Method of regulating microsphere drug-load rate by treating calcium alginate microspheres with sodium chloride solution

A technology of sodium chloride solution and calcium alginate is applied in pharmaceutical formulations, medical preparations of non-active ingredients, and bulk delivery, etc., which can solve the problem that the drug loading of microspheres is not easy to control, and the drug loading and embedding rate are inconsistent. It can achieve the effect of good application prospect, high encapsulation rate and wide source of raw materials.

Inactive Publication Date: 2012-08-15
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is difficult to obtain microspheres with a particle size of less than 50 μm by the electrostatic generation method, while the microspheres obtained by the stirring emulsification method have a wider particle size distribution, and the method of mixing

Method used

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  • Method of regulating microsphere drug-load rate by treating calcium alginate microspheres with sodium chloride solution
  • Method of regulating microsphere drug-load rate by treating calcium alginate microspheres with sodium chloride solution
  • Method of regulating microsphere drug-load rate by treating calcium alginate microspheres with sodium chloride solution

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 1) Prepare 10mL of 2% sodium alginate solution as the water phase, prepare 120mL of isooctane containing 3% emulsifier (Span 85: Tween 85=9:1) as the oil phase, pour the water phase and the oil phase Into a membrane emulsifier containing a cylindrical SPG membrane, the water phase and the oil phase are respectively on the outside and inside of the cylindrical SPG membrane, and pressure is applied with nitrogen gas under stirring to make the water phase squeeze through the SPG membrane and enter the oil phase to obtain an oil-in-oil phase. Water emulsion, add 20mL salt solution containing 5% calcium chloride and 20% sodium chloride to the water-in-oil emulsion, stir for 0.5h, then add 50mL isopropanol and continue stirring for 1h, separate liquid, centrifuge and wash to obtain alginic acid Calcium microspheres, the scanning electron micrographs of which are shown in figure 1 a, b, light microscope photos see figure 1 c;

[0022] 2) Add 2 mg of calcium alginate microsph...

Embodiment 2

[0025] Step is the same as embodiment 1, but adopting massfraction in step 2) is the sodium chloride solution of 0.9%, and its optical microscope photo is shown in figure 2 b, SEM photo after drying see image 3 b, The light microscope and laser confocal photos of the microspheres loaded with doxorubicin are shown in Figure 6 b.

Embodiment 3

[0027] Step is the same as embodiment 1, but adopting massfraction in step 2) is the sodium chloride solution of 1.8%, and its optical microscope photo is shown in figure 2 c, SEM pictures after drying are shown in image 3 c, The light micrograph of the microspheres loaded with doxorubicin is shown in Figure 6 c.

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Abstract

The invention discloses a method of regulating microsphere drug-load rate by treating calcium alginate microspheres with sodium chloride solution. The method comprises the following steps: preparing calcium alginate microspheres with uniform grain diameter by adopting a membrane emulsification-gelatinization method; soaking the microspheres with sodium chloride solutions with different concentrations to substitute sodium ions for part of calcium ions in the calcium alginate microspheres, and then cleaning with ultrapure water; and soaking the treated microspheres into medicinal solution with positive charges, and loading drugs by virtue of static effect to obtain the calcium alginate microspheres with different drug-load rates finally. The preparation method is easy and controllable, the material sources are wide, the drug-load rate of microspheres can be conveniently adjusted, and the method has the advantage of excellent application prospect.

Description

technical field [0001] The invention relates to a method for preparing microspheres and regulating their drug loading. Especially the method of treating the microspheres with different concentrations of sodium chloride solutions to regulate the drug loading of the microspheres. Background technique [0002] Polymer microspheres refer to a class of polymer materials with micron-scale diameters and spherical shapes. In recent years, polymer microspheres have been widely studied due to their potential huge application value in the fields of medicine, biochemistry, and electronic information. At present, the main preparation methods of microspheres are spray drying method, extrusion method, interfacial and in-situ polymerization method, phase separation method and multiple phase emulsion method. These methods have large yields, but the particle size distribution of the prepared microspheres is mostly very wide, which limits the application in some fields. Membrane emulsificat...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K9/16
Inventor 高长有仝维鋆宋亦超
Owner ZHEJIANG UNIV
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