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Preparation method of biodegradable supermolecule polylactic acid microspheres

A technology of polylactic acid microspheres and supramolecules, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve problems such as difficult removal and restrictions on the wide application of biodegradable particles. Achieve the effects of avoiding the use of emulsifiers, good biocompatibility, and high implementability

Active Publication Date: 2017-05-24
元嘉生物科技(衢州)有限公司
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  • Abstract
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AI Technical Summary

Problems solved by technology

However, the use of emulsifiers makes it difficult to completely remove from the microspheres, thus limiting the wide application of biodegradable particles

Method used

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  • Preparation method of biodegradable supermolecule polylactic acid microspheres
  • Preparation method of biodegradable supermolecule polylactic acid microspheres
  • Preparation method of biodegradable supermolecule polylactic acid microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～9

[0047] In Examples 1-9, linear or three-arm star-shaped PLLA and PDLA functionalized with UPy end groups are dissolved in good solvents such as dichloromethane, chloroform, tetrahydrofuran, etc. in a certain mass ratio, so that the concentration of the polymer solution is 1 mg / mL. After stirring and mixing for 2 hours, add dropwise into poor solvents such as ethanol and methanol, and stir until the volume fraction of poor solvents is 20% to 90%, and drop it off after 4 hours. Then after stirring for 24 h, it was centrifuged and washed to collect the solid precipitate. After the solid precipitate was vacuum-dried at 60° C. for 6 h, biodegradable supramolecular PLA microspheres were obtained.

[0048] In Comparative Examples 1 and 2, the same method was used to prepare PLA particles using hydroxyl end-functionalized linear or three-arm star-shaped PLLA, PDLA or a mixture of the two as raw materials. The proportion of PLLA and PDLA in Examples 1-9 and Comparative Examples 1-2,...

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Abstract

The invention relates to the field of biodegradable macromolecule, and aims at providing a preparation method of biodegradable supermolecule polylactic acid microspheres. The method comprises the steps that 2-carbamido-4-[1H]-pyrimidone (UPy) end group modified polylactic acid is dissolved in good solvent, poor solvent is dropwise added under the stirring condition; after stirring continues to be conducted, centrifugal washing is conducted, and solid precipitates are collected; vacuum drying is conducted, and then the biodegradable supermolecule polylactic acid microspheres are obtained. Accordingly, the preparation method is simple and easy to implement, and the feasibility of implementation is high. The morphology of polymer microspheres is regulated through a method of combining liquid-liquid separation and polymer crystallization; meanwhile, the structure and performance are regulated, and the application range is extended. Raw materials of prepared materials all come from biomass renewable resources, can be completely degraded after use, are green and environmentally friendly and have good biocompatibility. Chemical-loading particles are prepared through a chemical and polymer coprecipitation method, use of emulsifier can be effectively avoided, and then the polymer nanoparticles or microspheres have a wider application prospect.

Description

technical field [0001] The invention relates to the field of biodegradable polymers, in particular to a preparation method of biodegradable supramolecular polylactic acid microspheres. Background technique [0002] As a drug carrier material, nanoparticles or microspheres have been widely studied and applied in the field of controlled release of drugs. Microsphere carriers can overcome some disadvantages of existing pharmaceutical preparations, use their own small particle size and high dispersion of drugs, improve the water solubility and dissolution rate of insoluble drugs, and increase the bioavailability of drugs. [0003] The traditional methods of preparing polymer micro-nanoparticles or microspheres include spray drying, emulsion solvent volatilization and coagulation methods. These methods have obvious deficiencies, such as the use of toxic solvents or additives, which are difficult to completely remove from the microspheres, affecting The biocompatibility of micros...

Claims

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Application Information

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IPC IPC(8): C08J3/14C08L67/04A61K47/69A61K31/496A61K47/59
CPCA61K31/496C08J3/14C08J2367/04C08L67/04C08L2201/06C08L2203/02C08L2205/025
Inventor 潘鹏举常晓华包建娜单国荣包永忠
Owner 元嘉生物科技(衢州)有限公司
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