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Article

Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy

Department of Pharmaceutics and Biopharmaceutics, Philipps-University of Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany
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Author to whom correspondence should be addressed.
Academic Editors: Snezana Savic and Ivana Pantelić
Pharmaceutics 2022, 14(5), 1039; https://doi.org/10.3390/pharmaceutics14051039
Received: 26 March 2022 / Revised: 6 May 2022 / Accepted: 9 May 2022 / Published: 11 May 2022
(1) Background: The study systematically investigated the influence of dispersed particles within a topical formulation on the dermal penetration efficacy of active compounds that are dissolved in the water phase of this formulation. The aim was to prove or disprove if particle-assisted dermal penetration can be used for improved dermal drug delivery. (2) Methods: Fluorescein was used as a surrogate for a hydrophilic active ingredient (AI). It was dissolved in the water phase of different formulations with and without particles. Two different types of particles (titanium dioxide and nanostructured lipid carriers (NLC)) were used. The influence of particle size and number of particles and the influence of skin hydrating excipients was also investigated. (3) Results demonstrate that the addition of particles can strongly increase the dermal penetration efficacy of AI. The effect depends on the size of the particles and the number of particles in the formulation, where smaller sizes and higher numbers resulted in higher penetration parameters. Formulations with NLC that contained 20% w/w or 40% w/w particles resulted in an about 2-fold higher amount of penetrated AI and increased the penetration depth about 2.5-fold. The penetration-enhancing effect was highly significant (p < 0.001) and allowed for an efficient delivery of the AI in the viable dermis. In contrast, the penetration-enhancing effect of excipients that increase the skin hydration was found to be very limited and not significant (≤5%, p > 0.05). (4) Conclusions: Based on the results, it can be concluded that particle-assisted dermal penetration can be considered to be a simple but highly efficient and industrially feasible formulation principle for improved and tailor-made dermal drug delivery of active compounds. View Full-Text
Keywords: fluorescein; dermal penetration; ex vivo porcine ear model; digital image analysis; stratum corneum thickness; skin hydration fluorescein; dermal penetration; ex vivo porcine ear model; digital image analysis; stratum corneum thickness; skin hydration
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MDPI and ACS Style

Wiemann, S.; Keck, C.M. Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy. Pharmaceutics 2022, 14, 1039. https://doi.org/10.3390/pharmaceutics14051039

AMA Style

Wiemann S, Keck CM. Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy. Pharmaceutics. 2022; 14(5):1039. https://doi.org/10.3390/pharmaceutics14051039

Chicago/Turabian Style

Wiemann, Sabrina, and Cornelia M. Keck. 2022. "Particle-Assisted Dermal Penetration—A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy" Pharmaceutics 14, no. 5: 1039. https://doi.org/10.3390/pharmaceutics14051039

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