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<p>Worldwide, healthcare systems are increasingly overwhelmed by the significant burden of coronary artery disease (CAD). The risk of developing CAD is heightened in individuals with diabetes mellitus (DM). Isoxsuprine (IXP) is a potent beta receptor agonist and α1-adrenoreceptor antagonist. IXP exhibits various pharmacological effects, such as enhancing arterial blood flow, promoting glucose uptake, and providing antioxidant benefits. However, the limited utility of IXP is attributed to its low bioavailability, hepatic metabolism, and short half-life. The primary objectives of this study were to design a nasal spray containing IXP-loaded novasomes (ILN) for attenuating DM-associated CAD. The focus was on enhancing the efficacy, bioavailability, and sustained release behavior of IXP. Various ILNs have been optimized using Design Expert software. The optimal ILN formulation has been characterized in terms of zeta potential, particle size, release, permeation, and stability. Additionally, the bioavailability and efficacy of the nasal ILN formulation have been studied in albino Wistar rats. The optimal ILN formulation exhibited a significant (Student’s <i>t</i>-test, <i>p</i>-value &lt; 0.0001) 3.53-fold increase in the sustained release behavior of IXP, a 3.87-fold increase in its permeation, and a 3.72-fold enhancement in its bioavailability. Additionally, the nasal ILN formulation demonstrated significantly (one-way ANOVA, <i>p</i>-value &lt; 0.0001) greater cardioprotective and antioxidant activities compared to both oral and nasal IXP solutions. These results were further validated by the histopathological examination. The results indicate that the nasal ILN spray demonstrates preclinical efficacy in a rat model, suggesting its potential as a candidate for attenuating DM-associated CAD.</p>

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Design and optimization of isoxsuprine-loaded novasomes for the attenuation of coronary artery disease in rats

  • 期刊论文

  • 发表日期：

    2026年6月26日

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  • Amr Gamal Fouad,
  • Amany Belal,
  • Suhaib Mohammadmustafa Bukhari,
  • Nisreen Khalid Aref Albezrah,
  • Saeed Saad A. Alghamdi,
  • Atheer Talal Hamadi Aljahdali,
  • Rasha Hallal Alziyadi,
  • Fatma I. Abo El-Ela

摘要

Worldwide, healthcare systems are increasingly overwhelmed by the significant burden of coronary artery disease (CAD). The risk of developing CAD is heightened in individuals with diabetes mellitus (DM). Isoxsuprine (IXP) is a potent beta receptor agonist and α1-adrenoreceptor antagonist. IXP exhibits various pharmacological effects, such as enhancing arterial blood flow, promoting glucose uptake, and providing antioxidant benefits. However, the limited utility of IXP is attributed to its low bioavailability, hepatic metabolism, and short half-life. The primary objectives of this study were to design a nasal spray containing IXP-loaded novasomes (ILN) for attenuating DM-associated CAD. The focus was on enhancing the efficacy, bioavailability, and sustained release behavior of IXP. Various ILNs have been optimized using Design Expert software. The optimal ILN formulation has been characterized in terms of zeta potential, particle size, release, permeation, and stability. Additionally, the bioavailability and efficacy of the nasal ILN formulation have been studied in albino Wistar rats. The optimal ILN formulation exhibited a significant (Student’s t-test, p-value < 0.0001) 3.53-fold increase in the sustained release behavior of IXP, a 3.87-fold increase in its permeation, and a 3.72-fold enhancement in its bioavailability. Additionally, the nasal ILN formulation demonstrated significantly (one-way ANOVA, p-value < 0.0001) greater cardioprotective and antioxidant activities compared to both oral and nasal IXP solutions. These results were further validated by the histopathological examination. The results indicate that the nasal ILN spray demonstrates preclinical efficacy in a rat model, suggesting its potential as a candidate for attenuating DM-associated CAD.