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PLGA (Poly Lactic-co-Glycolic Acid)-gelatin composite microspheres carrying genistein and preparation method thereof

A technology of genistein and composite microspheres, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and drug combinations, etc., can solve the problem of uneven liquid force, uneven particle size, and equipment cost. Low-level problems, to avoid spherical irregularity and size increase, the effect of orderly binding of peptide chains

Inactive Publication Date: 2017-05-31
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The PLGA microspheres prepared by the double emulsion method control the particle size by stirring speed and time, but due to the uneven force of the liquid during the emulsification process, the formed particle size is uneven and the drug loading rate is low
The spray drying method not only requires special equipment, but also has poor particle size uniformity and low drug loading rate
The membrane emulsification method obtains better particle uniformity, and the cost of professional equipment and consumables used is relatively high, which is not conducive to industrialization
In the preparation of the hydrophobic flavonoid drug-loaded system, the limitations of the above methods include: the drug-loading rate is too low, and there is an obvious burst release phenomenon during the release process, and the improved solid / oil / water (S / O / W ) emulsified solvent evaporation method can prepare composite microspheres with high drug loading rate, which can effectively overcome the burst release phenomenon, and at the same time, the required equipment cost is low, which is conducive to the industrialization of small and medium-sized enterprises

Method used

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  • PLGA (Poly Lactic-co-Glycolic Acid)-gelatin composite microspheres carrying genistein and preparation method thereof
  • PLGA (Poly Lactic-co-Glycolic Acid)-gelatin composite microspheres carrying genistein and preparation method thereof
  • PLGA (Poly Lactic-co-Glycolic Acid)-gelatin composite microspheres carrying genistein and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1) Take 500mg of type A gelatin (with an isoelectric point of 7-9) and add it to 10mL of deionized water, heat and dissolve to make an aqueous gelatin solution; then add 10mL of acetone to the aqueous gelatin solution to obtain precipitated gelatin;

[0036] 2) Take 240 mg of the precipitated gelatin obtained in step 1), and then redissolve it with 10 mL of deionized water to obtain an aqueous gelatin solution, and use hydrochloric acid and sodium hydroxide to adjust the pH value of the solution to 2.5;

[0037] 3) Add 30 mL of acetone dropwise to the gelatin aqueous solution obtained in step 2) under 500 rpm magnetic stirring to emulsify the system; then immediately add 40 μL of 50% glutaraldehyde aqueous solution to the above system, and continue Stir for 1 hour, then let the emulsion stand at room temperature for 8 hours to solidify the gelatin nanoparticles, and refrigerate at 4°C;

[0038] 4) Take 4mL of the solution prepared in step 3) and centrifuge at 6000rpm, r...

Embodiment 2

[0043] 1) Add 500 mg of type A gelatin to 15 mL of deionized water, heat and dissolve to make an aqueous gelatin solution; then add 15 mL of acetone to the aqueous gelatin solution to obtain precipitated type A gelatin;

[0044] 2) Take 200 mg of the precipitated gelatin obtained in step 1), and then dissolve it again with 15 mL of deionized water to obtain an aqueous gelatin solution, and adjust the pH value of the solution to 3.0;

[0045] 3) Add 40 mL of acetone dropwise to the gelatin aqueous solution obtained in step 2) under magnetic stirring at 750 rpm to emulsify the system; then immediately add 40 μL of 50% glutaraldehyde aqueous solution to the above system, and continue Stir for 1.5 hours, then let the emulsion stand at room temperature for 10 hours to solidify the gelatin nanoparticles, and refrigerate at 4°C;

[0046] 4) Take 2 mL of the solution prepared in step 3) and centrifuge at 6000 rpm, remove the supernatant, wash the precipitate with deionized water 4 tim...

Embodiment 3

[0051] 1) Add 500mg of type A gelatin to 15mL of deionized water, heat and dissolve to make an aqueous gelatin solution; then add 20mL of acetone to the aqueous gelatin solution to obtain precipitated type A gelatin;

[0052] 2) Take 270 mg of the precipitated gelatin obtained in step 1), and then dissolve it again with 20 mL of deionized water to obtain an aqueous gelatin solution, and adjust the pH value of the solution to 3.5;

[0053] 3) Add 40 mL of acetone dropwise to the gelatin aqueous solution obtained in step 2) under 1000 rpm magnetic stirring to emulsify the system; then immediately add 50 μL of glutaraldehyde aqueous solution with a mass fraction of 50% to the above system, and continue Stir for 1 hour, then let the emulsion stand at room temperature for 12 hours to solidify the gelatin nanoparticles, and refrigerate at 4°C;

[0054] 4) Take 2 mL of the solution prepared in step 3) and centrifuge at 7000 rpm, remove the supernatant, wash the precipitate with deioniz...

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Abstract

The invention discloses PLGA (Poly Lactic-co-Glycolic Acid)-gelatin composite microspheres carrying genistein and having a controlled-release effect and a preparation method thereof, and belongs to the technical field of biomedical materials. The method comprises the following steps: preparing gelatin nanoparticles by a two-step desolvation method; adsorbing the genistein in the gelatin nanoparticles; entrapping the gelatin nanoparticles adsorbing drugs in PLGA microspheres by an improved S / O / W method to prepare the PLGA-gelatin composite microspheres carrying the genistein, which have the advantages of high drug loading capacity, capability of overcoming burst release of drugs and uniform particle sizes and are applied in the field of drug delivery. The obtained PLGA-gelatin composite microspheres carrying the genistein are white or faint yellow in appearance, and are 3 to 8mu m in particle sizes, the particles are dispersed, and adhesion is prevented; the highest drug loading amount of the genistein is about 12.1 percent by weight. The gelatin nanoparticles prepared in a preparing process are 60 to 300 nanometers in particle sizes, drugs are released hardly within 24 hours, and the release rate of the genistein is about 80 percent within 20 days along with the degradation of the composite microspheres.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials, and in particular relates to a genistein-loaded PLGA-gelatin composite microsphere with controlled release and a preparation method thereof. Background technique [0002] Poly(lactic-co-glycolic acid) (PLGA) is a degradable polymer material that can be degraded into water and carbon dioxide in the body. It has good biocompatibility and has been approved by the US Food and Drug Administration (FDA) for use in clinical. The exploration of the application of PLGA focuses on the design and preparation of polymeric drug delivery systems, which can protect the drug from degradation and provide a pre-designed way of drug delivery at the target site of drug release to obtain better efficacy while excluding Possibility of overdosing and underdosing. For the traditional route of administration of single-layer polymeric microspheres, there are mainly oral, pulmonary and in vitro injection rou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/42A61K47/34A61K31/352A61P19/10A61P19/08A61P35/00
CPCA61K9/1641A61K9/1658A61K31/352
Inventor 刘红宋效庆魏清陈天杰刘称称路政宽刘秀菊
Owner JILIN UNIV
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