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Fabrication and Evaluation of Spironolactone-Loaded Nanostructured Lipid Carries for Cardiac Tissue Regeneration Publisher



Falak M1 ; Mehdikhani M1 ; Varshosaz J2 ; Hashemibeni B3 ; Ebrahimian Hosseinabadi M1
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Authors Affiliations
  1. 1. Department of Biomedical Engineering, Faculty of Engineering, University of Isfahan, Isfahan, Iran
  2. 2. Department of Pharmaceutics, Novel Drug Delivery Systems Research Centre, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  3. 3. Department of Anatomical Sciences, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Journal of Medical Signals and Sensors Published:2020


Abstract

Background: Spironolactone (SP) is a lipophilic aldosterone receptor antagonist that few studies have reported its effect on cardiac remodeling. In addition, fewer researches have considered its influence on cardiomyocyte viability and potential benefits for myocardial tissue remodeling. Method: In this study, stearic acid (SA) (solid lipid) and oleic acid (OA) (liquid lipid) were utilized to produce nanostructured lipid carries (NLCs) (various ratios of SA to OA and water amount, F1: 80:20 [30 ml water], F2: 80:20 [60 ml water], F3: 70:30 [30 ml water], and F4: 70:30 [60 ml water]) containing SP and their particle size, polydispersity index, zeta potential, entrapment efficiency, and release profile were measured. The purpose of encapsulating SP in NLCs was to provide a sustain release system. Meanwhile, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay with different concentrations of SP-loaded NLCs (SP-NLCs) was conducted to evaluate the cytotoxicity of the NLCs on rat myocardium cells (H9C2). Results: Increase of oil content to 10 wt% reduced the particle size from 486 nm (F1) to 205 nm (F2). Zeta potential of the samples at around −10 mV indicated their agglomeration tendency. After 48 h, SP-NLCs with the concentrations of 5 and 25 μM showed significant improvement in cell viability while the same amount of free SP-induced cytotoxic effect on the cells. SP-NLCs with higher concentration (50 μM) depicted cytotoxic effect on H9C2 cells. Conclusion: It can be concluded that 25 μM SP-NLCs with sustain release profile had a beneficial effect on cardiomyocytes and can be used as a mean to improve cardiac tissue regeneration. © 2020 Journal of Medical Signals & Sensors | Published by Wolters Kluwer - Medknow
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