<p>Atopic Dermatitis (AD), commonly termed as atopic eczema or chronic eczema, is a persistent inflammatory condition associated with impaired skin and characterized by an overreactive immunological response to environmental stimuli. Naringenin (NGN) is citrus derived natural flavonoid, has drawn considerable research interest due to its anti-inflammatory, antioxidant property, this research primarily aims to develop and evaluate the NGN-TE formulation using the cold method. Transethosomes (TE) were utilized to improve the solubility, bioavailability and skin penetration. A Box-Behnken design (BBD) approach was employed for the TE formulation optimization with lipoid S100, ethanol and tween 80 as independent variables. The particle size, zeta potential, PDI and entrapment efficiency of optimized NGN-loaded transethosome formulation (NGN-TE) were evaluated and found to be 149.3 ± 2.1&#xa0;nm, -26.8 ± 2.73, 0.289 ± 0.4 and 90.5 ± 2.3%, respectively. Whereas, with TEM imaging spherical and sealed vesicle were observed. The NGN-loaded transethosomal gel (NGN-TE Gel) was prepared by 1% Carbopol 934. In Vitro release study showed that both NGN-TE and NGN-TE gel formulation demonstrate the sustained release for 24&#xa0;h in 7.4 pH in contrast to 5.5 pH buffer media as compared to pure drug. The result of ex vivo and dermatokinetic study depicts the enhanced permeation for NGN-TE gel (7.42 ± 1.5&#xa0;µg/cm2/h) and greater Cskin max and AUC0-8 as compared to pure drug gel in rat skin. There is no any irritation for NGN-TE gel demonstrated as a safe. TE system ensures sustained release, antioxidant action, deeper penetration, enhancing therapeutic effects in AD management.</p> Graphical Abstract <p></p>

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Naringenin-Encapsulated Transethosomal Gel for Dermal Delivery: Ex Vivo Skin Permeation, Dermatokinetic Profiling and Safety Assessment Study

  • Swati Raysing,
  • Asta Chaudhari,
  • Kalpesh Patil,
  • Gita Aher

摘要

Atopic Dermatitis (AD), commonly termed as atopic eczema or chronic eczema, is a persistent inflammatory condition associated with impaired skin and characterized by an overreactive immunological response to environmental stimuli. Naringenin (NGN) is citrus derived natural flavonoid, has drawn considerable research interest due to its anti-inflammatory, antioxidant property, this research primarily aims to develop and evaluate the NGN-TE formulation using the cold method. Transethosomes (TE) were utilized to improve the solubility, bioavailability and skin penetration. A Box-Behnken design (BBD) approach was employed for the TE formulation optimization with lipoid S100, ethanol and tween 80 as independent variables. The particle size, zeta potential, PDI and entrapment efficiency of optimized NGN-loaded transethosome formulation (NGN-TE) were evaluated and found to be 149.3 ± 2.1 nm, -26.8 ± 2.73, 0.289 ± 0.4 and 90.5 ± 2.3%, respectively. Whereas, with TEM imaging spherical and sealed vesicle were observed. The NGN-loaded transethosomal gel (NGN-TE Gel) was prepared by 1% Carbopol 934. In Vitro release study showed that both NGN-TE and NGN-TE gel formulation demonstrate the sustained release for 24 h in 7.4 pH in contrast to 5.5 pH buffer media as compared to pure drug. The result of ex vivo and dermatokinetic study depicts the enhanced permeation for NGN-TE gel (7.42 ± 1.5 µg/cm2/h) and greater Cskin max and AUC0-8 as compared to pure drug gel in rat skin. There is no any irritation for NGN-TE gel demonstrated as a safe. TE system ensures sustained release, antioxidant action, deeper penetration, enhancing therapeutic effects in AD management.

Graphical Abstract