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A locally deliverable nano-preparation for inhibiting inflammation of radiofrequency ablation cardiac tissue, its preparation method and application

A technology of nano-preparation and radiofrequency ablation, which is applied in the field of medicine to achieve the effect of inhibiting inflammation and avoiding large side effects

Active Publication Date: 2022-05-03
胥玲玲
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fat-soluble glucocorticoids can better enter local tissues to exert their effects, but because they are insoluble in water, they can only be administered by external use, atomization inhalation, etc.

Method used

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  • A locally deliverable nano-preparation for inhibiting inflammation of radiofrequency ablation cardiac tissue, its preparation method and application
  • A locally deliverable nano-preparation for inhibiting inflammation of radiofrequency ablation cardiac tissue, its preparation method and application
  • A locally deliverable nano-preparation for inhibiting inflammation of radiofrequency ablation cardiac tissue, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: the preparation method of PLGA-BUD-CS nanoparticle

[0051] figure 1 A flow chart for the preparation of PLGA-BUD nanoparticles is provided. Specifically, the preparation method of PLGA-BUD-CS nanoparticles is as follows: dissolve 1.5mg budesonide (BUD) and 10mg PLGA in 0.5mL chloroform, add 8mL Stir in 2% polyvinyl alcohol aqueous solution for 30 minutes, and then use ultrasonic crushing, 150w ultrasonic for 5 minutes to form a uniform emulsion. Chloroform was removed by rotary evaporation at 40°C to obtain a suspension. Centrifuge at 17800 g for 30 min to remove free drug in the supernatant to obtain a BUD-PLGA nanoparticle solution. Weigh the prepared nanoparticles and disperse them in MES buffer (0.1mmol / L, pH5.5) to a final concentration of 0.5mg / mL, add ethyldimethylaminopropylcarbodiimide hydrochloride (EDC ) (0.2mg / mL) and hydroxysuccinimide (NHS) (0.4mg / mL) activation reaction for 3 hours. Use acetic acid solution with pH=4 to dissolve chitosa...

Embodiment 2

[0054] Embodiment 2: budesonide liposome construction

[0055] Put DPPC, PEG-DSPE and total cholesterol into a 50mL round bottom flask at a mass ratio of 1.85:0.15:1, add 10mL of absolute ethanol, heat in a water bath to 50°C until completely dissolved, and remove the ethanol by rotary evaporation to obtain a dry liposome membrane , followed by drying in a nitrogen stream for 30 min. 100mg / mL budesonide phosphate aqueous solution was heated to 50°C and then added to the liposome membrane at 50°C for 5-10 minutes and rotated for hydration to obtain liposomes with uneven particle size, followed by five injections of polycarbonate with a pore size of 200nm Ester liposome extruder, inject the polycarbonate liposome extruder of 100nm aperture repeatedly five times again, obtain the liposome particle of uniform particle size. Free drug was removed by dialysis of the solution against MWCO 30,000 Da dialysis bags at 4-8°C for 48 hours. Finally, budesonide liposome solution is obtain...

Embodiment 3

[0056] Example 3: Construction of Budesonide Albumin Nanoparticles

[0057] With chloroform and ethanol mixed solvent (11:1, v / v) as solvent, add 1% w / v bovine serum albumin (BSA) solution in different molar ratio (BUD:BSA=1:1), BSA solution adopts Presaturated with 1% chloroform. Then the system was sonicated for 5 min (interval 1 s), and then transferred to a rotary evaporator at 30° C. to remove chloroform to prepare BUD-BSA nanoparticles.

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Abstract

The invention belongs to the field of nano-pharmaceutical preparations, and in particular relates to a locally-deliverable nano-preparation for inhibiting radiofrequency ablation of heart tissue inflammation, a preparation method and application thereof. The nano-preparation includes a nano-carrier and a fat-soluble glucocorticoid contained in the nano-carrier, and the fat-soluble glucocorticoid is included in the nano-preparation in a therapeutically effective amount, so that the nano-preparation can suppress radio frequency Ablation of inflamed heart tissue. The PLGA-BUD-CS nanoparticles provided by the preferred example of the present invention can exist stably in water, form a uniform suspension, and can be locally delivered to the inner wall of the heart cavity through a radiofrequency ablation catheter, and the fat solubility of budesonide ensures sufficient drug entry Local tissues, play an anti-inflammatory effect, and PLGA makes the drug stay in the tissue for a longer time.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a locally deliverable nano-preparation for inhibiting inflammation of radiofrequency ablated cardiac tissue, a preparation method and application thereof. Background technique [0002] Atrial fibrillation can significantly increase the risk of ischemic stroke and arterial embolism, and ablation for symptomatic paroxysmal atrial fibrillation has entered category I indications. For paroxysmal supraventricular tachycardia, ventricular or atrial premature beats and other types of arrhythmia, radiofrequency ablation is more accurate. During radiofrequency ablation, the effective release of radiofrequency energy and the size of the damaged area are crucial to the success of the operation. Catheter stability, contact pressure, energy output, temperature, and ablation time are important factors that determine the extent of damage and whether it is transmural. [0003] The infiltration of inflam...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/127A61K9/52A61K31/573A61K31/58A61K45/00A61K47/34A61K47/36A61M31/00A61P5/44A61P9/00
CPCA61K9/5146A61K9/5161A61K9/1271A61K9/1075A61K47/34A61K31/58A61K31/573A61K45/00A61P9/00A61P5/44A61M31/00
Inventor 刘晔胥玲玲刘小青杨新春李舟
Owner 胥玲玲
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