dc.contributor.author
Köpke, Daniel
dc.contributor.author
Pyo, Sung Min
dc.date.accessioned
2020-04-17T11:16:20Z
dc.date.available
2020-04-17T11:16:20Z
dc.identifier.uri
https://refubium.fu-berlin.de/handle/fub188/27121
dc.identifier.uri
http://dx.doi.org/10.17169/refubium-26881
dc.description.abstract
Several of most common dermatoses worldwide, e.g., psoriasis and atopic dermatitis, are worsened in their clinical picture when the skin is regularly exposed to an increased air pollution level, e.g., particulate matter. This is explainable by the activation of the aryl hydrocarbon receptor (AhR) in the skin, which results in an increased release of proinflammatory cytokines and matrix metalloproteinases. Symurban is a competitive AhR antagonist and thus allows the effective protection of skin. In order to improve its dermal bioavailability as a poorly soluble active agent (0.25 µg/mL), nanocrystals were prepared and evaluated. Nanocrystals are pure active crystals reduced in particle size to the submicron range of 100 to 1000 nm. They feature the properties of nanocrystals, such as increased saturation solubility and dissolution velocity, without having to be declared as nanomaterial. Production methods and parameters were systematically investigated. Wet bead milling at 2000 rpm for 30 min yielded the best results. A z-average of 280 nm was achieved for a 10% Symurban suspension with a polydispersity index of 0.20, indicating a narrow size distribution. For the long-term stabilization of the nanocrystal suspension, the performance of 15 surfactants of different categories and HLB values were investigated and evaluated. It was found that non-ionic surfactants in general were better able to stabilize the system than anionic or amphoteric surfactants. Highest stability of over 12 months at 25 °C was achieved with 2% Plantacare 810 UP, an ECOCERT surfactant with high skin tolerance. The suspension was also chemically long-term stable with >97% of remaining Symurban over 12 months. The saturation solubility of Symurban as nanocrystals was significantly increased from 0.25 to 2.9 μg/mL, which corresponds to a factor of >11. In a case study of one male volunteer with healthy skin conditions, penetration profiles of Symurban nanocrystal hydrogel and commercial anti-pollution serum containing an identical amount of Symurban were determined and compared. After 20 min of exposure, the relative Symurban concentration in the deeper skin layers (tape 19-30) was more than two times higher for nanocrystal hydrogel (16%) than the commercial serum (7%). These results suggest that nanocrystals are a promising delivery system for the poorly soluble anti-pollution agent Symurban.
en
dc.format.extent
13 Seiten
dc.rights.uri
https://creativecommons.org/licenses/by/4.0/
dc.subject
benzylidene dimethoxydimethylindanone
en
dc.subject
competitive inhibitor of aryl hydrocarbon receptor
en
dc.subject
high pressure homogenization
en
dc.subject
wet bead milling
en
dc.subject
nanosuspension
en
dc.subject
gas chromatography-mass spectrometry
en
dc.subject
saturation solubility
en
dc.subject
skin penetration
en
dc.subject.ddc
600 Technik, Medizin, angewandte Wissenschaften::610 Medizin und Gesundheit::616 Krankheiten
dc.subject.ddc
600 Technik, Medizin, angewandte Wissenschaften::610 Medizin und Gesundheit::615 Pharmakologie, Therapeutik
dc.title
Symurban Nanocrystals for Advanced Anti-Pollution Skincare
dc.type
Wissenschaftlicher Artikel
dcterms.bibliographicCitation.articlenumber
17
dcterms.bibliographicCitation.doi
10.3390/cosmetics7010017
dcterms.bibliographicCitation.journaltitle
Cosmetics
dcterms.bibliographicCitation.number
1
dcterms.bibliographicCitation.originalpublishername
MDPI
dcterms.bibliographicCitation.volume
7
dcterms.bibliographicCitation.url
https://doi.org/10.3390/cosmetics7010017
refubium.affiliation
Biologie, Chemie, Pharmazie
refubium.affiliation.other
Institut für Pharmazie

refubium.resourceType.isindependentpub
no
dcterms.accessRights.openaire
open access
dcterms.isPartOf.eissn
2079-9284