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Preparation method of novel magnetic 5-fluorouracil carrying polylactic-co-glycolic acid (PLGA) material

The technology of fluorouracil poly(lactic acid glycolic acid and lactic acid glycolic acid) is applied in the field of preparation of polymer materials and drug-carrying nanomaterials, which can solve the problems of low drug loading and instability of microspheres, and achieves wide sources, low damage, The effect of the simple and easy synthesis method

Inactive Publication Date: 2014-06-25
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

5-Fu is currently widely used clinically, especially in the treatment of digestive tract malignant tumors, so far there is no other drug that can replace it
But 5-Fu is a kind of insoluble in water, insoluble in the white crystal of organic solvents such as ethanol, methyl alcohol and acetone, has run into a lot of difficult problems aspect the preparation loaded 5-Fu microsphere, and the method that uses most at present is exactly to make drug Preparation of drug-loaded microspheres by suspending in an organic solution, resulting in extremely low and unstable drug loading of the microspheres

Method used

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  • Preparation method of novel magnetic 5-fluorouracil carrying polylactic-co-glycolic acid (PLGA) material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 200 mg of polylactic-co-glycolic acid (PLGA), wherein the copolymerization ratio of lactic acid (LA) to glycolic acid (GA) is 75:25. It was then dissolved in dichloromethane, and 5 mg of magnetic nanoparticles Fe were added to the solution 2 o 3 Then ultrasonic 2min to make it evenly dispersed; 200mg of 5-Fu was dissolved in 2mL of DMSO, then added to the dichloromethane solution of PLGA, ultrasonic 2min to obtain oil-in-oil O / O emulsion; the resulting emulsion Add it dropwise to 60 mL of PVA aqueous solution saturated with 5-Fu, stir mechanically for 3 hours, volatilize the dichloromethane, and solidify the microspheres; stop stirring, settle, pour off the upper layer of liquid, collect the lower layer of microspheres, and wash with deionized water three times; Suction filtration with a Buchner funnel, and freeze-drying to obtain magnetic drug-loaded microspheres.

Embodiment 2

[0028] Weigh 200 mg of polylactic-co-glycolic acid (PLGA), wherein the copolymerization ratio of lactic acid (LA) to glycolic acid (GA) is 50:50. It was then dissolved in dichloromethane, and 10 mg of magnetic nanoparticles MnFe was added to the solution 2 o 4 Then ultrasonic 2.5min to make it evenly dispersed; 180mg of 5-Fu was dissolved in 2mL of DMSO, then added to the dichloromethane solution of PLGA, ultrasonic 2.5min to obtain oil-in-oil O / O emulsion; Add the emulsion dropwise to 70 mL of PVA aqueous solution saturated with 5-Fu, stir mechanically for 4 hours, volatilize the methylene chloride, and solidify the microspheres; stop stirring, settle, pour off the upper liquid, collect the microspheres in the lower layer, and wash with deionized water Three times; suction filtration with a Buchner funnel, and freeze-drying to obtain magnetic drug-loaded microspheres.

Embodiment 3

[0030] Weigh 250 mg of polylactic-co-glycolic acid (PLGA), wherein the copolymerization ratio of lactic acid (LA) to glycolic acid (GA) is 80:20. It was then dissolved in dichloromethane, and 5 mg of magnetic nanoparticles CoFe 2 o 4 , and then sonicated for 1.5min to make it uniformly dispersed; 190mg of 5-Fu was dissolved in 2mL of DMSO, and then added to the dichloromethane solution of PLGA, sonicated for 3min to obtain an oil-in-oil O / O emulsion; the resulting Add the emulsion dropwise to 70 mL of PVA aqueous solution saturated with 5-Fu, and stir mechanically for 3.5 h to volatilize the dichloromethane and solidify the microspheres; stop stirring, settle, pour off the upper liquid, collect the lower layer of microspheres, Wash three times; filter with Buchner funnel, and freeze-dry to obtain magnetic drug-loaded microspheres.

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Abstract

The invention relates to a preparation method of a novel magnetic 5-fluorouracil carrying polylactic-co-glycolic acid (PLGA) material. The preparation method of the novel magnetic 5-fluorouracil carrying PLGA material comprises the following steps: adding nano particles into a PLGA solution, dissolving 5-fluorouracil into dimethyl sulfoxide (DMSO), adding 5-Fu DMSO solution into the PLGA solution, and carrying out ultrasonic treatment, so that oil in oil (O / O) emulsion is obtained; then adding the O / O emulsion into PVA aqueous solution saturated by 5-Fu, stirring for evaporating a solvent, solidifying microspheres, washing with deionized water, and performing freeze drying, so that the magnetic 5-Fu carrying PLGA microspheres are obtained. The obtained drug carrying microspheres are uniform in particle size, and the particle size is 100-500 microns. Drug loading capacity of the microspheres is high and can be 10%. Drug releasing rate is regulated by regulating ratio of LA to GA in PLGA. As magnetic nano particles are introduced, under the control action of an external magnetic field, the drug carrying microspheres can be concentrated in a tumour region, and drug concentration in the tumour region is increased, so that apoptosis of tumour cells is quick, and harm of anti-tumour drug to normal cells is reduced to minimum. The preparation method of the novel magnetic 5-fluorouracil carrying PLGA material is simple and practicable, raw materials can be industrially produced, and the preparation method of the novel magnetic 5-fluorouracil carrying PLGA material has good popularization and application values.

Description

technical field [0001] The invention belongs to the field of preparation of polymer materials and drug-loaded nanometer materials, and in particular relates to a preparation method of a novel magnetically loaded 5-fluorouracil poly(lactic-co-glycolic acid) (PLGA) material. Background technique [0002] Poly(lactic-co-glycolic-acid) copolymer (PLGA) is a degradable functional polymer compound formed by the random copolymerization of two monomers - lactic acid and glycolic acid. It has good biocompatibility and biodegradability, non-toxic and harmless, it is degraded into carbon dioxide and water in the body, and it is not easy to accumulate in the body. It has been approved by the US Drug and Food Administration (FDA) as a medicinal product Excipients have been widely used in pharmaceuticals, medical engineering materials and modern industrial fields. Due to its excellent encapsulation and film-forming properties, many drugs have used PLGA as a framework material to prepare ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34A61K47/02A61K31/513A61P35/00
Inventor 袁伟忠沈进任杰李茂全李建波
Owner TONGJI UNIV
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