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Ultrasonic biological effect mediated recombinant human endostatin controlled release preparation

A vascular endothelium and biological effect technology, which can be used in medical preparations containing active ingredients, drug combinations, non-active ingredients of polymer compounds, etc., can solve the problem of limited anti-tumor angiogenesis effect, etc. No toxic side effects, slow down the degradation rate

Inactive Publication Date: 2013-04-24
FUJIAN MEDICAL UNIV UNION HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug that enters the blood circulation will soon reach the whole body with the blood flow, and can actually remain in the local tumor. The amount of drug that acts on blood vessels is very small, and the anti-tumor angiogenesis effect is limited.

Method used

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  • Ultrasonic biological effect mediated recombinant human endostatin controlled release preparation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Take 2mg of rh-ES, add 1ml of medical biological protein glue (produced by Guangzhou Beixiu Biotechnology Co., Ltd.) main glue solution (fibrinogen concentration is 50mg / ml), mix well, and mix with 1ml of catalyst solution (containing 400IU thrombin) Mix to form drug-loaded biogel. Put the drug-loaded biogel in 10ml phosphate buffer (0.01mol / L, pH7.2, containing 0.2mg / ml NaN 3 ), in a constant temperature shaker at 37°C, 80 times / min, oscillating, for in vitro release, and ELISA to measure the released drug amount. The drug-loaded bioglue releases rh-ES more stably in vitro, 21.5% in 2 hours, and 89.7% of the cumulative drug release in 5 days; see figure 1 .

[0014] The above-mentioned medical biological protein glue: produced and provided by Guangzhou Beixiu Biotechnology Co., Ltd., is a commercially available product. Each set of "medical biological protein glue" includes the main body glue of medical biological protein glue (the present invention is formulated to...

Embodiment 2

[0016] The drug-loaded bioglue released in vitro was irradiated with ultrasound at a sound intensity of 1.0 W / cm 2 , after 3 minutes of irradiation, samples were taken once at 10 minutes and 30 minutes respectively, and the drug release was measured. It was found that ultrasonic irradiation significantly promoted the drug release rate of bioglue, and had the effect of controlling drug release.

[0017] Table 1 Effect of ultrasonic irradiation on drug release rate of drug-loaded biogel (%)

[0018] group 10min 30min control group 5.2±1.6 10.1±3.3 Ultrasound irradiation group 15.7±6.8 ** 19.5±7.5 **

[0019] Note: Compared with the control group, ** P < 0.01.

Embodiment 3

[0021] Human breast cancer cell MDA-MB-231 was cultured in vitro, amplified in large quantities, and subcutaneously inoculated into the root of the right forelimb of nude mice to establish a subcutaneous xenograft tumor model in nude mice bearing human breast cancer. Fifteen tumor-bearing nude mice were selected, with the largest tumor diameter ranging from 1.2cm to 1.5cm, and randomly divided into 3 groups, 5 mice in each group, respectively (group A) rh-ES biogel intratumoral injection group, (group B) Erh-ES Intratumoral injection of biological glue+ultrasound irradiation group, (Group C) intratumoral injection of rh-ES biological glue+microbubble contrast agent+ultrasound irradiation group. In group A, the drug-loaded biological glue was injected into the tumor, the dose of rh-ES was 10mg / kg, and the injection volume of biological glue was 0.5ml; 2 Tumor tissue was irradiated with ultrasound for 3 minutes; 10 minutes after intratumoral injection in nude mice in group C, ul...

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Abstract

The invention discloses an ultrasonic biological effect mediated recombinant human endostatin controlled release preparation. A preparation method of the biological effect mediated recombinant human endostatin controlled release preparation comprises the following steps: taking 2mg of recombinant human endostatin, adding 1ml of a medical fibrin glue main glue solution with the fibrinogen concentration of 50mg / ml, uniformly mixing, and mixing with 1ml of a catalyst solution containing 400IU of thrombin to form a drug loaded biogel; and placing the drug loaded biogel in 10ml of a phosphate buffer solution having a concentration of 0.01mol / L, having a pH value of 7.2 and containing 0.2mg / ml of NaN3, and shaking on a 37DEG C constant temperature shaking table at a speed of 80times / min for in-vitro release, wherein the release amount is 21.5% 2h later, and the accumulated drug release amount reaches 89.7% 5 days later. Ultrasonic irradiation obviously promotes the drug release speed of the biogel, so the ultrasonic biological effect mediated recombinant human endostatin controlled release preparation has the drug release control effect, and can be applied to the preparation of biological effect mediated tumor blood vessel generation inhibition drugs; and the tumor inhibition rate of the ultrasonic biological effect mediated recombinant human endostatin controlled release preparation reaches 53.2%.

Description

technical field [0001] The invention relates to a biological glue preparation loaded with recombinant human vascular endostatin and its application in the preparation of drugs for inhibiting tumor angiogenesis mediated by the biological effect produced by ultrasound combined with microbubble contrast agents. Background technique [0002] Endostatin is a protein drug discovered in recent years that can inhibit angiogenesis. It specifically acts on neovascular endothelial cells, inhibits cell growth and migration, induces apoptosis, and exerts an anti-angiogenic effect. In addition, endostatin can also inhibit the expression of vascular endothelial growth factor and the activity of proteolytic enzymes on the surface of tumor cells, and play an anti-angiogenic role at multiple targets. Recombinant human endostatin (rh-ES) has higher purity and stability than endostatin, and stronger anti-angiogenic activity, and has been used in clinical anti-tumor. However, due to the lack of...

Claims

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Application Information

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IPC IPC(8): A61K38/17A61K47/42A61K9/00A61P35/00
Inventor 陈志奎林礼务薛恩生
Owner FUJIAN MEDICAL UNIV UNION HOSPITAL
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