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Preparation method and application of implantable fullerene polylactic acid self-agglomerating drug-loaded sustained release microspheres

A technology of fullerene polylactic acid and slow-release microspheres is applied in the field of medicine and achieves the effects of easy preparation conditions, simple preparation methods and satisfactory preparation conditions

Inactive Publication Date: 2014-05-07
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Then, how to prepare fullerene polylactic acid self-agglomerated drug-loaded sustained-release microspheres has not been reported publicly so far.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] 1) Add 2.0g of amino acid and 2.0g of sodium hydroxide to a mixed solvent of 40mL of water and absolute ethanol, where the volume ratio of water and absolute ethanol is 8:30, stir evenly, and then add dropwise to 60mL of rich In the toluene solution of fullerene, wherein the weight ratio of fullerene to toluene is 5:3, under the rotating speed of 400r / min, at room temperature, the magnetic stirring reaction is carried out for 4h, and the mixed solution of toluene, water and absolute ethanol in the upper layer is removed, After washing with absolute ethanol for 3 times, vacuum drying for 24 hours to obtain fullerene amino acid derivatives; the amino acid is any one of phenylalanine, glycine, lysine, leucine, and knott A sort of;

[0015] 2) Put 10 mg of fullerene amino acid derivatives into a container, add 5 mL of lactic acid, then add 6-12 mg of anhydrous stannous chloride, and blow nitrogen (N 2 ), saturate at room temperature for 5 minutes, in a vacuum environme...

Embodiment 2

[0018] 1) Add 2.5g of amino acid and 2.5g of sodium hydroxide to a mixed solvent of 42mL of water and absolute ethanol, where the volume ratio of water and absolute ethanol is 8:30, stir evenly, and then add dropwise to 60mL of rich In the toluene solution of fullerene, wherein the weight ratio of fullerene to toluene is 5:3, under the rotating speed of 400r / min, at room temperature, the magnetic stirring reaction is carried out for 4.5h, and the mixed solution of toluene, water and absolute ethanol in the upper layer is removed , and then washed 3 times by suction filtration of absolute ethanol, and vacuum-dried for 24 hours to obtain fullerene amino acid derivatives; any one;

[0019] 2) Put 13 mg of fullerene amino acid derivatives into a container, add 6 mL of lactic acid, then add 8 mg of anhydrous stannous chloride, and blow nitrogen (N 2 ), saturated at room temperature for 6 minutes, in a vacuum environment, preheated for 1 hour under 110°C oil bath with magnet...

Embodiment 3

[0022] 1) Add 3g of amino acid and 3g of sodium hydroxide to a mixed solvent of 45mL of water and absolute ethanol, where the volume ratio of water and absolute ethanol is 8:30, stir evenly, and then add dropwise to 60mL of fullerene In toluene solution, wherein the weight ratio of fullerene to toluene is 5:3, under the rotating speed of 400r / min, under room temperature, magnetic stirring reaction is 4.5h, removes the mixed solution of toluene, water and dehydrated alcohol of upper layer, again Suction and washing with absolute ethanol for 3 times, and vacuum drying for 24 hours to obtain fullerene amino acid derivatives; the amino acid is any one of phenylalanine, glycine, lysine, leucine, and knottine kind;

[0023] 2) Put 15 mg of fullerene amino acid derivatives into a container, add 8 mL of lactic acid, then add 9 mg of anhydrous stannous chloride, and blow nitrogen (N 2 ), saturate at room temperature for 8 minutes, in a vacuum environment, preheat for 1 hour under...

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Abstract

The invention relates to a preparation method and an application of implantable fullerene polylactic acid self-agglomerating drug-loaded sustained release microspheres so as to effectively solve the problems of preparation of the implantable fullerene polylactic acid self-agglomerating drug-loaded sustained release microspheres and application of the implantable fullerene polylactic acid self-agglomerating drug-loaded sustained release microspheres in medicines for photodynamic therapy of tumors. According to the technical scheme for solving the problems, the preparation method is characterized in that fullerene molecules are connected to polylactic acids through chemical bonds, the relative molecular weight of the polylactic acids is 10000-18000, fullerene is C60 fullerene, and the particle sizes of the microspheres are 1-10 micrometers. The preparation method is simple; preparation conditions are easily satisfied; the intrinsic characteristics of the fullerene are not damaged; and the implantable fullerene polylactic acid self-agglomerating drug-loaded sustained release microspheres enable photodynamic therapy and chemotherapy to simultaneously play a role in tumor treatment and are innovation of the medicines for treating the tumors.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method and application of implantable fullerene polylactic acid self-agglomeration drug-loaded slow-release microspheres. Background technique [0002] Fullerene (Fullerene), also known as C 60 , is the third allotrope of carbon, and is one of the great discoveries of the twentieth century. C 60 With a π electron system, it can absorb photon energy of a certain wavelength, change from the ground state to an excited state, and the C of the excited state 60 It interacts with oxygen in tissues, catalyzes the generation of active oxygen and superoxide negative free radicals, and these products interact with macromolecules in tumor cells, damaging the structure and function of cells, thereby killing tumor cells. Fullerenes can be used as photosensitizers in photodynamic therapy (PDT) of tumors. [0003] Photodynamic therapy (PDT) refers to an emerging treatment method that pr...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/34A61K9/16C08G63/08A61P35/00
Inventor 李志张振中潘丽丽张飞龙祝侠丽夏亚丹闫淑娟
Owner ZHENGZHOU UNIV
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