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<p>Heart failure (HF) remains a major global health challenge, underscoring the need for therapeutic strategies that enhance drug performance and improve clinical outcomes. Dapagliflozin, a sodium–glucose cotransporter-2 (SGLT2) inhibitor, has demonstrated clinically relevant cardiovascular benefits; however, its oral delivery is limited by poor aqueous solubility and scope for improved oral delivery performance. In the present study, we developed a bile salt-stabilized nanovesicular system to optimize oral delivery and evaluate the therapeutic performance of dapagliflozin. The optimized formulation, obtained using a central composite design, exhibited a vesicle size of 120.9&#xa0;nm, zeta potential of − 41.69 mV, and entrapment efficiency of 92.8%. Physicochemical characterization confirmed the formation of bile salt-stabilized nanovesicles with reduced drug crystallinity, suggesting effective incorporation within the vesicular matrix. The formulation demonstrated sustained drug release over 24&#xa0;h and improved intestinal penetration compared with dapagliflozin suspension, as evidenced by in vitro release studies and confocal laser scanning microscopy. In an isoproterenol-induced heart failure rat model, nanovesicle<b>-</b>encapsulated dapagliflozin attenuated oxidative stress, reduced cardiac injury biomarkers, and preserved myocardial architecture relative to the conventional drug. These findings support further investigation of bile salt-stabilized nanovesicular delivery as a strategy to enhance dapagliflozin therapy in heart failure.</p>

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Bile-Salt Stabilized Nanovesicular System Enhances the Cardioprotective Effects of Dapagliflozin in Isoproterenol-Induced Experimental Heart Failure

  • 期刊论文

  • 发表日期：

    2026年6月25日

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  • Faisal Ashraf Bhat,
  • Mohd Aqil,
  • Syed Ehtaishamul Haque,
  • Mohd Akhtar,
  • Mohan Kamthan,
  • Abul Kalam Najmi

摘要

Heart failure (HF) remains a major global health challenge, underscoring the need for therapeutic strategies that enhance drug performance and improve clinical outcomes. Dapagliflozin, a sodium–glucose cotransporter-2 (SGLT2) inhibitor, has demonstrated clinically relevant cardiovascular benefits; however, its oral delivery is limited by poor aqueous solubility and scope for improved oral delivery performance. In the present study, we developed a bile salt-stabilized nanovesicular system to optimize oral delivery and evaluate the therapeutic performance of dapagliflozin. The optimized formulation, obtained using a central composite design, exhibited a vesicle size of 120.9 nm, zeta potential of − 41.69 mV, and entrapment efficiency of 92.8%. Physicochemical characterization confirmed the formation of bile salt-stabilized nanovesicles with reduced drug crystallinity, suggesting effective incorporation within the vesicular matrix. The formulation demonstrated sustained drug release over 24 h and improved intestinal penetration compared with dapagliflozin suspension, as evidenced by in vitro release studies and confocal laser scanning microscopy. In an isoproterenol-induced heart failure rat model, nanovesicle-encapsulated dapagliflozin attenuated oxidative stress, reduced cardiac injury biomarkers, and preserved myocardial architecture relative to the conventional drug. These findings support further investigation of bile salt-stabilized nanovesicular delivery as a strategy to enhance dapagliflozin therapy in heart failure.