Method for preparing PLGA microspheres

A PLGA and microsphere technology, applied in the field of medicine, can solve the problems of increasing the viscosity of the solution, and achieve the effect of easy dispersion and difficult aggregation.

Inactive Publication Date: 2018-02-23
天津双硕医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, the application of polyvinyl alcohol still has certain limitations. For example, it increases the viscosity of the solution,

Method used

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  • Method for preparing PLGA microspheres
  • Method for preparing PLGA microspheres
  • Method for preparing PLGA microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Using hydrophilic nanocellulose as an emulsifier to prepare fat-soluble drug blank drug-loaded PLGA microspheres:

[0053] 1) Dispersing hydrophilic nanocellulose in water, and dissolving a certain amount of sodium chloride or other ionic solutes as the aqueous phase A of the emulsion;

[0054] 2) Dissolving PLGA (molecular weight 20000, lactic acid: glycolic acid molar ratio = 1:1) in the oil phase solvent as the oil phase B of the emulsion;

[0055] 3) Mix the above water phase A and oil phase B, ultrasonically prepare O / W emulsion, remove the water phase and oil phase solvent,

[0056] After washing, filtering, and freeze-drying, the PLGA microspheres can be obtained.

[0057] The test results under each test parameter are listed as follows:

[0058]

[0059] .

[0060] According to experiments 1 to 9, the following conclusions can be drawn:

[0061] The diameter of PLGA microspheres is closely related to the concentration of NaCl in the aqueous ph...

Embodiment 2

[0065] The steps for preparing hydrophilic drug blank drug-loaded PLGA microspheres with hydrophilic nanocellulose are as follows:

[0066] 1) Dissolve PLGA (molecular weight 25000, lactic acid: glycolic acid molar ratio = 1:3) and W / O emulsion stabilizer span60 in the oil phase solvent, which is oil phase A;

[0067] 2) Purified water is used as the water phase B;

[0068] 3) Mix the above oil phase A and water phase B, and ultrasonically prepare W / O type colostrum C;

[0069] 4) Disperse the hydrophilic nanocellulose in water, and dissolve sodium chloride as the aqueous phase D of the emulsion;

[0070] 5) Colostrum C is mixed with water phase D, and ultrasonically prepared to prepare W / O / W double emulsion type emulsion. After removing the water phase and oil phase solvent,

[0071] After washing, filtering, and freeze-drying, the PLGA microspheres can be obtained.

[0072] The test results under each test parameter are listed as follows:

[0073]

[0074] .

[007...

Embodiment 3

[0081] Example 3 Preparation of O / W type PLGA microspheres with risperidone as model drug

[0082] 1) Disperse the hydrophilic nanocellulose in water, and dissolve a certain amount of sodium chloride as the aqueous phase A of the emulsion;

[0083] 2) Dissolving PLGA (molecular weight 25000, lactic acid: glycolic acid molar ratio = 1:1), risperidone raw material in the oil phase solvent dichloromethane as the oil phase B of the emulsion;

[0084] 3) Mix the above water phase A and oil phase B, ultrasonically prepare O / W emulsion, remove the water phase and oil phase solvent, wash,

[0085] PLGA microspheres can be obtained by freeze-drying.

[0086] The test results under each test parameter are listed as follows:

[0087] .

[0088] As can be seen from the above table, the above six groups of test parameters can be prepared by the above method to obtain risperidone PLGA drug-loaded microspheres.

[0089] Its diameter decreases with increasing sodium chloride concentrati...

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Abstract

The invention relates to a method for preparing PLGA microspheres with hydrophilic nano-cellulose as an emulsifier. After the nano-cellulose is adsorbed to the surfaces of the PLGA microspheres, the nano-cellulose stabilizes an oil-water interface as a stabilizer. Meanwhile, because the nano-cellulose has certain zeta electric potentials, the nano-cellulose is easy to scatter and difficult to gather, after an oil phrase and a water phrase are mixed, there is no need to consume a large amount of energy, and the microspheres can be formed through simple ultrasound. Finally, due to the presence of the zeta electric potentials, in the formation process of the microspheres, the thickness of electrified layers of the surfaces of the microspheres can be further adjusted by adjusting the ion strength in the water phase, such as by adding sodium chloride, and the function of adjusting the particle size of the microspheres is achieved at last.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of PLGA microspheres. Background technique [0002] The tiny spherical entities formed by dispersing, adsorbing or dissolving drugs in polymer carrier materials by physical or chemical methods are called drug microspheres. Microspheres are used in drug sustained and controlled release systems to treat many diseases. The treatment of these diseases requires the drug to maintain a certain concentration in the blood, or the drug can be released slowly after reaching specific tissues and organs through targeting. Different types of drug microspheres have different slow and controlled drug release characteristics, and by changing the properties of the microspheres, they can be targeted to specific tissues and organs, so that the concentration of the drug at the target site can be significantly increased, the action time can be prolonged, and the drug ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/519A61K38/22A61K47/38A61K47/34
CPCA61K9/5042A61K9/5031A61K31/519A61K38/22
Inventor 不公告发明人
Owner 天津双硕医药科技有限公司
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