Soft X-ray microscopy for probing of topical tacrolimus delivery via micelles
| Autor: | Moritz Radbruch, Jörg Raabe, Annika Vogt, Lars Mundhenk, Sebastian Bachmann, Achim D. Gruber, Fiorenza Rancan, Eckart Rühl, R. Gurny, Benjamin Watts, A. Klossek, Hannah Pischon, K. Yamamoto, R. Flesch, Petra Schrade, Ulrike Blume-Peytavi, K. Fuchs |
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| Rok vydání: | 2019 |
| Předmět: |
Time Factors
Skin Absorption Pharmaceutical Science 02 engineering and technology Administration Cutaneous 030226 pharmacology & pharmacy Micelle Permeability Tacrolimus Ointments Mice 03 medical and health sciences 0302 clinical medicine Stratum corneum medicine Animals Tissue Distribution Penetration depth Micelles Skin Drug Carriers Microscopy Corneocyte integumentary system Chemistry X-Rays General Medicine Penetration (firestop) 021001 nanoscience & nanotechnology Membrane medicine.anatomical_structure Drug delivery Biophysics 0210 nano-technology Drug carrier Biotechnology |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 139:68-75 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2019.03.006 |
| Popis: | The penetration of topically applied tacrolimus formulated in micelles into murine skin is reported, measured by X-ray microscopy. Tacrolimus and micelles are probed for the first time by this high spatial resolution technique by element-selective excitation in the C 1s- and O 1s-regimes. This method allows selective detection of the distribution and penetration depth of drugs and carrier molecules into biologic tissues. It is observed that small, but distinct quantities of the drug and micelles, acting as a drug carrier, penetrate the stratum corneum. A comparison is made with the paraffin-based commercial tacrolimus ointment Protopic®, where local drug concentrations show to be low. A slight increase in local drug concentration in the stratum corneum is observed, if tacrolimus is formulated in micelles, as compared to Protopic®. This underscores the importance of the drug formulations for effective drug delivery. Time-resolved penetration shows presence of drug in the stratum corneum 100 min after formulation application, with penetration to deeper skin layers at 1000 min. High resolution micrographs give indications for a penetration pathway along the lipid membranes between corneocytes, but also suggest that the compound may penetrate corneocytes. |
| Databáze: | OpenAIRE |
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