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Adriamycin-containing nanometer medicament microspheres and preparation method thereof

A nano-drug, doxorubicin technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations containing active ingredients, etc., can solve the problem of low encapsulation rate, incomplete release and burst release, local microencapsulation and inflammation To achieve the effect of enhancing cell adhesion, reducing inflammation and microencapsulation, regular particles without adhesion

Inactive Publication Date: 2014-01-15
JINSHAN HOSPITAL FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to address the deficiencies in the prior art and provide a nanoparticle suspension oil-in-oil doxorubicin nano-drug (N / O / N) microspheres to solve the problem of doxorubicin in the prior art. The encapsulation rate of the preparation is not high, incomplete release and burst release, and the hydrophobic surface will cause local microencapsulation and inflammation.

Method used

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  • Adriamycin-containing nanometer medicament microspheres and preparation method thereof
  • Adriamycin-containing nanometer medicament microspheres and preparation method thereof
  • Adriamycin-containing nanometer medicament microspheres and preparation method thereof

Examples

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Effect test

Embodiment 1

[0050] The preparation of polylactic-glycolic acid (PLGA) microspheres loaded with doxorubicin nano-medicine comprises the following steps:

[0051] (1) Dissolve 20 mg of doxorubicin in 0.5 ml of water, then stir with 20 mg of porous silica nanoparticles for 24 hours, so that the doxorubicin is fully adsorbed in the porous silica nanoparticles, and centrifuge to remove the supernatant solution, fully washed 3 times, and then freeze-dried to form adriamycin nano-medicine;

[0052] (2) Mix the above-mentioned doxorubicin nanomedicine with 20% (w / w) PLGA in dichloromethane solution at a weight ratio of 1:9 and sonicate for 5 minutes to form a uniform suspension, that is, doxorubicin in oil Suspension of element nano drug (N / O);

[0053] (3) Add the doxorubicin in oil nano drug (N / O) suspension obtained in step (2) dropwise into 50 ml of silver nanoparticle aqueous suspension with a concentration of 10% (w / w), and stir for 5 Form nanoparticle suspension oil-in-oil-in-oil doxorub...

Embodiment 2

[0061] The preparation of polycaprolactone (PCL) microspheres loaded with doxorubicin nanomedicine comprises the following steps:

[0062] (1) Dissolve 20 mg of doxorubicin in 0.5 ml of water, then stir with 20 mg of porous titanium dioxide nanoparticles for 24 hours, so that the doxorubicin is fully adsorbed in the porous titanium dioxide nanoparticles, centrifuge to remove the supernatant, and then fully Washed 3 times, then freeze-dried to form doxorubicin nanomedicine;

[0063] (2) Mix the above-mentioned doxorubicin nanomedicine with the ethyl acetate solution of PCL with a concentration of 0.5% (w / w) according to the weight ratio of 1:10 and ultrasonicate for 5 minutes to form a uniform suspension, that is, doxorubicin in oil Suspension of element nano drug (N / O);

[0064] (3) Add the doxorubicin in oil nano-drug (N / O) suspension obtained in step (2) dropwise to 50 ml containing 10% (w / w) silver nanoparticles and 1% (w / w) polyethylene In the aqueous suspension of alcoh...

Embodiment 3

[0070] The preparation of polylactic acid (PLA) microspheres loaded with doxorubicin nano-medicine comprises the following steps:

[0071] (1) Dissolve 10 mg doxorubicin and 10 mg dextran into 0.4 ml of water to form a drug aqueous solution, and then transfer the above solution to 3.2 ml of polyethylene glycol (PEG8000) with a concentration of 5% (w / w) Mix well in aqueous solution, then pre-freeze in -80°C refrigerator for 12 hours, then freeze-dry with a freeze dryer, then dissolve PEG with dichloromethane and centrifuge to remove PEG to obtain adriamycin nano-medicine;

[0072] (2) Mix the above-mentioned doxorubicin nanomedicine with PLA acetonitrile solution with a concentration of 30% (w / w) at a weight ratio of 1:8, and ultrasonicate for 1 minute to form a uniform suspension, that is, doxorubicin in oil Suspension of element nano drug (N / O);

[0073] (3) Add the doxorubicin in oil nano drug (N / O) suspension obtained in step (2) dropwise into 40 ml of 20% (w / w) hydroxyapa...

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Abstract

The invention discloses adriamycin-containing nanometer medicament microspheres, which comprises adriamycin, nanoparticles, a polymer and medicinal auxiliary materials. The invention further provides a preparation method of the microspheres. The method comprises the following steps of: preparing adriamycin and the medicinal auxiliary materials into a nanometer medicament; adding the nanometer medicament into a polymer-containing organic solvent mixed solution for emulsifying; adding a nanometer medicament-in-oil mixed suspension into a water mixed suspension containing nanoparticles or containing nanoparticles and a surfactant for emulsifying to obtain an oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil compound emulsion; and curing the obtained compound emulsion, and centrifugally collecting microspheres. An appropriate polymer material and an appropriate microsphere preparation method are selected, the prepared microspheres have high envelop rate, and a layer of self-assembled nanoparticles on the surfaces of the microspheres has the effects of improving cell adhesion and reducing inflammation and microencapsulation caused by local excessive acid and hydrophobic materials. The method disclosed by the invention can be applied to preparation of other medicament slow release or controlled release microspheres.

Description

technical field [0001] The invention relates to nano-medicine microspheres, in particular to nano-medicine microspheres containing doxorubicin and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Doxorubicin is a broad-spectrum anticancer drug that hinders the synthesis of nucleic acids in cancer cells, and has antibacterial and anticancer effects. It has strong anti-cancer activity, but it has high toxicity and side effects in clinical application, and it will cause serious damage to normal tissues and organs. In order to improve its drug effect and reduce its toxic and side effects, people explore its ultrafine particle controlled release and targeting system, and load it on a series of drug carriers such as liposomes, nanoparticles, polymer conjugates and polymer micelles. system. [0003] Chinese patent document CN200510105254.0, published on April 4, 2007, discloses microspheres containing doxorubicin, its use a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/704A61K47/34A61P31/00A61K47/10
Inventor 陈英辉袁伟恩陈碧琴
Owner JINSHAN HOSPITAL FUDAN UNIV
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