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<p>The study aimed to develop an ivabradine hydrochloride (IVA HCl)–loaded nanosuspension-based transdermal gel to improve diffusivity and bioavailability. Ivabradine hydrochloride, a selective <i>I</i><sub><i>f</i></sub> channel blocker, is widely used for anti-ischemic therapy to reduce heart rate. However, its extensive hepatic metabolism limits its oral bioavailability to approximately 40%, necessitating an alternative delivery approach. A double-emulsion solvent evaporation/diffusion method combined with central composite design was used to optimize the nanosuspension. Key formulation parameters—particle size, polydispersity index, zeta potential, entrapment efficiency, pH, drug content, spreadability, viscosity, and gelling strength—were systematically evaluated. The optimized nanosuspension demonstrated a particle size of 225&#xa0;nm, PDI of 0.12, zeta potential of + 36&#xa0;mV, and 95.31% entrapment efficiency, confirming stability and uniformity. The nanosuspension-based gel exhibited desirable rheological properties and significantly higher ex vivo permeation (flux, 98.48&#xa0;µg/cm<sup>2</sup>/h; permeability coefficient, 49.24&#xa0;cm/h) compared to plain gel (15.42&#xa0;µg/cm<sup>2</sup>/h; 7.71&#xa0;cm/h). Stability studies under ICH-accelerated conditions indicated no significant changes after 6&#xa0;months. These findings demonstrate that the nanosuspension gel can enhance ivabradine delivery and support its potential as an alternative to oral administration. Comparative drug permeation studies confirmed that the nanosuspension-based transdermal gel significantly improved diffusivity and bioavailability over conventional formulations. Moreover, the nanosuspension formulation supports sustained and controlled drug release, which is particularly beneficial for drugs like ivabradine that require steady plasma concentrations for optimal therapeutic action. This approach offers a promising alternative delivery strategy for ivabradine HCl, potentially enhancing its therapeutic efficacy and patient compliance.</p> Graphical Abstract <p></p>

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Development of Ivabradine Hydrochloride Nanosuspension Containing Gel for Transdermal Delivery: In Vitro and Ex Vivo Characterization

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Malaykumar Chotaliya,
  • Kiran Dudhat,
  • Bhupendra Prajapati

摘要

The study aimed to develop an ivabradine hydrochloride (IVA HCl)–loaded nanosuspension-based transdermal gel to improve diffusivity and bioavailability. Ivabradine hydrochloride, a selective If channel blocker, is widely used for anti-ischemic therapy to reduce heart rate. However, its extensive hepatic metabolism limits its oral bioavailability to approximately 40%, necessitating an alternative delivery approach. A double-emulsion solvent evaporation/diffusion method combined with central composite design was used to optimize the nanosuspension. Key formulation parameters—particle size, polydispersity index, zeta potential, entrapment efficiency, pH, drug content, spreadability, viscosity, and gelling strength—were systematically evaluated. The optimized nanosuspension demonstrated a particle size of 225 nm, PDI of 0.12, zeta potential of + 36 mV, and 95.31% entrapment efficiency, confirming stability and uniformity. The nanosuspension-based gel exhibited desirable rheological properties and significantly higher ex vivo permeation (flux, 98.48 µg/cm2/h; permeability coefficient, 49.24 cm/h) compared to plain gel (15.42 µg/cm2/h; 7.71 cm/h). Stability studies under ICH-accelerated conditions indicated no significant changes after 6 months. These findings demonstrate that the nanosuspension gel can enhance ivabradine delivery and support its potential as an alternative to oral administration. Comparative drug permeation studies confirmed that the nanosuspension-based transdermal gel significantly improved diffusivity and bioavailability over conventional formulations. Moreover, the nanosuspension formulation supports sustained and controlled drug release, which is particularly beneficial for drugs like ivabradine that require steady plasma concentrations for optimal therapeutic action. This approach offers a promising alternative delivery strategy for ivabradine HCl, potentially enhancing its therapeutic efficacy and patient compliance.

Graphical Abstract