Method for preparing medicine-carrying hydroxyapatite/poly glycolide-co-lactide (PLGA)/chitosan demixing microspheres

A technology for drug hydroxyapatite and hydroxyapatite is applied in the field of preparation of biomedical materials, and can solve the problems of low drug concentration, insufficient therapeutic effect, insufficient effective drug content, irregular spherical structure, etc. release effect, improved drug encapsulation efficiency, and low cost

Active Publication Date: 2012-07-18
广州智园生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

With the continuous development of medicine, pharmacy, biology and other disciplines, new drugs for bone tissue diseases emerge in an endless stream, but systemic administration often results in insufficient effective drug content in the "focus" of bone tissue, while the distribution of drugs in other tissues is poor. It is easy to cause toxic and side effects; in addition, there is also the problem of sustained and stable drug release in the body: whether it is oral administration or intravenous injection, the change of blood drug concentration will appear "peak-valley" phenomenon, and the drug concentration is too low to achieve the therapeutic effect , too high will lead to greater toxic side effects
However, the microspheres prepared by the above-mentioned prior art generally have the problems of fast drug release and irregular sphere structure.

Method used

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  • Method for preparing medicine-carrying hydroxyapatite/poly glycolide-co-lactide (PLGA)/chitosan demixing microspheres
  • Method for preparing medicine-carrying hydroxyapatite/poly glycolide-co-lactide (PLGA)/chitosan demixing microspheres
  • Method for preparing medicine-carrying hydroxyapatite/poly glycolide-co-lactide (PLGA)/chitosan demixing microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) Dissolve 0.2g of isoniazid in 10mL of deionized water, add 1.0g of hydroxyapatite powder, stir at a speed of 200r / min for 15 minutes in the dark to obtain a translucent emulsion, and then freeze-dry for 54 hours get powder;

[0030] (2) Dissolve 0.5g PLGA in 10mL dichloromethane to obtain 5.0% (wt.) PLGA solution; mix 10mL PLGA solution and 1.5g powder evenly to obtain 10mL HA / PLGA blend containing isoniazid;

[0031] (3) Heat 100mL of deionized water to 90°C, dissolve 2g of polyvinyl alcohol 1788 in it, cool down to 40°C, and obtain 2.0% (wt.) polyvinyl alcohol aqueous solution; dissolve 0.4g of chitosan in 10mL of 1 % (wt.) acetic acid aqueous solution to obtain 40% (wt.) chitosan solution; mix 10mL chitosan solution with 100mL polyvinyl alcohol aqueous solution to obtain 110mL chitosan / polyvinyl alcohol solution;

[0032] (4) Add 10mL of the isoniazid-containing hydroxyapatite / PLGA blend obtained in step (2) into the 110mL chitosan / polyvinyl alcohol solution obt...

Embodiment 2

[0036] (1) Dissolve 1.0g of isoniazid in 10mL of deionized water, add 1.0g of hydroxyapatite powder, stir at a speed of 100r / min for 20 minutes in the dark to obtain a translucent emulsion, and then freeze-dry for 72h get powder;

[0037] (2) Dissolve 1.5g PLGA in 10mL dichloromethane to obtain 15% (wt.) PLGA solution; mix 10mL PLGA solution and 2.0g powder evenly to obtain 10mL HA / PLGA blend containing isoniazid;

[0038] (3) Heat 200mL of deionized water to 100°C, dissolve 2g of polyvinyl alcohol 1788 in it, cool down to 45°C, and obtain 1.0% (wt.) polyvinyl alcohol aqueous solution; dissolve 0.6g of chitosan in 10mL of 3 % (wt.) acetic acid aqueous solution to obtain 6.0% (wt.) chitosan solution; mix 10mL chitosan solution with 200mL polyvinyl alcohol aqueous solution to obtain 210mL chitosan / polyvinyl alcohol solution;

[0039] (4) Add 10mL of the isoniazid-containing hydroxyapatite / PLGA blend obtained in step (2) into the 210mL chitosan / polyvinyl alcohol solution obtaine...

Embodiment 3

[0041] (1) Dissolve 0.3g of isoniazid in 10mL of deionized water, add 0.6g of hydroxyapatite powder, stir at a speed of 160r / min for 16 minutes in the dark to obtain a translucent emulsion, and then freeze-dry for 36 hours get powder;

[0042] (2) Dissolve 0.8g PLGA in 10mL dichloromethane to obtain 8.0% (wt.) PLGA solution; mix 10mL PLGA solution and 0.9g powder evenly to obtain 10mL HA / PLGA blend containing isoniazid;

[0043] (3) Heat 150mL deionized water to 95°C, dissolve 2.25g polyvinyl alcohol 1788 in it, cool down to 40°C, and obtain 1.5% (wt.) polyvinyl alcohol aqueous solution; dissolve 0.5g chitosan in 10mL 5.0% (wt.) chitosan solution was obtained in 2% (wt.) acetic acid aqueous solution; 10mL chitosan solution was mixed with 150mL polyvinyl alcohol aqueous solution to obtain 160mL chitosan / polyvinyl alcohol solution;

[0044] (4) Add 10mL of the isoniazid-containing hydroxyapatite / PLGA blend obtained in step (2) into the 160mL chitosan / polyvinyl alcohol solution ...

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Abstract

The invention discloses a method for preparing medicine-carrying hydroxyapatite/poly glycolide-co-lactide (PLGA)/chitosan demixing microspheres. The method comprises the following steps of: dissolving isoniazide in deionized water, adding hydroxyapatite powder, stirring in a dark place, and freeze-drying to obtain powder; mixing PLGA and the powder uniformly to obtain a hydroxyapatite/PLGA commixed solution containing the isoniazide; dissolving chitosan in an acetic acid aqueous solution to obtain a chitosan solution; mixing the chitosan solution and a polyvinyl alcohol aqueous solution to obtain a chitosan/polyvinyl alcohol solution; and pouring the hydroxyapatite/PLGA commixed solution containing the isoniazide into the chitosan/polyvinyl alcohol solution, stirring under vacuum, washingby using water, and freeze-drying to obtain the medicine-carrying hydroxyapatite/PLGA/chitosan demixing microspheres. The prepared medicine-carrying composite microspheres are regular in spherical shapes, uniform in particle size distribution, high in envelop rate of medicines, long in in-vitro medicine release time and small in burst release; and a preparation process is simple, raw materials are readily available, and industrialization is easy to realize.

Description

technical field [0001] The invention belongs to the technical field of preparation of biomedical materials, and relates to the preparation technology of drug-loaded microsphere materials, in particular to a preparation method of drug-loaded hydroxyapatite / PLGA / chitosan layered microspheres. Background technique [0002] Bone tissue is a composite composed of inorganic minerals and organic components. The inorganic mineral phase accounts for about 60-70% of the dry bone weight. The main component is nanocrystals of hydroxyapatite, and the rest of the organic components are mainly collagen fibers. With the continuous development of medicine, pharmacy, biology and other disciplines, new drugs for bone tissue diseases emerge in an endless stream, but systemic administration often results in insufficient effective drug content in the "focus" of bone tissue, while the distribution of drugs in other tissues is poor. It is easy to cause toxic and side effects; in addition, there is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/36
Inventor 魏坤许为康
Owner 广州智园生物科技有限公司
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