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Target-oriented sustained-release microsphere containing paclitaxel and albumin and preparation process thereof

A slow-release microsphere and paclitaxel technology, which is applied in the direction of bulk delivery, inorganic non-active ingredients, polymer compound non-effective ingredients, etc., can solve the problem of non-targeting of microspheres

Inactive Publication Date: 2007-07-11
NANJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Abraxane (I), a new type of "protein-bound particle" paclitaxel formulation from American Bioscience (AB), has been approved by the US FDA, but it only consists of albumin-bound paclitaxel nanoparticles, and the microspheres do not have targeting properties

Method used

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  • Target-oriented sustained-release microsphere containing paclitaxel and albumin and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0030] Take nano-magnetic liquid (average particle size 16.3nm) and separate it by magnet, wash with distilled water several times to obtain magnetic precipitation, take 20mg of magnetic powder and add 50ml of double distilled water, after ultrasonic dispersion for 5 minutes; Add 200μL of 30mg / 5ml) to the above rice magnetic liquid, stir, and disperse ultrasonically at 40°C for 15min. The above solution is heated in a water bath to 90°C, and after ultrasonic treatment at 90kHZ for 5 minutes, add 100μL of human serum albumin after thorough mixing. After reacting for 1 hour, the mixture was quickly ice-bathed at 11000r·min -1 centrifuged at a high speed, and freeze-dried to obtain magnetic nanoparticle paclitaxel microspheres. The composition and the weight percent content ratio of the magnetic nano-paclitaxel albumin targeted sustained-release microspheres made are about paclitaxel: magnetic material: emulsifier: albumin=0.1%: 30%: 50%: 19.9%, the average particle size of the p...

example 2

[0032] Dissolve 5 mg of paclitaxel bulk drug and 2 mg of emulsifier polyoxyethylene castor oil in 2 ml of absolute ethanol with a content of more than 98.5%, fully stir and dissolve, and add it to the aqueous solution containing 5 mg of nano-magnetic particles treated as in Example 1, Ultrasonic dispersion at 20°C for 30min, the above solution was heated in a water bath at 120°C, and stirred at a speed of 1000r / min to disperse, after thorough mixing, 100μL of human serum albumin was added and fully reacted for 30min. -1 centrifuged at a high speed, and freeze-dried to obtain magnetic nanoparticle paclitaxel microspheres. The composition and weight percentage ratio of the prepared magnetic nano-paclitaxel albumin targeted slow-release microspheres are about paclitaxel:magnetic material:emulsifier:albumin=20%:25%:10%:45%. The average particle diameter of the particles was 300 nm.

example 3

[0034] Dissolve 5 mg of the paclitaxel raw material drug with a content of more than 98.5% in chloroform, stir and dissolve fully, take paclitaxel and add it to the aqueous solution of 20 mg of nano-magnetic particles treated as in Example 1, and ultrasonically disperse at 30 ° C for 20 minutes. Heat in a water bath at 70°C, stir and disperse at a speed of 3000r / min, add 3mL of human serum albumin after thorough mixing, mix and react for 10 hours, evaporate the chloroform, put the mixture in an ice bath, and put it in an ice bath at 11000r·min -1 centrifuged at a high speed, and freeze-dried to obtain magnetic nanoparticle paclitaxel microspheres. The composition and weight percentage ratio of the prepared magnetic nano-paclitaxel albumin targeted slow-release microspheres are about paclitaxel:magnetic material:albumin=0.5%:9.5%:90%, and the average particle diameter of the particles is 120nm.

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Abstract

The invention relates to a method for preparing magnetic nanometer Paclitaxel albumin target slow-release agent, wherein its production comprises that: dissolving Paclitaxel into organic solvent; adding nanometer magnetic flow, to be emulsified and mixed; adding albumin with higher combination with Paclitaxel as carrier, to be heated and solidified. The average diameter of product is 50-500nm; via magnetic function, it can directionally move with slow-release property, to target slowly release. The invention has low cost and high effect.

Description

technical field [0001] The present invention relates to paclitaxel albumin targeted slow-release microspheres and a preparation method thereof, in particular to a preparation method of magnetic nano-paclitaxel albumin targeted slow-release microspheres, which is a kind of application research of nano-magnetic materials in the field of medicine . Background technique [0002] Due to its nanometer size and special magnetic targeting properties, nano-magnetic powders have broad application prospects in pharmaceutical preparations, and new preparations can improve drug efficacy, reduce patient pain, and reduce costs, and have great economic benefits and social benefits. The research on Paclitaxel in "New Anticancer Drugs Paclitaxel and Docetaxel" edited by Yuan Yingjin showed that Paclitaxel has a novel mechanism of action as a microtubule depolymerization stabilizer, and it is effective for a variety of solid tumors in clinical trials. It has outstanding curative effect on re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K47/42A61K47/02A61K9/16A61P35/00
Inventor 沈晓冬崔升林本兰
Owner NANJING UNIV OF TECH
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