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<p>This study aimed to develop and evaluate a transethosome-based gel formulation of nebivolol to enhance its transdermal delivery for hypertension management. Transethosomes were prepared and characterized using SEM and TEM, revealing uniform, spherical vesicles with nanoscale dimensions and smooth morphology. A validated RP-HPLC method confirmed the chemical integrity of nebivolol post-encapsulation. The optimized formulation was incorporated into carbopol gel, demonstrating favorable physicochemical attributes, including a pH of 6.4, viscosity of 1215 cP, and excellent spreadability. In vitro drug release studies showed sustained release from the transethosomal gel (80% CDR over 10&#xa0;h) compared to the plain gel (65%), fitting the Korsmeyer–Peppas kinetic model. Ex vivo permeation studies through goat skin confirmed superior permeation, with cumulative release approaching 89% and a 1.7-fold higher flux compared to control. Skin irritancy assessment in rats showed no erythema or edema, indicating excellent dermal tolerability. In vivo antihypertensive evaluation using a DOCA-salt-induced hypertensive rat model demonstrated a significant reduction in systolic blood pressure (129&#xa0;mmHg) in the transethosomal gel group compared to disease control (181&#xa0;mmHg) and marketed oral formulation (146&#xa0;mmHg). Stability studies under refrigerated and ambient conditions over 60&#xa0;days confirmed preservation of physicochemical characteristics. These findings collectively highlight the potential of the transethosomal gel as a promising transdermal platform for sustained nebivolol delivery with improved efficacy and patient compliance.</p>

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Formulation, Characterization, and In Vivo Assessment of Nebivolol-Encapsulated Transethosomal Gel: A Novel Strategy for Sustained Transdermal Antihypertensive Therapy

  • 期刊论文

  • 发表日期：

    2025年9月29日

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  • Umashri A. Kokatanur,
  • Panchaxari M. Dandagi

摘要

This study aimed to develop and evaluate a transethosome-based gel formulation of nebivolol to enhance its transdermal delivery for hypertension management. Transethosomes were prepared and characterized using SEM and TEM, revealing uniform, spherical vesicles with nanoscale dimensions and smooth morphology. A validated RP-HPLC method confirmed the chemical integrity of nebivolol post-encapsulation. The optimized formulation was incorporated into carbopol gel, demonstrating favorable physicochemical attributes, including a pH of 6.4, viscosity of 1215 cP, and excellent spreadability. In vitro drug release studies showed sustained release from the transethosomal gel (80% CDR over 10 h) compared to the plain gel (65%), fitting the Korsmeyer–Peppas kinetic model. Ex vivo permeation studies through goat skin confirmed superior permeation, with cumulative release approaching 89% and a 1.7-fold higher flux compared to control. Skin irritancy assessment in rats showed no erythema or edema, indicating excellent dermal tolerability. In vivo antihypertensive evaluation using a DOCA-salt-induced hypertensive rat model demonstrated a significant reduction in systolic blood pressure (129 mmHg) in the transethosomal gel group compared to disease control (181 mmHg) and marketed oral formulation (146 mmHg). Stability studies under refrigerated and ambient conditions over 60 days confirmed preservation of physicochemical characteristics. These findings collectively highlight the potential of the transethosomal gel as a promising transdermal platform for sustained nebivolol delivery with improved efficacy and patient compliance.