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Peer-reviewedCC BYPharmaceutics

Crisaborole-Loaded Nanoemulsion for Atopic Dermatitis: Localized Dermal Delivery of a Phosphodiesterase-4 Inhibitor.

  • Lupe Carolina Espinoza1
  • Lilian Sosa2,3,4
  • Paulo Sarango-Granda1
  • Elena Sánchez-López5,6
  • Jandry Rosales-Sánchez1
  • Dagmar Gualotuña Campoverde1
  • Rafaela Polo1
  • Mireia Mallandrich5,6
  • Ana Cristina Calpena5,6
6 affiliations
  1. 1Departamento de Química, Facultad de Ciencias Exactas y Naturales, Universidad Técnica Particular de Loja, Loja 110107, Ecuador.
  2. 2Universidad Pedagógica Nacional Francisco Morazán, Tegucigalpa 11101, Honduras.
  3. 3Instituto de Investigaciones en Microbiología (IIM), Facultad de Ciencias, Universidad Nacional Autónoma de Honduras (UNAH), Tegucigalpa 11101, Honduras.
  4. 4Facultad de Ciencias Químicas y Farmacia, Universidad Nacional Autónoma de Honduras (UNAH), Tegucigalpa 11101, Honduras.
  5. 5Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain.
  6. 6Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, Spain.
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Abstract

Background/Objectives: Crisaborole (CRB) is a phosphodiesterase-4 inhibitor used for the topical treatment of mild-to-moderate atopic dermatitis (AD). However, its low aqueous solubility presents challenges for topical formulation and localized drug delivery. This study aimed to develop a CRB-loaded nanoemulsion (CRB-NE) and evaluate its physicochemical and biopharmaceutical characteristics, tolerability, and anti-inflammatory activity. Methods: CRB-NE (0.5% w/w) was developed using pseudo-ternary phase diagrams. Droplet size, morphology, rheological behavior, spreadability, and stability were characterized. Drug release and ex vivo permeation in human skin were evaluated. Biological compatibility was investigated using HaCaT keratinocytes and the hen's egg test-chorioallantoic membrane (HET-CAM) assay, while skin barrier compatibility was assessed in healthy volunteers. Anti-inflammatory activity was evaluated through IL-8 secretion in stimulated HaCaT cells and a xylene-induced ear inflammation model in mice. Results: CRB-NE showed a droplet size of 105.3 ± 6.7 nm, a polydispersity index of 0.287 ± 0.012, Newtonian flow behavior, and physical stability over 60 days. Approximately 80% of CRB was released following first-order kinetics. After 24 h, ex vivo experiments showed cutaneous retention of 1098.43 μg CRB/g skin/cm² and cumulative permeation of 23.75 ± 4.44 μg/cm². Keratinocyte viability exceeded 80% at CRB concentrations of 2.5-10 μg/mL, and HET-CAM results indicated low irritation potential. The vehicle did not adversely affect skin barrier measurements in healthy volunteers. CRB-NE significantly reduced IL-8 secretion in TNF-α-stimulated keratinocytes and attenuated erythema, inflammatory cell infiltration, edema, vascular congestion, and tissue damage in vivo. Conclusions: CRB-NE demonstrated favorable physicochemical properties, substantial cutaneous drug retention, and anti-inflammatory activity, supporting its potential as a localized topical delivery system.

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Cite

BibTeXRIS
BibTeX
@article{espinoza2026crisaboroleloaded,
  title = {{Crisaborole-Loaded Nanoemulsion for Atopic Dermatitis: Localized Dermal Delivery of a Phosphodiesterase-4 Inhibitor.}},
  author = {Lupe Carolina Espinoza and Lilian Sosa and Paulo Sarango-Granda and Elena Sánchez-López and Jandry Rosales-Sánchez and Dagmar Gualotuña Campoverde and Rafaela Polo and Mireia Mallandrich and Ana Cristina Calpena},
  journal = {Pharmaceutics},
  year = {2026},
  month = oct,
  doi = {10.3390/pharmaceutics18101342},
  url = {https://europepmc.org/article/MED/42942871},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - Crisaborole-Loaded Nanoemulsion for Atopic Dermatitis: Localized Dermal Delivery of a Phosphodiesterase-4 Inhibitor.
AU  - Lupe Carolina Espinoza
AU  - Lilian Sosa
AU  - Paulo Sarango-Granda
AU  - Elena Sánchez-López
AU  - Jandry Rosales-Sánchez
AU  - Dagmar Gualotuña Campoverde
AU  - Rafaela Polo
AU  - Mireia Mallandrich
AU  - Ana Cristina Calpena
PY  - 2026
DA  - 2026/10/21
JO  - Pharmaceutics
DO  - 10.3390/pharmaceutics18101342
UR  - https://europepmc.org/article/MED/42942871
AB  - Background/Objectives: Crisaborole (CRB) is a phosphodiesterase-4 inhibitor used for the topical treatment of mild-to-moderate atopic dermatitis (AD). However, its low aqueous solubility presents challenges for topical formulation and localized drug delivery. This study aimed to develop a CRB-loaded nanoemulsion (CRB-NE) and evaluate its physicochemical and biopharmaceutical characteristics, tolerability, and anti-inflammatory activity. Methods: CRB-NE (0.5% w/w) was developed using pseudo-ternary phase diagrams. Droplet size, morphology, rheological behavior, spreadability, and stability were characterized. Drug release and ex vivo permeation in human skin were evaluated. Biological compatibility was investigated using HaCaT keratinocytes and the hen's egg test-chorioallantoic membrane (HET-CAM) assay, while skin barrier compatibility was assessed in healthy volunteers. Anti-inflammatory activity was evaluated through IL-8 secretion in stimulated HaCaT cells and a xylene-induced ear inflammation model in mice. Results: CRB-NE showed a droplet size of 105.3 ± 6.7 nm, a polydispersity index of 0.287 ± 0.012, Newtonian flow behavior, and physical stability over 60 days. Approximately 80% of CRB was released following first-order kinetics. After 24 h, ex vivo experiments showed cutaneous retention of 1098.43 μg CRB/g skin/cm² and cumulative permeation of 23.75 ± 4.44 μg/cm². Keratinocyte viability exceeded 80% at CRB concentrations of 2.5-10 μg/mL, and HET-CAM results indicated low irritation potential. The vehicle did not adversely affect skin barrier measurements in healthy volunteers. CRB-NE significantly reduced IL-8 secretion in TNF-α-stimulated keratinocytes and attenuated erythema, inflammatory cell infiltration, edema, vascular congestion, and tissue damage in vivo. Conclusions: CRB-NE demonstrated favorable physicochemical properties, substantial cutaneous drug retention, and anti-inflammatory activity, supporting its potential as a localized topical delivery system.
SN  - 1999-4923
ER  -