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Nanometer NAMI-A particle and its prepn process and application

A NAMI-A, nanoparticle technology, applied in antitumor drugs, drug combinations, powder delivery, etc., can solve the problems of fast metabolism, lack of selectivity, enhanced drug side effects, etc., achieving good biocompatibility and simple preparation method , good anticancer activity

Inactive Publication Date: 2007-03-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are certain defects in the administration of macromolecular drugs. Through oral administration or injection, the drug concentration in the body in a short period of time far exceeds the actual demand, and there is a lack of selectivity to enter the human body; macromolecular drugs have fast metabolism and short half-life, making the drug The concentration in the body decreases quickly and affects the curative effect, so large doses of drug administration are required, and excessive drug concentration will enhance the side effects of the drug; biomacromolecular drugs are easily degraded or inactivated by enzymes in the body, and the biological half-life is short. Repeated administration is also limited by the immune system, tissues, cell membranes, etc. Most of them are not easy to pass through these biological barriers, so the bioavailability of macromolecular drugs is low

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Dissolve 150mg of PLGA (molecular weight: 8000) in 4ml of dichloromethane, add 6ml of an aqueous solution containing 20mg of NAMI-A into the PLGA solution, and ultrasonically emulsify for 5min with an ultrasonic cell disruptor. The formed suspension was added to 20 ml of an aqueous solution in which 100 mg of sodium cholate was dissolved, and ultrasonically emulsified for 5 min to obtain a suspension. The above suspension was passed through a microporous filter membrane with a pore size of 0.12 μm, and the filtrate was centrifuged (15000 rpm) for 15 min in a high-speed centrifuge to collect the solid. The collected solid was dispersed with distilled water, and centrifuged once more (15000 rpm) to collect the solid. The collected solid was freeze-dried for 24 hours with a freeze dryer to obtain NAMI-A nanoparticles in the form of white powder. The particle diameter measured by a laser particle size analyzer is 195nm; the particle is a regular spherical shape as observed...

Embodiment 2

[0027] 100 mg of PLGA (molecular weight: 8000) was dissolved in 4 ml of dichloromethane, 6 ml of an aqueous solution dissolved with 10 mg of NAMI-A was added to the PLGA solution, and ultrasonically emulsified for 10 min. The formed suspension was added to 20 ml of an aqueous solution in which 150 mg of sodium cholate was dissolved, and ultrasonically emulsified for 10 min to obtain a suspension. The above suspension was passed through a microporous filter membrane with a pore size of 0.12 μm, and the filtrate was centrifuged (15000 rpm) for 15 min in a high-speed centrifuge to collect the solid. The collected solid was dispersed with distilled water, and centrifuged once more (15000 rpm) to collect the solid. The collected solid was freeze-dried for 24 hours with a freeze dryer to obtain NAMI-A nanoparticles in the form of white powder. The particle diameter measured by a laser particle size analyzer is 133nm; the particle is a regular spherical shape observed by a thermal f...

Embodiment 3

[0029] Dissolve 100mg chitosan in 50ml 1% acetic acid solution and pass through a 0.22μm filter membrane. 10mg NAMI-A is dissolved in the chitosan solution, under stirring at room temperature (200rpm), the above solution is added dropwise into 20ml of the TPP aqueous solution with a concentration of 1.0mg / ml with a No. 7 syringe, so that the mass of chitosan and TPP The ratio was 5:1, and stirred for 10 minutes. Centrifuge at high speed (12000rpm) for 10min to collect the solid. The collected solid was dispersed with distilled water, and centrifuged once more (15000 rpm) to collect the solid. Vacuum-dried at room temperature to obtain white powdery NAMI-A nanoparticles. The particle is observed by the thermal field and the scanning electron microscope as a regular spherical shape, and the particle diameter is about 50nm.

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Abstract

The present invention relates to nanometer antitumor medicine, and discloses nanometer NAMI-A particle and its preparation process and application. The nanometer NAMI-A particle contains Ru complex NAMI-A and basic material of chitosan or PLGA. The nanometer NAMI-A particle may be prepared through a double emulsifying process or an ionic gel process, and has simple preparation process, high stability and high repeatability. The nanometer NAMI-A particle with biodegradable chitosan or PLGA as basic material has high biocompatibility, high anticancer activity, no toxic side effect, regular spherical form and controllable medicine release.

Description

technical field [0001] The invention relates to nanometer antitumor drugs, in particular to NAMI-A nanoparticle and its preparation method and application. Background technique [0002] Malignant tumors have a high mortality rate and are one of the most serious diseases that endanger human health. In recent years, the research on non-platinum metal anti-tumor drugs has been greatly developed, and the most concerned ones are ruthenium complexes. The antitumor activity of ruthenium (Ru) complexes is related to its physiological activity. Usually Ru complexes have a much stronger binding ability to DNA than Pt complexes. Under physiological conditions, the antitumor activity of Ru complexes lies in the remarkable selectivity of binding to plasma and proteins (albumin and transferrin), which is derived from the imidazole ligand. The results of in vitro and in vivo physiological experiments show that the complexes of NAMI-A and some ruthenium are almost non-toxic, and the comp...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/555A61P35/00
Inventor 刘杰张璇陈兰美谭彩萍石硕计亮年
Owner SUN YAT SEN UNIV