A kind of multi-layer slow-release microsphere preparation loaded with VEGF and vancomycin, preparation method and application

A sustained-release microsphere preparation, vancomycin technology, applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the problem of reducing the therapeutic effect of drugs, increasing the complexity of application, Problems such as low drug loading and encapsulation efficiency can achieve the effect of maintaining drug concentration, meeting the needs of double repair, and avoiding excessive side effects

Inactive Publication Date: 2016-09-07
JILIN UNIV
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

Conventional anti-infection is mainly administered orally or intravenously. Although it can achieve a certain effect, the dose of the drug is large, which is likely to cause side effects; moreover, for patients with severe bone tissue infection, the blood flow around the infected bone tissue slows down and decreases, and it is easy to The phenomenon of high concentration in the blood and low concentration in the local bone tissue reduces the local therapeutic effect of the drug
In recent years, some progress has been made in the development of locally applied antibiotics and sustained-release drugs that promote angiogenesis, but they are all sustained-release dosage forms loaded with a single drug, with low drug loading and encapsulation efficiency, and the phenomenon of burst release is relatively serious , and the simultaneous local application of two drugs increases the complexity of the application

Method used

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  • A kind of multi-layer slow-release microsphere preparation loaded with VEGF and vancomycin, preparation method and application
  • A kind of multi-layer slow-release microsphere preparation loaded with VEGF and vancomycin, preparation method and application
  • A kind of multi-layer slow-release microsphere preparation loaded with VEGF and vancomycin, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Take 20mL of deionized aqueous solution of sodium alginate (SA) with a mass volume ratio of 4.0g: 100mL, stir and mix with 0.4mL sterile aqueous solution containing 0.8ug VEGF, and then add 5.0g: 100mL dropwise 30mL CaCl 2 In the solution, stir at a constant speed of 200r / min for 30min to prepare calcium alginate core microspheres;

[0033] (2) The core sphere that step (1) obtains is added to the mass volume ratio that is dissolved with 100mg vancomycin being stirred and is 3.0g:100mL, 30mL chitosan (CS) dilute acetic acid aqueous solution (the volume of dilute acetic acid aqueous solution Fraction is 1%), stirring speed is 500r / min, and stirring time is 10min, makes calcium alginate-chitosan composite drug-loaded monolayer core microsphere;

[0034] (3) Add the microspheres prepared in step (2) to the sodium alginate solution containing 0ug VEGF mass volume ratio of 1.0g: 100mL, 30mL, 500r / min, and stir for 10min to obtain calcium alginate- Chitosan-sodium algin...

Embodiment 2

[0044] (1) Take 20mL of sodium alginate (SA) solution with a mass volume ratio of 1.0g: 100mL, stir and mix with 0.4mL sterile aqueous solution dissolved in 0.8ug VEGF, and then drop in a mass volume ratio of 15.0g: 100mL, 30mL of CaCl 2 In the solution, stir at a constant speed of 200r / min for 30min to prepare calcium alginate core microspheres;

[0045] (2) The core sphere obtained in step (1) is added to the mass volume ratio of 2.0g:100mL, 30mL of chitosan (CS) dilute acetic acid aqueous solution that is dissolved with 100mg vancomycin being stirred, and the stirring speed is 500r / min, the stirring time is 10min, and the calcium alginate-chitosan composite drug-loaded single-layer core microspheres are prepared;

[0046] (3) Add the microspheres prepared in step (2) to the sodium alginate solution containing 0ug VEGF mass volume ratio of 1.0g: 100mL, 30mL, 500r / min, and stir for 10min to obtain calcium alginate- Chitosan-sodium alginate two-layer microspheres;

[0047]...

Embodiment 3

[0052] (1) Take 20mL of sodium alginate (SA) solution with a mass volume ratio of 4.0g: 100mL, stir and mix with 0.4mL sterile aqueous solution dissolved in 0.8ug VEGF, and then drop in a mass volume ratio of 15.0g: 100mL, 30mL of CaCl 2 In the solution, stir at a constant speed of 200r / min for 30min to prepare calcium alginate core microspheres;

[0053] (2) The core sphere obtained in step (1) is added to the mass volume ratio of 1.0g:100mL, 30mL chitosan (CS) dilute acetic acid aqueous solution that is dissolved with 100mg vancomycin being stirred, and the stirring speed is 500r / min, the stirring time is 10min, and the calcium alginate-chitosan composite drug-loaded single-layer core microspheres are prepared;

[0054] (3) Add the microspheres prepared in step (2) to the sodium alginate solution containing 0ug VEGF with a mass volume ratio of 1.0g: 100mL and 30mL, and stir at a speed of 500r / min for 10min to obtain seaweed Calcium acid-chitosan-sodium alginate two-layer ...

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Abstract

A kind of multi-layer topical slow-release microsphere preparation loaded with sodium alginate and chitosan and loaded with VEGF and vancomycin, its preparation method and its application in the preparation of medicines for treating bone defects, bone tissue regeneration and wound healing application. The invention belongs to the technical field of drug slow-release microspheres. In the present invention, except that the preparation of the core sphere is a dripping method, the preparation of the other multilayer microspheres is based on the principle of mutual attraction of positive and negative charges and layer-by-layer self-assembly. Sodium alginate and chitosan are both natural polymer polysaccharides. Chitosan is a polycationic polymer material with a large number of free amino groups in the side chain structure; and sodium alginate is a polyanionic material with a large number of carboxyl groups on the molecular side chain. , the two undergo a complexation reaction through the mutual attraction of positive and negative charges, and are sequentially wrapped to form multi-layer balls of core-shell type multi-layer sustained-release drugs according to the principle of layer-by-layer self-assembly, so that the product of the present invention can simultaneously promote local angiogenesis and improve blood circulation. And the effect of controlling local infection.

Description

technical field [0001] The invention belongs to the technical field of drug slow-release microspheres, in particular to a multi-layer topical slow-release microsphere loaded with sodium alginate and chitosan and loaded with vascular endothelial growth factor (VEGF) and vancomycin (VCM). Ball preparation, preparation method and application thereof in the preparation of medicines for treating bone defect, bone tissue regeneration and wound healing. Background technique [0002] In recent years, with people's increasing attention to quality of life and physical health, as well as road traffic and industrial accidents brought about by the rapid economic development, the clinical diagnosis and treatment of bone defects have become complicated. For large bone defects, the blood supply to the central part of the constructed tissue engineered bone is limited, and nutritional disorders are prone to occur; complex fractures are often complicated by bone defect and infection; at this t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/18A61K47/36A61K9/16A61P19/08A61P17/02A61K38/14
Inventor 刘志辉王博蔚韩舒杨军星王琦王敬龙宋志光郭玉鹏王媛媛姚佳伟
Owner JILIN UNIV
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