Method for preparing microspheres through oil in nano-particle suspension-oil in oil-water in oil

Abstract

The invention discloses a method for preparing microspheres through oil in nano-particle suspension-oil in oil-water in oil (W / O / O / S) and belongs to the technical field of pharmacy. The method includes adding medicine aqueous solution to a polymer organic solution for emulsification to obtain an emulsion, adding the emulsion into a hydrophilic oil phase, stirring, mixing, choosing the nano-particle suspension to serve as a surface active agent ball, finally performing hardening in another large aqueous phase, removing the organic solvent, and collecting the microspheres. The prepared microspheres comprise, by weight, 0.1%-40% of medicines, 9.9%-96% of nano-particles, 90%-3.65% of polymers and 0-30% of pharmaceutic adjuvants. According to the method for preparing the microspheres through oil in nano-particle suspension-oil in oil-water in oil (W / O / O / S), the problem of poor tissue compatibility caused by the fact that the microspheres are prepared through conventional methods of water in oil (W / O), water in oil in water (W / O / W) and solid in oil in oil (S / O / O) is solved, the surfaces of the prepared microspheres are assembled with the nano-particles, the prepared microspheres have effect of enhancing cell adhesion, inflammation and microencapsulation caused by local peracid and a hydrophobic material can be reduced, and the method can be applied to preparation of various medicine sustained-release or controlled-release microspheres and treatment of diseases.

Description

technical field

[0001] The invention relates to microspheres in the technical field of pharmacy and a preparation method thereof, in particular to a method for preparing microspheres by nanoparticle suspension oil-in-oil-water-in-oil (W / O / O / S). Background technique

[0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. Some of the drugs need long-term administration to be cured; others need targeted and other local administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release long-acting dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels, etc. .

[0003] Regarding the preparation method of microsphere preparation...

Examples

Embodiment 1

[0047] Example 1 Small molecule drug microspheres taking doxorubicin as an example

example 1

[0048] Example 1: The preparation of polylactic-glycolic acid (PLGA) microspheres loaded with an aqueous solution of doxorubicin with antibacterial and anticancer effects comprises the following steps:

[0049] (1) Dissolve 20mg of doxorubicin in 0.5ml of water to form an aqueous drug solution;

[0050] (2) Mix the above-mentioned aqueous solution of the drug with a dichloromethane solution of 20% PLGA according to a weight ratio of 1:9 and ultrasonicate for 5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion;

[0051] (3) Add the water-in-oil (W / O) emulsion obtained in step (2) dropwise into 5ml of hydrophilic oil phase ethylene glycol and stir for 5 minutes to form an oil-in-oil-water-in-oil (W / O / O) complex milk;

[0052] (4) the oil-in-oil-water-in-oil (W / O / O) double emulsion that step (3) gained is added dropwise to 50ml weight percent concentration and is in the silver nanoparticle suspension of 10% and stirs 5 minutes to form nanoparticle Sus...

example 2

[0059] Example 2: Preparation of polylactic-glycolic acid (PLGA) microspheres loaded with an aqueous solution of doxorubicin with antibacterial and anticancer effects

[0060] The difference between this example 2 and example 1 is that in step (4), the oil-in-oil-water-in-oil (W / O / O) double emulsion obtained in step (3) is added dropwise to silver nanoparticles containing 10% and 1% (w / w) PVA surfactant in suspension.

technical field

[0001] The invention relates to microspheres in the technical field of pharmacy and a preparation method thereof, in particular to a method for preparing microspheres by nanoparticle suspension oil-in-oil-water-in-oil (W / O / O / S). Background technique

[0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. Some of the drugs need long-term administration to be cured; others need targeted and other local administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release long-acting dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels, etc. .

[0003] Regarding the preparation method of microsphere preparation...

Examples

Embodiment 1

[0047] Example 1 Small molecule drug microspheres taking doxorubicin as an example

example 1

[0048] Example 1: The preparation of polylactic-glycolic acid (PLGA) microspheres loaded with an aqueous solution of doxorubicin with antibacterial and anticancer effects comprises the following steps:

[0049] (1) Dissolve 20mg of doxorubicin in 0.5ml of water to form an aqueous drug solution;

[0050] (2) Mix the above-mentioned aqueous solution of the drug with a dichloromethane solution of 20% PLGA according to a weight ratio of 1:9 and ultrasonicate for 5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion;

[0051] (3) Add the water-in-oil (W / O) emulsion obtained in step (2) dropwise into 5ml of hydrophilic oil phase ethylene glycol and stir for 5 minutes to form an oil-in-oil-water-in-oil (W / O / O) complex milk;

[0052] (4) the oil-in-oil-water-in-oil (W / O / O) double emulsion that step (3) gained is added dropwise to 50ml weight percent concentration and is in the silver nanoparticle suspension of 10% and stirs 5 minutes to form nanoparticle Sus...

example 2

[0059] Example 2: Preparation of polylactic-glycolic acid (PLGA) microspheres loaded with an aqueous solution of doxorubicin with antibacterial and anticancer effects

[0060] The difference between this example 2 and example 1 is that in step (4), the oil-in-oil-water-in-oil (W / O / O) double emulsion obtained in step (3) is added dropwise to silver nanoparticles containing 10% and 1% (w / w) PVA surfactant in suspension.

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