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Preparation method of biodegradable polymer-encapsulated water-soluble molecular microspheres

A high-molecular, water-soluble technology, applied in the direction of powder transportation, block transportation, etc., can solve the problem of low encapsulation rate of water-soluble molecules

Inactive Publication Date: 2014-10-08
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to overcome the problem of low encapsulation efficiency of water-soluble molecules in the double emulsion method, and provide a preparation method for biodegradable polymer-encapsulated water-soluble molecule microspheres. The specific technical scheme is as follows

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 0.5 g of polylactic acid-glycolic acid copolymer with a molecular weight of 17800 into 5 mL of dichloromethane and shake to dissolve to obtain a degradable polymer oil solution. Take 500 μl of a prepared 100 mg / mL aqueous solution of ofloxacin (containing 0.1% methylcellulose, g / mL), add 0.1 g of mesoporous silicon with a particle size of 25 nm and shake well to obtain the inner aqueous phase. Add the internal water phase into the degradable polymer oil solution, and disperse at 7200rpm for 10 minutes to obtain colostrum. Dissolve 30 mg of methylcellulose in 50 mL of water (0.06%, g / mL), add colostrum and disperse at 7200 rpm for 10 minutes to obtain double emulsion. Add the double emulsion to 400mL water for precipitation at 35°C for 4h. After the microspheres were obtained by suction filtration, they were dried at 40°C for 10 hours. Compared with the microspheres without mesoporous silicon, the encapsulation efficiency of ofloxacin increased from 25% to 72%.

Embodiment 2

[0027] Add 0.4 gram of polylactic acid with a molecular weight of 23000 into 5 mL of dichloromethane and shake to dissolve to obtain a degradable polymer oil solution. Take 600μl prepared 50mg / mL TGF-β 3 Aqueous solution (containing 1% polyethylene glycol, g / mL), adding 0.1 mg of mesoporous silicon with a particle size of 30 nm and shaking to obtain the inner aqueous phase. Add the internal water phase into the degradable polymer oil solution, and disperse at 9000rpm for 25 minutes to obtain colostrum. Dissolve 300 mg of polyethylene glycol in 30 mL of water (1%, g / mL), add colostrum and disperse at 10,000 rpm for 30 minutes to obtain double emulsion. Add the double emulsion to 400mL water for precipitation at 35°C for 4h. After the microspheres were obtained by suction filtration, they were dried at 40°C for 10 h. TGF-β 3 Encapsulation increased from 15% to 42%.

Embodiment 3

[0029] 0.6 gram of polycaprolactone with a molecular weight of 38000 was added into 4 mL of dichloromethane and shaken to dissolve to obtain a degradable polymer oil solution. Take 400 μl of prepared 10 mg / mL vitamin C aqueous solution, add 50 mg of mesoporous hydroxyapatite with a particle size of 25 nm and shake well to obtain the inner water phase. Add the internal water phase into the degradable polymer oil solution, and disperse at 10,000 rpm for 50 minutes to obtain colostrum. Dissolve 30 mg of methylcellulose in 40 mL of water (0.075%, g / mL), add colostrum and disperse at 12000 rpm for 20 minutes to obtain double emulsion. The double emulsion was added to 400mL of water for precipitation at 35°C for 3h. After the microspheres were obtained by suction filtration, they were dried at 40°C for 10 h. Vitamin C encapsulation increased from 15% to 45%.

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Abstract

The invention relates to a preparation method of water-soluble molecular microspheres encapsulated by biodegradable high molecules. According to the method, a mesoporous nano material is firstly added into a water solution containing water-soluble molecules so as to form an inner water phase, and initial emulsion is formed by high-speed dispersion after the inner water phase is mixed with a degradable high-molecular organic solution. Then, compound emulsion is formed by high-speed dispersion after the initial emulsion is mixed with a water solution containing a surfactant, and solidified degradable high-molecular microspheres are obtained by removing an organic solvent. The microspheres which can be used for releasing hydrophilic molecules are obtained after being washed, filtered and dried. Because the mesoporous nano material is added in the inner water phase, the encapsulation rate of the water-soluble molecules in hydrophobic degradable high molecules is greatly enhanced, and the period of slow release is also increased.

Description

technical field [0001] The invention relates to the technical field of preparation of biodegradable microspheres, in particular to a method for preparing microspheres in which biodegradable polymers encapsulate water-soluble molecules. Background technique [0002] Microspheres refer to tiny spherical entities formed by dissolving or dispersing small molecules in a polymer material matrix. The common particle size is 1-500 μm, which belongs to matrix-type skeleton particles. Microspheres based on degradable polymers have received increasing attention and applications due to their superiority in long-acting and sustained release. In the past ten years, it has been widely used in small molecule sustained / controlled release systems to transport various small molecules. The small molecules currently involved include hormones, drugs, vitamins, proteins, short peptides, etc. A variety of small molecule microsphere formulations have been marketed and sold today. [0003] The prep...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/16A61K47/34A61K47/38
Inventor 吴刚陈龙邓春林
Owner SOUTH CHINA UNIV OF TECH
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