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Particle-Assisted Dermal Penetration — A Simple Formulation Strategy to Foster the Dermal Penetration Efficacy
(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 pe...
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| Main Authors: | , |
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| Format: | Article |
| Language: | English |
| Published: |
Philipps-Universität Marburg
2023
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| Subjects: | |
| Online Access: | PDF Full Text |
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| Summary: | (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. |
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| Item Description: | Gefördert durch den Open-Access-Publikationsfonds der UB Marburg. |
| Physical Description: | 17 Pages |
| DOI: | 10.3390/pharmaceutics14051039 |