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Preparation method of PLGA biodegradable microspheres loading disulfiram drug

A technology of biodegradation and disulfiram, which is applied in the field of preparation of PLGA biodegradable microspheres, can solve the problems of high residual surfactant, high residual organic solvent, and high drug loading on the surface of microspheres, so as to reduce solvent residual, Effects of avoiding the purge step

Inactive Publication Date: 2019-08-09
苏州岸谷纳米技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Purpose of the invention: In view of the problems of high surfactant residues, high drug loading on the surface of microspheres and high organic solvent residues in the precipitation method in the existing emulsification method, the present invention provides a PLGA biodegradable drug loaded with disulfiram Preparation method of microspheres

Method used

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  • Preparation method of PLGA biodegradable microspheres loading disulfiram drug
  • Preparation method of PLGA biodegradable microspheres loading disulfiram drug
  • Preparation method of PLGA biodegradable microspheres loading disulfiram drug

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Experimental program
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Effect test

Embodiment 1

[0017] Dissolve the PLGA biodegradable polymer with an intrinsic viscosity of 0.15dL / g (the molar ratio of LA to GA is 2:1) and disulfiram drug in dichloromethane at a mass ratio of 15:1, and transfer the solution to a syringe In the process, the needle of the syringe is submerged in distilled water which is vigorously stirred at 45°C. The stirring rate of the distilled water is 1000r / min. Under the control of the metering pump, the mixed solution of disulfiram / PLGA is added dropwise to the distilled water. The volume ratio is 1:45. After the dropwise addition, the emulsion was continuously stirred for 4 hours, and then filtered through a filter membrane with a pore size of 1 micron. After the microspheres on the filter membrane were freeze-dried, the PLGA biodegradable microspheres loaded with disulfiram drug were obtained. The SEM picture like figure 1 .

Embodiment 2

[0019] Dissolve the PLGA biodegradable polymer with an intrinsic viscosity of 0.5dL / g (the molar ratio of LA to GA is 1:1) and disulfiram drug in dichloromethane at a mass ratio of 10:1, and transfer the solution to a syringe In the process, the needle of the syringe is submerged in distilled water which is vigorously stirred at 70°C. The stirring rate of the distilled water is 5000r / min. Under the control of the metering pump, the mixed solution of disulfiram / PLGA is added dropwise to the distilled water. The volume ratio is 1:10. After the dropwise addition was completed, the emulsion was continuously stirred for 5 hours, filtered through a filter membrane with a pore size of 1 micron, and the microspheres on the filter membrane were freeze-dried to obtain PLGA biodegradable microspheres loaded with disulfiram drug. The SEM figure and figure 1 similar.

Embodiment 3

[0021] Dissolve the PLGA biodegradable polymer with an intrinsic viscosity of 0.3dL / g (the molar ratio of LA to GA is 5:1) and disulfiram drug in dichloromethane according to the mass ratio of 20:1, and transfer the solution to the syringe In the process, the needle of the syringe was submerged in distilled water with vigorous stirring at 50°C, and the stirring rate of the distilled water was 3000r / min. Under the control of the metering pump, the mixed solution of disulfiram / PLGA was added dropwise to the distilled water. The volume ratio is 1:50. After the dropwise addition was completed, the emulsion was continuously stirred for 3 hours, then filtered through a filter membrane with a pore size of 1 micron, and the microspheres on the filter membrane were freeze-dried to obtain PLGA biodegradable microspheres loaded with disulfiram drug. The SEM figure and figure 1 similar.

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Abstract

The invention provides a preparation method of PLGA biodegradable microspheres loading a disulfiram drug. The method comprises the following steps of (1) dissolving a polylactic acid-glycolic acid copolymer and the disulfiram drug in dichloromethane, and transferring an obtained solution into a syringe; (2) immersing a needle of the syringe in vigorously stirred water at the temperature higher than the boiling point of the dichloromethane, and then dropwise adding a mixed solution of disulfiram / PLGA into the water; (3) after dropwise addition, stirring an obtained emulsion to obtain microspheres with different particle sizes, grading the microspheres, and taking the micron-sized microspheres for freeze drying to obtain the finished microspheres. The preparation method combines the advantages of an emulsification method and a precipitation method and meanwhile avoids the defects of the emulsification method and the precipitation method. Compared with the emulsification method, the preparation method has the advantage that a surfactant is not required to stabilize emulsion drops, and therefore the influence of the surfactant adsorbed by the surfaces of the microspheres on the drug loading quantity is avoided. Compared with the precipitation method, the preparation method has the advantages that since a water-soluble organic solvent is not adopted, later tedious cleaning steps areavoided, and solvent residues are reduced.

Description

technical field [0001] The invention relates to a preparation method of PLGA biodegradable microspheres, in particular to a preparation method of PLGA biodegradable microspheres loaded with disulfiram medicine, and belongs to the field of biomedical polymer materials. Background technique [0002] Disulfiram (DSF) has been used for more than 60 years as a drug to treat alcohol addiction. Recent studies have found that disulfiram has high specificity for tumor cells, and only kills tumor cells without harming normal cells. DSF can target and kill tumor stem cells, but its mechanism of action on tumor stem cells is still unclear. The disulfide bonds in DSF molecules are easily destroyed by glutathione reducing agents during blood transport, and the half-life in blood is less than 4 minutes, which makes DSF inactivated before it reaches the tumor tissue. Nanoparticles loaded with DSF can slow down its degradation and inactivation. The half-life of DSF in vivo can be prolonged...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34A61K31/145A61P35/00
CPCA61K9/5031A61K31/145A61P35/00
Inventor 何斌陈建华
Owner 苏州岸谷纳米技术有限公司