Non-spherical polymer particles uniform in particle size as well as preparation method and application of non-spherical polymer particles

A polymer particle, non-spherical technology, applied in the field of polymer materials, can solve the problems of difficulty in obtaining nano-scale particles, non-spherical polymer particles not suitable for hydrophilic drug embedding, and cumbersome process of non-spherical polymer particles.

Active Publication Date: 2016-08-10
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the cumbersome process and difficulty in industrial scale-up in the above-mentioned existing preparation of non-spherical polymer particles, the severe reaction conditions are not conducive to the activity maintenance of active substances, and it is difficult to prepare nano-scale particles with uniform particle size, and the obtained non-spherical Polymer particles are not suitable for the embedding of hydrophilic drugs, and the activity loss of embedding active substances is large. The present invention provides a non-spherical polymer particle with uniform particle size and its preparation method and application

Method used

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  • Non-spherical polymer particles uniform in particle size as well as preparation method and application of non-spherical polymer particles
  • Non-spherical polymer particles uniform in particle size as well as preparation method and application of non-spherical polymer particles
  • Non-spherical polymer particles uniform in particle size as well as preparation method and application of non-spherical polymer particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0150] Example 1: Preparation of non-spherical PLGA particles by direct membrane emulsification

[0151] First, 100mg PLGA (molecular weight is 13kDa, the polymerization ratio of LA:GA is 20:80) is dissolved in 4mL dichloromethane as the oil phase, 0.25mL ultrapure water is added to the oil phase as the internal water phase, and the The primary emulsion was prepared with an ultrasonic breaker with a power of 80W and an ultrasonic time of 30s. Then the colostrum is poured into the direct membrane emulsifier liquid storage bottle, under the nitrogen pressure of 50kPa, the colostrum is hydraulically passed through a microporous ceramic membrane with a membrane aperture of 1.8 μm into 400mL containing 0.1wt.%PVA and 0.08mol / L phosphoric acid In the aqueous solution of disodium hydrogen, magnetically stir at 250rpm for more than 4h to make the solvent dichloromethane volatilize naturally. The solidified solution was centrifuged and washed 4 times with deionized water, and the conc...

Embodiment 2

[0161] Example 2: Preparation of non-spherical PELA particles by rapid membrane emulsification

[0162] First, 300 mg of PELA (molecular weight 40 kDa, mPEG:PLA=1:19) was dissolved in 2 mL of dichloromethane as the oil phase, and 0.1 mL of ultrapure water containing 0.1 wt % Tween80 was added to the oil phase as the internal water phase, and the Under the conditions, the first emulsion was prepared with an ultrasonic breaker, the power was 80W, and the ultrasonic time was 30s. Then pour the primary emulsion into 50mL aqueous solution containing 0.1wt.% Tween80 and 0.001mol / L disodium hydrogen phosphate, prepare the pre-multiplex emulsion by homogenizing at 1000rpm for 30s, then pour it into the liquid storage bottle of the rapid membrane emulsifier, under 10kPa Under nitrogen pressure, the pre-complex emulsion was hydraulically passed through a microporous polytetrafluoroethylene membrane with a membrane pore size of 20 μm, and a uniform emulsion was obtained after repeated pa...

Embodiment 3

[0171] Example 3: Preparation of non-spherical PLA particles by rotating membrane emulsification method

[0172] First, 100mg PLA (molecular weight 70kDa) was dissolved in 3mL of dichloromethane as the oil phase, 0.5mL of ultrapure water containing 5mg / mL octreotide and 0.2wt% Tween 80 was added as the inner water phase into the oil phase, and used under ice-bath conditions. The homogenizer prepares the primary emulsion, the rotation speed is 3000rpm, and the time is 60s. Then the primary emulsion is poured into the rotating membrane emulsifier liquid storage tank, with 500rpm rotating stainless steel microporous membrane (the membrane aperture is 30 μ m), the primary emulsion enters the outer water phase (200mL contains 1wt% Tween80 and 0.08mol / L aqueous solution of disodium hydrogen phosphate) to obtain a double emulsion, solidify overnight with magnetic stirring at 300rpm at room temperature, and make the solvent dichloromethane volatilize naturally. The solidified solutio...

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Abstract

The invention provides non-spherical polymer particles uniform in particle size as well as a preparation method and an application of the non-spherical polymer particles. The non-spherical polymer particles are in the form of ellipsoids, short rods or fibers, and the interiors of the non-spherical polymer particles are of solid, hollow or porous structures; the short diameter of the non-spherical polymer particles ranges from 100nm to 30[micron]m, the long diameter of the non-spherical polymer particles is 1-60[micron]m, the ratio of the long diameter to the short diameter is 2-40, and the particle size distribution coefficient of the particles is less than 20%. The non-spherical polymer particles disclosed by the invention, which are uniform and controllable in particle size, are prepared by taking disodium hydrogen phosphate and / or sodium dihydrogen phosphate as a deformation inducing agent and by taking the influence of such conditions as the concentration of the disodium hydrogen phosphate and / or sodium dihydrogen phosphate, self-properties of a polymer, mass concentration of the polymer in an oil phase, the size of emulsion drops and the like into comprehensive consideration; the non-spherical polymer particles can be applied to various fields such as biological drug delivery, vaccine adjuvants, enzymatic catalysis, bio-separation, human tissue engineering field and the like; and the preparation method is simple to operate, mild in condition and easy for industrial enlarged production.

Description

technical field [0001] The invention belongs to the field of polymer materials, and relates to a non-spherical polymer particle and its preparation method and application, in particular to a non-spherical polymer particle with uniform particle size, its preparation method and application. Background technique [0002] In recent years, with the rapid development of material science and biotechnology, nanoparticle materials with different characteristics are used as drug carriers, vaccine adjuvants, diagnostic reagents and enzyme carriers in many fields such as biomedicine, tissue engineering, biocatalysis and bioseparation. field has been applied. Studies have shown that the physical and chemical properties of the nanoparticle material, such as surface properties, particle size, shape, internal structure and mechanical strength, directly affect and determine the application effect of the nanoparticle material. For example, Gratton SE et al. (The effect of particle design on ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/48A61K47/32A61K47/34A61L27/16A61L27/18A61L27/50C08J3/12
CPCA61K9/5138A61K9/5146A61K38/08A61K38/38A61K39/12A61L27/16A61L27/18A61L27/50C08J3/12C08J2367/04C12N2730/10134C12N2760/16134
Inventor 马光辉吴颉范清泽苗春宇巩方玲
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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