Localization of dexamethasone within dendritic core-multishell (CMS) nanoparticles and skin penetration properties studied by multi-frequency electron paramagnetic resonance (EPR) spectroscopy

[Display omitted] The skin and especially the stratum corneum (SC) act as a barrier and protect epidermal cells and thus the whole body against xenobiotica of the external environment. Topical skin treatment requires an efficient drug delivery system (DDS). Polymer-based nanocarriers represent novel...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2017-07, Vol.116, p.94-101
Main Authors: Saeidpour, S., Lohan, S.B., Anske, M., Unbehauen, M., Fleige, E., Haag, R., Meinke, M.C., Bittl, R., Teutloff, C.
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Dendritic core-multishell (CMS) systems
Dexamethasone
Dexamethasone - chemistry
Dexamethasone - metabolism
Drug Carriers - chemistry
Drug Carriers - metabolism
Drug delivery system (DDS)
Drug Delivery Systems - methods
Dual-frequency EPR
Electron Spin Resonance Spectroscopy - methods
Mobility
Nanoparticles - chemistry
Nanoparticles - metabolism
Polymers - chemistry
Polymers - metabolism
Skin - metabolism
Skin Absorption - drug effects
Skin penetration
Solvent polarity
Spin Labels
Swine
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Summary:[Display omitted] The skin and especially the stratum corneum (SC) act as a barrier and protect epidermal cells and thus the whole body against xenobiotica of the external environment. Topical skin treatment requires an efficient drug delivery system (DDS). Polymer-based nanocarriers represent novel transport vehicles for dermal application of drugs. In this study dendritic core-multishell (CMS) nanoparticles were investigated as promising candidates. CMS nanoparticles were loaded with a drug (analogue) and were applied to penetration studies of skin. We determined by dual-frequency electron paramagnetic resonance (EPR) how dexamethasone (Dx) labelled with 3-carboxy-2,2,5,5-tetramethyl-1-pyrrolidinyloxy (PCA) is associated with the CMS. The micro-environment of the drug loaded to CMS nanoparticles was investigated by pulsed high-field EPR at cryogenic temperature, making use of the fact that magnetic parameters (g-, A-matrices, and spin-lattice relaxation time) represent specific probes for the micro-environment. Additionally, the rotational correlation time of spin-labelled Dx was probed by continuous wave EPR at ambient temperature, which provides independent information on the drug environment. Furthermore, the penetration depth of Dx into the stratum corneum of porcine skin after different topical applications was investigated. The location of Dx in the CMS nanoparticles is revealed and the function of CMS as penetration enhancers for topical application is shown.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2016.10.001