Method for preparing PLGA slow-release microsphere carrying docetaxel and application thereof in chemotherapy of mesenchyma stroma of tumors under ultrasonic mediation

A docetaxel and docetaxel-loaded technology, which is applied in the field of interstitial chemotherapy of tumors and sustained-release preparations of docetaxel, can solve the problems of obvious systemic adverse reactions, low tumor drug concentration, poor curative effect, etc. Toxic and side effects, reducing the effect of drug hydrolysis

Inactive Publication Date: 2010-04-28
FUJIAN MEDICAL UNIV UNION HOSPITAL
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Problems solved by technology

[0003] After systemic administration of traditional chemotherapy, the local drug concentration in the tumor is low, an

Method used

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  • Method for preparing PLGA slow-release microsphere carrying docetaxel and application thereof in chemotherapy of mesenchyma stroma of tumors under ultrasonic mediation
  • Method for preparing PLGA slow-release microsphere carrying docetaxel and application thereof in chemotherapy of mesenchyma stroma of tumors under ultrasonic mediation
  • Method for preparing PLGA slow-release microsphere carrying docetaxel and application thereof in chemotherapy of mesenchyma stroma of tumors under ultrasonic mediation

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Embodiment

[0018] 1. Preparation of PLGA sustained-release microspheres loaded with docetaxel

[0019] The PLGA microspheres loaded with docetaxel were prepared by solvent evaporation method. Accurately weigh 50 mg of PLGA, dissolve in 1 ml of dichloromethane, add 3 mg of docetaxel, vortex and oscillate to fully dissolve, and form an organic phase. Draw the organic phase with a 1ml syringe, slowly inject it into 50ml of 3% PVA aqueous solution, stir with electric force at 800rpm for 2 minutes, and continue magnetic stirring for 3 hours. The solidified drug-loaded microspheres were filtered through a 0.22 μm microporous membrane, washed repeatedly with 500 ml of distilled water, collected the drug-loaded microspheres, and vacuum freeze-dried to obtain PLGA microspheres loaded with docetaxel.

[0020] Experiments show that: when the feed ratio of PLGA and docetaxel is 50mg / 3mg, the obtained PLGA sustained-release microspheres loaded with docetaxel have the best encapsulation efficiency an...

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Abstract

The invention discloses a method for preparing a PLGA slow-release microsphere carrying docetaxel and an application thereof in the chemotherapy of the mesenchyma stroma of tumors under ultrasonic mediation. The PLGA slow-release microsphere carrying the docetaxel is a medicine-carrying microsphere prepared from PLGA and the docetaxel by a single emulsification method, the molecular weight of the PLGA in the medicine-carrying microsphere is 5000-50000dal, the mole ratio of lactic acid to glycollic acid is 75:25-50:50, the feeding ratio of the PLGA to the docetaxel is 100/1-100/10, and the PLGA slow-release microsphere carrying the docetaxel is prepared by emulsification in an organic solvent. The slow-release microsphere preparation carrying the docetaxel is injected into the tumor tissues of nude mice with human liver cancer, beast cancer and ovarian cancer, and the necrosis situation of the tumors is checked by pathological histology; the result shows that the slow-release microsphere carrying the docetaxel can thoroughly ablate and inactivate the tumors, reduces the whole-body toxic or side effect of the medicine obviously and is a novel method for the chemotherapy of the mesenchyma stroma of the tumors under ultrasonic intervention with very good clinical application prospect.

Description

Technical field: [0001] The present invention relates to a slow-release preparation for tumor interstitial chemotherapy, specifically, the present invention is to prepare a slow-release preparation of docetaxel, which is guided and injected into tumor tissue by ultrasonic imaging technology, and establishes a It is a new method of tumor interstitial chemotherapy that can completely inactivate tumors, is easy to operate, and has low systemic side effects. Background technique: [0002] Docetaxel is a new type of antineoplastic drug, mainly by inhibiting the depolymerization of cell microtubules, causing the spindle to lose its normal function and leading to cell death. In addition, docetaxel can also inhibit the synthesis of cellular DNA, RNA or protein, and is effective for liver cancer, ovarian cancer, breast cancer, peripheral lung cancer, pancreatic cancer, head and neck and other tumors. Because docetaxel is poorly soluble in water, the current preparations usually use ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/337A61K47/34A61P35/00
Inventor 林礼务陈志奎薛恩生蔡敏娴
Owner FUJIAN MEDICAL UNIV UNION HOSPITAL
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