Effects of Ethanol on the Transport of β-Estradiol in Hairless Mouse Skin

Higuchi, William I.; Rohr, Uwe D.; Burton, Scott A.; Liu, P.; Fox, Jeffrey L.; Ghanem, Abdel‐Halim; Mahmoud, Hanaa; Borsadia, S.; Good, William R.

doi:10.1021/bk-1987-0348.ch017

Cited by 6 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This could be rationalized by the different treatments of the skin samples. In the referenced study, the skin was treated with a Dx dispersion containing ethanol [35,54], which is known to reduce the barrier function of the SC [55]. In the current study, however, neither the base cream nor the nanocrystal solution contained ethanol.…”

Section: Discussionmentioning

confidence: 80%

Nanocrystals for Improved Drug Delivery of Dexamethasone in Skin Investigated by EPR Spectroscopy

et al. 2020

View full text Add to dashboard Cite

Nanocrystals represent an improvement over the traditional nanocarriers for dermal application, providing the advantages of 100% drug loading, a large surface area, increased adhesion, and the potential for hair follicle targeting. To investigate their advantage for drug delivery, compared to a base cream formulation, dexamethasone (Dx), a synthetic glucocorticoid frequently used for the treatment of inflammatory skin diseases, was covalently linked with the paramagnetic probe 3-(carboxy)-2,2,5,5-tetramethyl-1-pyrrolidinyloxy (PCA) to DxPCA. To investigate the penetration efficiency between these two vehicles, electron paramagnetic resonance (EPR) spectroscopy was used, which allows the quantification of a spin-labeled drug in different skin layers and the monitoring of the drug release. The penetration behavior in excised healthy and barrier-disrupted porcine skin was monitored by EPR, and subsequently analyzed using a numerical diffusion model. As a result, diffusion constants and free energy values in the different layers of the skin were identified for both formulations. Dx-nanocrystals showed a significantly increased drug amount that penetrated into viable epidermis and dermis of intact (factor 3) and barrier-disrupted skin (factor 2.1) compared to the base cream formulation. Furthermore, the observed fast delivery of the spin-labeled drug into the skin (80% DxPCA within 30 min) and a successive release from the aggregate unit into the viable tissue makes these nanocrystals very attractive for clinical applications.

show abstract

Section: Discussionmentioning

confidence: 80%