Method for preparing microspheres through oil in nano-particle suspension-oil in oil and sustained-release microspheres

A nanoparticle and suspension technology, used in bulk delivery, drug combination, antitumor drugs, etc., can solve the problem that microspheres cannot overcome the encapsulation rate of local microencapsulation and inflammation, and can not overcome the encapsulation rate of local microencapsulation. It can reduce inflammation and microencapsulation, and enhance cell adhesion.

Inactive Publication Date: 2013-01-30
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to provide a nanoparticle suspension oil-in-oil method for preparing microspheres, so as to solve the problem that the microspheres in the prior art cannot overcome the local microcapsules caused by low encapsulation efficiency and hydrophobic surface. Technical Issues of Chemistry and Inflammation
[0004] Another object of the present invention is to provide a sustained-release microsphere to solve the technical problems that the microspheres in the prior art cannot overcome the low encapsulation rate and the local microencapsulation and inflammation caused by the hydrophobic surface

Method used

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  • Method for preparing microspheres through oil in nano-particle suspension-oil in oil and sustained-release microspheres
  • Method for preparing microspheres through oil in nano-particle suspension-oil in oil and sustained-release microspheres
  • Method for preparing microspheres through oil in nano-particle suspension-oil in oil and sustained-release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1 Preparation of doxorubicin polylactic-glycolic acid (PLGA) microspheres with antibacterial and anticancer effects

[0056] (1) Dissolve 20mg of doxorubicin in 0.5ml of dimethyl sulfoxide (DMSO);

[0057] (2) Sonicate the above drug solution and 0.1% PLGA dichloromethane solution at a weight ratio of 1:9 for 1-5 minutes to form a uniform oil phase;

[0058] (3) Add the oil phase of step (2) dropwise to mineral oil (4-10ml), stir, vortex or sonicate for 0.1-5 minutes to form a double emulsion (O / O) emulsion;

[0059] and Stir, vortex or sonicate for 0.1-5 minutes to form double emulsion (O / O / S) emulsion;

[0060] (5) Add the double emulsion emulsion in step (4) dropwise to 200-500ml cottonseed oil and solidify for 2-3 hours;

[0061] (6) The microspheres are collected by centrifugation, washed with ether for 3-5 times, and then vacuum-dried to obtain the microspheres.

[0062] The scanning electron microscope image of the prepared microspheres is shown in f...

Embodiment 2

[0063] Example 2 Preparation of Exenatide Polylactic-Glycolic Acid (PLGA) Microspheres

[0064] (1) 20mg of exenatide and 10mg of polyethylene glycol (PEG molecular weight 6000) dissolved in 0.5ml of dimethylsulfoxide (DMSO);

[0065] (2) Sonicate the above drug solution and 10% PLGA in dichloromethane solution at a weight ratio of 1:9 for 1-5 minutes to form a uniform oil phase;

[0066] (3) Add the oil phase of step (2) dropwise to mineral oil (4-10ml), stir, vortex or sonicate for 0.1-5 minutes to form a double emulsion (O / O) emulsion;

[0067] (4) Add the emulsion of step (3) dropwise to the suspension of hydroxyapatite nanoparticles with a concentration of 60% by weight or the suspension of nanoparticles and PVA surfactant with a concentration of 30% by weight And stir, vortex or ultrasonic for 0.1-5 minutes to form double emulsion (O / O / S) emulsion;

[0068] (5) Add the double emulsion emulsion in step (4) dropwise to 200-500ml cottonseed oil and solidify for 2-3 hours;...

Embodiment 3

[0071] Example 3 Preparation of octreotide polylactic-glycolic acid (PLGA) microspheres

[0072] (1) 20mg octreotide dissolved in 0.5ml dimethyl sulfoxide (DMSO) solution;

[0073] (2) Sonicate the above drug solution and PLGA dichloromethane solution with a percentage concentration of 20% in a weight ratio of 1:9 for 1-5 minutes to form a uniform oil phase;

[0074] (3) Add the oil phase of step (2) to mineral oil (4-10ml) dropwise and stir, vortex or sonicate for 0.1-5 minutes to form a double emulsion (O / O) emulsion;

[0075] (4) Add the double emulsion emulsion of step (3) dropwise to the suspension of hydroxyapatite nanoparticles with a concentration of 80% by weight or the suspension of nanoparticles and PVA surfactant with a concentration of 50% by weight Mix in the solution and stir, vortex or sonicate for 0.1-5 minutes to form double emulsion (O / O / S) emulsion;

[0076] (5) Add the double emulsion of step (4) dropwise to 200-500ml cottonseed oil and solidify for 2-3 ...

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Abstract

The invention provides a method for preparing microspheres through oil in nano-particle suspension-oil in oil. The method includes that step one, embedded medical ingredients are prepared to a medicine oil solution; step two, the medicine oil solution is added into a polymer organic solution, namely the medicine oil solution is added into an oil phase, and a suspension is formed through uniformly mixing; step three, the suspension prepared in the step two is dropwise added into mineral oil, and a multiple emulsion is formed through stirring, whirling or ultrasound; step four, the multiple emulsion prepared in the step three is dropwise added into a suspension containing the nano-particles, and the microspheres are formed through stirring, whirling or ultrasound; step five, the microspheres prepared in the step four are dispersed into cottonseed oil for curing; and step six, the microspheres are collected in a centrifuged mode, and drying is performed to obtain the microspheres with surfaces self assembled with the nano-particles. Compared with methods for preparing microspheres in prior art, the method for preparing the microspheres through oil in nano-particle suspension-oil in oil has the advantages that a layer of nano-particles is assembled on the surfaces of the microspheres, and the microspheres with surfaces assembled with the nano-particles have effects of enhancing cell adhesion and reducing inflammation and microencapsulation caused by local peracid and a hydrophobic material.

Description

technical field [0001] The invention relates to a method for preparing microspheres, in particular to a method for preparing microspheres by oil-in-oil-in-oil (O / O / S) nanoparticle suspension and sustained-release microspheres. Background technique [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. Among them, some drugs require long-term administration to be cured; others require 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 in PLA (polylactic acid) dosage form; for the treatment of some tumors, some drugs need to be targeted to the lesion, such as embolization microsphere preparations targeting tumor blood vessels Wait. After searching the prior art documents, it was found that "Double walled PLA / PLGA micros...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61P35/00
Inventor 袁伟恩金拓吴飞胡振华马柳青徐建雄
Owner SHANGHAI JIAO TONG UNIV
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