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Nilotinib-loaded heart microneedle patch for targeted myocardial anti-fibrosis treatment, and preparation method of nilotinib-loaded heart microneedle patch

A Nilotinib-loaded, anti-fibrosis technology, applied to improve cardiac function, Nilotinib-loaded cardiac microneedle patch and its preparation, preventing ventricular remodeling, inhibiting myocardial fibrosis, and preventing Effects of cardiac rupture, improvement of cardiac function, and reduction of toxic effects

Pending 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

Unfortunately, ACEI / ARB and β-receptor blockers, which are widely used in clinical practice, can only indirectly or partially inhibit fibrosis.
However, the systemic administration of the anti-fibrotic drug tyrosine kinase inhibitor nilotinib is difficult to avoid multi-organ toxicity, so it has not been promoted in clinical practice.

Method used

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  • Nilotinib-loaded heart microneedle patch for targeted myocardial anti-fibrosis treatment, and preparation method of nilotinib-loaded heart microneedle patch
  • Nilotinib-loaded heart microneedle patch for targeted myocardial anti-fibrosis treatment, and preparation method of nilotinib-loaded heart microneedle patch
  • Nilotinib-loaded heart microneedle patch for targeted myocardial anti-fibrosis treatment, and preparation method of nilotinib-loaded heart microneedle patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of a Nilotinib-loaded microneedle patch suitable for targeting myocardial anti-fibrosis therapy in mice

[0035] Step 1, preparation of GelMA: Add 10 g of type A pigskin gelatin into 100 mL of PBS solution at 60° C., and keep stirring until completely dissolved. Gradually add 8 mL of methacrylic anhydride, stir at 60°C for 2 hours, until the solution is milky white, continue to add 5 times (obtained solution) volume of PBS solution 500 mL to the obtained solution and continue stirring for 1 hour to terminate the reaction. The solution became clear and pale yellow again, and was dialyzed in ultrapure water at 45° C. for one week in a dialysis tube (molecular weight cut-off of 12-14 kDa) to remove residual salt and methacrylic anhydride. After lyophilization for 1 week, GelMA was obtained in the form of a porous foam and stored at -20°C for further use.

[0036] Step 2, preparation of cardiac microneedle patch loaded with nilotinib: 0.1 mg nilotini...

Embodiment 2

[0037] Example 2: Preparation of a drug-loaded microneedle patch suitable for rats loaded with nilotinib for targeted myocardial anti-fibrosis therapy

[0038] Step 1, preparation of GelMA: Add 10 g of type A pigskin gelatin into 100 mL of PBS solution at 60° C., and keep stirring until completely dissolved. Gradually add 8 mL of methacrylic anhydride, stir at 60°C for 2 hours, until the solution is milky white, continue to add 5 times (obtained solution) volume of PBS solution 500 mL to the obtained solution and continue to stir for 2 hours to terminate the reaction. The solution became clear and pale yellow again, and was dialyzed in ultrapure water at 45° C. for one week in a dialysis tube (molecular weight cut-off of 12-14 kDa) to remove residual salt and methacrylic anhydride. After lyophilization for 1 week, GelMA was obtained in the form of a porous foam and stored at -20°C for further use.

[0039]Step 2, preparation of cardiac microneedle patch loaded with nilotinib:...

Embodiment 3

[0040] Example 3: Nilotinib-loaded drug-loaded microneedle patch for targeted myocardial anti-fibrosis therapy in the treatment of post-myocardial infarction fibrosis in rats

[0041] The cardiac microneedle patch loaded with nilotinib for targeted treatment of myocardial fibrosis prepared by the present invention can effectively inhibit cardiac fibrosis and prevent ventricular remodeling, and pathological verification shows that the area of ​​fibrosis / left ventricle of rats in the simple myocardial infarction group The area was 7.26%-8.09%, the left ventricular wall thickness was 532.0μm-553.4μm, and the fibrosis area / left ventricular area of ​​the rats using the cardiac microneedle patch loaded with nilotinib was 4.99%-5.87%, the left The wall thickness is 1536.0μm-1705.0μm( Figure 4 ). The cardiac microneedle patch loaded with nilotinib has good mechanical properties and drug release performance, and the mechanical strength of the microneedle measured by the stress strain...

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Abstract

The invention discloses a nilotinib-loaded heart microneedle patch for targeted myocardial administration and myocardial fibrosis treatment, and a preparation method of the nilotinib-loaded heart microneedle patch. According to the method, GelMA hydrogel with natural biocompatibility and biodegradability is used for loading an anti-fibrosis drug nilotinib; a drug-loaded microneedle patch is prepared through ultraviolet light cross-linking curing; the microneedle patch naturally forms a radian attached to the surface of the heart in the curing process, has good mechanical properties and drug release performance, is attached to the surface of an epicardium, not only can release drugs in a targeted myocardial manner and exert the drug effect at a safe dosage, but also can provide mechanical support for the heart, prevent cardiac rupture, prevent left ventricular remodeling after myocardial infarction, and improve cardiac functions; 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 nilotinib-loaded heart microneedle patch for targeted myocardial anti-fibrosis therapy and a preparation method thereof, and its effect on inhibiting heart disease. Application in muscle fibrosis, prevention of ventricular remodeling, and improvement of cardiac function. Background technique [0002] Acute myocardial infarction is one of the major diseases causing death and disability in my country. With the popularization of emergency intervention, the mortality rate in the acute phase of myocardial infarction has decreased significantly, but the leftover cardiac insufficiency after myocardial infarction seriously affects the quality of life and life expectancy of patients. Heart failure after myocardial infarction manifests pathologically as ventricular remodeling and histologically as cardiac hypertrophy, apoptosis, and myocard...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/506A61K47/42A61P9/10
CPCA61K9/0021A61K9/7023A61K31/506A61K47/42A61P9/10
Inventor 谢峻陈海婷
Owner NANJING DRUM TOWER HOSPITAL
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