissolution method, an emulsified solvent volatilization method or a dialyses method. The new preparation disclosed by the invention is applicable to treatment on many kinds of tumors of mammary gland, thyroid gland, liver, pancreas, kidney, ovary, peritonea and the like.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the preparation of a temperature-sensitive nano-micelle loaded with docetaxel by modern pharmacy technology, which undergoes a phase transition under the thermal effect generated by ultrasonic waves, from nano-sized micelles to micron-sized plugs It can achieve the dual anti-tumor effect of tumor vascular embolism and chemotherapy, is easy to operate, safe and efficient, and has broad clinical application prospects. Background technique [0002] Transcatheter arterial chemoembolization (TACE) mixes chemotherapy drugs and embolic agents and injects them into the tumor blood supply target artery through the catheter. On the one hand, it embolizes the tumor blood supply artery and causes tumor tissue ischemia and necrosis. The contact time with tumor tissue has dual anti-tumor effects of embolization and chemotherapy, and has been widely used in the treatment of liver cancer, brain tumors, a...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61P35/00A61K9/00A61K47/34
Inventor 陈志奎林礼务薛恩生何以敉黄静
Owner FUJIAN MEDICAL UNIV UNION HOSPITAL
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