Heart microneedle patch loaded with TGF (Transforming Growth Factor)-beta inhibitor Galunsertib, and preparation method of heart microneedle patch

A β-inhibitor, TGF-technology, applied in pharmaceutical formulations, tablet delivery, cardiovascular system diseases, etc., can solve problems such as multi-organ dysfunction, reduce toxicity, improve heart function, and prevent heart rupture Effect

Inactive Publication Date: 2021-06-18
NANJING DRUM TOWER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since TGF-β receptors are found in all organs of the body, intravenous administration of TGF-β inhibitors will inevitably lead to impairment of multiple organ functions, so finding ways to target myocardial delivery of TGF-β inhibitors can significantly improve safety

Method used

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  • Heart microneedle patch loaded with TGF (Transforming Growth Factor)-beta inhibitor Galunsertib, and preparation method of heart microneedle patch
  • Heart microneedle patch loaded with TGF (Transforming Growth Factor)-beta inhibitor Galunsertib, and preparation method of heart microneedle patch
  • Heart microneedle patch loaded with TGF (Transforming Growth Factor)-beta inhibitor Galunsertib, and preparation method of heart microneedle patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Preparation of a heart microneedle patch loaded with TGF-β inhibitor Galunsertib suitable for mice

[0036] Step 1, preparation of GelMA pregel loaded with TGF-β inhibitor Galunsertib

[0037] (1) Add 10g of gelatin to 100mL PBS solution at 60°C and stir for 2 hours until completely dissolved, gradually add 8mL of methacrylic anhydride and stir at 60°C until the solution is milky white, and continue to add 5 times (obtained solution) volume of The PBS solution was about 500mL, and the stirring was continued for 1 hour to terminate the reaction until the solution was clear and pale yellow. Place in a dialysis tube (molecular weight cut-off 12kDa) and dialyze in ultrapure water at 45°C for one week to remove residual salt and methacrylic anhydride. After lyophilization for 1 week, the GelMA in the form of porous foam was obtained and stored at -20°C for use;

[0038] (2) 0.3mg Galunsertib (average body weight of mice is 30g), volume concentration of 30% GelMA...

Embodiment 2

[0041] Example 2: Preparation of a heart microneedle patch loaded with TGF-β inhibitor Galunsertib suitable for rats

[0042] Step 1, preparation of GelMA pregel loaded with TGF-β inhibitor Galunsertib

[0043] (1) Add 10g of gelatin to 100mL PBS solution at 60°C and stir for 2 hours until completely dissolved, gradually add 8mL of methacrylic anhydride and stir at 60°C until the solution is milky white, and continue to add 5 times (obtained solution) volume of The PBS solution was about 500mL, and the stirring was continued for 1 hour to terminate the reaction until the solution was clear and pale yellow. Place in a dialysis tube (molecular weight cut-off 12kDa) and dialyze in ultrapure water at 45°C for one week to remove residual salt and methacrylic anhydride. After lyophilization for 1 week, the GelMA in the form of porous foam was obtained and stored at -20°C for use;

[0044] (2) 2.5mg Galunsertib (rat average body weight is 250g), volume concentration is 30% GelMA, vol...

Embodiment 3

[0047] Example 3: Cardiac Microneedle Patch Loaded with TGF-β Inhibitor Galunsertib Treats Fibrosis After Myocardial Infarction in Rats

[0048] The cardiac microneedle patch loaded with the TGF-β inhibitor Galunsertib prepared by the present invention can effectively inhibit cardiac fibrosis and prevent ventricular remodeling, which can be found by HE staining and Sirius red staining of cardiac tissue 4 weeks after myocardial infarction. The area of ​​fibrosis / area of ​​the left ventricle of the rats in the myocardial infarction group was 7.26%-8.09%, and the wall thickness of the left ventricle was 532.0 μm-553.4 μm, while the area of ​​fibrosis / area of ​​the left ventricle of the rats using the cardiac microneedle patch loaded with Galunsertib was 5.29%-6.06%, the left ventricular wall thickness is 1436.0μm-1695.0μm ( Figure 4 ). Cardiac microneedle patches loaded with the TGF-β inhibitor Galunsertib have good mechanical properties and drug release properties. The mechani...

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Abstract

The invention discloses a heart microneedle patch loaded with a TGF-beta inhibitor Galunsertib, and a preparation method of the heart microneedle patch. According to the method, natural polymer hydrogel GelMA and an anti-fibrosis drug TGF-beta inhibitor Galunsertib are premixed according to a certain proportion; a drug-loaded microneedle patch is prepared through ultraviolet light cross-linking curing; the microneedle patch has good mechanical properties and drug release performance and is attached to the surface of an epicardium after myocardial infarction; a microneedle array can absorb interstitial fluid to swell and degrade, target myocardial release drugs and inhibit myocardial fibrosis; furthermore, mechanical support is provided for a heart by forming a membrane structure system with certain strength, so that heart rupture is prevented; and the drug-loaded heart microneedle patch has pharmacological and mechanical treatment effects at the same time, has good prospects for treating excessive cardiac fibrosis after myocardial infarction, preventing ventricular remodeling and improving cardiac functions, and has the advantages of high targeting property and high safety.

Description

technical field [0001] The invention relates to the field of biomedical materials and post-myocardial infarction tissue repair, in particular to a heart microneedle patch loaded with TGF-β inhibitor Galunsertib and a preparation method thereof, and its role in inhibiting myocardial fibrosis and preventing ventricular remodeling , Improve the application of heart function. Background technique [0002] Acute myocardial infarction is a major disease that threatens national health. With the popularization of emergency PCI, the mortality rate in the acute phase of myocardial infarction has decreased significantly. The mortality rate is still greater than 50%. Heart failure after myocardial infarction is mainly due to adverse ventricular remodeling, and the key pathological change is myocardial fibrosis. Active anti-fibrotic therapy is currently the key target for the treatment of heart failure, but unfortunately there is currently no drug that directly inhibits myocardial fibr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/4709A61K47/42A61P9/10
CPCA61K9/7023A61K9/0021A61K31/4709A61K47/42A61P9/10
Inventor 谢峻陈海婷
Owner NANJING DRUM TOWER HOSPITAL
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