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A kind of preparation method and application of plga microspheres based on vortex oscillator

A technology of oscillators and microspheres, which is applied in the field of polymer microsphere preparation, can solve problems such as the limitation of emulsification degree and uniformity, the rotor flying off the bottom surface, and the loss of homogenization, etc., and achieves strong scalability, good safety, The effect of short emulsification time

Active Publication Date: 2020-10-09
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the emulsification degree and uniformity of this method relying on the mechanical stirring of the rotor are relatively limited. On the one hand, because the rotor of the magnetic stirrer is not fixed, the speed of the rotor is too fast, which will cause the rotor to fly off the bottom surface and move irregularly, losing the homogenization effect; On the one hand, the rotation of glass beads in the emulsion depends on the driving force generated by the collision of the rotor. If the speed is too fast, the collision force may be too large and the glass beads will be broken.
Due to the above limitations, this method is mainly realized at 1000rpm or below, and it takes 2 hours to fully emulsify, and this method is mainly limited to the preparation of microspheres above 2 μm, and the yield of microspheres with smaller particle sizes is very low

Method used

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  • A kind of preparation method and application of plga microspheres based on vortex oscillator
  • A kind of preparation method and application of plga microspheres based on vortex oscillator
  • A kind of preparation method and application of plga microspheres based on vortex oscillator

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Embodiment 1: Preparation of PLGA microspheres of different particle sizes based on a uniform emulsification method of a vortex oscillator

[0033] (1) Preparation of the oil phase: Weigh 0.6g of PLGA, dissolve it in 10mL of dichloromethane, and prepare a 6% PLGA solution;

[0034] (2) Preparation of polyvinyl alcohol (PVA) aqueous solution: Weigh 2.5g of PVA solid, add it to 100mL of distilled water, heat and stir to fully dissolve, and prepare 2.5% PVA aqueous solution;

[0035] (3) Oscillating emulsification: In a 50mL centrifuge tube, add 10mL 2.5% PVA solution to each bottle, and disperse 1mL 6% PLGA oil phase solution in it, then add 7 glass beads with a diameter of 4-6mm, use the vortex The oscillator vibrates for 5min, 10min, and 20min at 1500 times / min, 3000 times / min, and 3000 rev / min oscillation frequencies respectively (the force of the emulsified solution based on the vortex oscillator is as follows: figure 2 shown);

[0036] (4) The volatilization of or...

Embodiment 2

[0040] Example 2: Preparation and enrichment of PLGA microspheres with uniform particle size of 2-3 μm

[0041] (1) Preparation of the oil phase: Weigh 0.6g of PLGA, dissolve it in 10mL of dichloromethane, and prepare a 6% PLGA solution;

[0042] (2) Preparation of PVA aqueous solution: Weigh 2.5g of PVA solid, add it into 100mL distilled water, heat and stir to fully dissolve, and prepare 2.5% PVA aqueous solution;

[0043] (3) Oscillating emulsification: In a 50mL centrifuge tube, add 10mL 2.5% PVA solution to each bottle, and disperse 1mL 6% PLGA oil phase solution in it, then add 8 glass beads with a diameter of 4-6mm, use the vortex The oscillator oscillates for 10 minutes at an oscillation frequency of 3000 times / min;

[0044] (4) The volatilization of organic solvent: place in fume hood and stir slowly to make dichloromethane organic solvent fully volatilize;

[0045] (5) Collection of PLGA microspheres: PLGA microspheres were collected by centrifugation at 2000 g for 2...

Embodiment 3

[0050] Example 3: Preparation of PLGA drug-loaded microspheres wrapped with rifampicin

[0051] In this example, rifampicin was used as the carrying object to prepare drug-loaded microspheres. The main purpose is to illustrate the application of the method of the present invention in the preparation of PLGA microspheres carrying oil-soluble drugs.

[0052] (1) Preparation of the oil phase: Weigh 0.6g PLGA and 0.05g rifampicin, dissolve them together in 10mL of dichloromethane, and prepare a solution containing 6% PLGA and 0.5% rifampicin;

[0053] (2) Preparation of PVA aqueous solution: Weigh 2.5g of PVA solid, add it into 100mL distilled water, heat and stir to fully dissolve, and prepare 2.5% PVA aqueous solution;

[0054] (3) Oscillating emulsification: In a 50mL centrifuge tube, add 10mL 2.5% PVA solution to each bottle, and disperse 1mL 6% PLGA oil phase solution in it, then add 8 glass beads with a diameter of 4-6mm, use the vortex The oscillator oscillates for 10 minu...

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Abstract

The invention discloses a PLGA microsphere preparation method based on a vortex oscillator and an application thereof in the technical field of preparation of polymer microspheres. The preparation method comprises the following steps: dissolving PLGA into dichloromethane to serve as an oil phase, taking a polyvinyl alcohol solution as an aqueous phase, dispersing the oil phase into the aqueous phase according to a certain ratio, adding glass beads with the diameter of 4-6mm to assist emulsification, and performing shock emulsification on the vortex oscillator; and volatilizing the organic solvent, washing, and performing differential centrifugal enrichment, thereby obtaining the PLGA microspheres with uniform particle size. According to the method disclosed by the invention, the preparation of the PLGA microspheres is based on the vortex oscillator, the glass beads in the container rapidly rotate around a center shaft of the container under the vortex effect and are distributed on different levels of the solution, and mechanical force stressed by different levels of the solution is uniform, so that a uniform emulsifying effect is achieved, and the PLGA microspheres with uniform particle size are obtained. The diameter of the prepared microspheres can be as small as 1-2 microns, and the method is simple and convenient and high in generalizability.

Description

technical field [0001] The invention belongs to the technical field of preparing polymer microspheres, and in particular relates to a method for preparing PLGA microspheres based on a vortex oscillator and an application thereof. Background technique [0002] Polylactic acid hydroxylactic acid (PLGA) has good biocompatibility, is regarded as an excellent medical material, and has been approved by the US Food and Drug Administration (FDA) for clinical use. PLGA microsphere carrier is widely used in the field of biomedicine, such as drug delivery, antibody preparation, vaccine adjuvant, etc. Based on this, the research on PLGA microspheres has always been one of the hot spots in the field of biological carrier research. [0003] The preparation process of PLGA microspheres is an important aspect that researchers in this field pay attention to. At present, the solvent emulsification and evaporation method is one of the most classic and commonly used methods for the preparatio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/34A61K31/496
CPCA61K9/5031A61K9/5089A61K31/496
Inventor 刘志强杨锡琴段翠密冯晓燕张贺秋李江雪张旭辉阙海萍
Owner ACADEMY OF MILITARY MEDICAL SCI
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