bromochloroacetic-acid and laurocapram

The interactions of 1-dodecyl-azacycloheptan-2-one (Azone), a penetration enhancer, with mouse skin were analyzed by fluorescence microscopy, solid-state 13C-CP/MAS-NMR spectroscopy and Attenuated Total Reflectance Fourier-transform infrared (ATR-FT-IR) spectroscopy. Ferulic acid was employed as fluorescent probe to observe the delivery pathway in the stratum corneum (SC) after treatment with Azone. Results suggested that the interaction between Azone and the SC occurs in the lipid domains as well as the protein domains. FT-IR measurements show that treatment with Azone results in significant shifts toward larger wavenumbers at v(as)CH2 and v(s)CH2, indicating an increased gauche conformational isomer content of lipid CH2. Further, a decrease of (13C)T1 values and a shift of the SC protein amide-II band to a short wavenumber were found when the SC was pretreated with Azone. It is concluded that Azone can partially convert the SC protein from an alpha-helix conformation to a beta-sheet conformation and loosen the aggregating SC keratins at room temperature.

Topics: Adjuvants, Pharmaceutic; Administration, Cutaneous; Animals; Azepines; Coumaric Acids; Diffusion; Fluorescent Dyes; In Vitro Techniques; Keratins; Lipids; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Microscopy, Fluorescence; Protein Structure, Secondary; Skin; Skin Absorption; Spectroscopy, Fourier Transform Infrared

We have studied the effect of various absorption promoters on the percutaneous absorption dynamics of 6-carboxyfluorescein (CF) which is a poorly absorbable drug. The absorption of CF was determined by fluorescence photographic image since CF emits a strong light yellow fluorescence. The co-administration of sodium dodecylsulfate (SDS) and 2-mercaptoethanol (MER), the pretreatment with calcium thioglycolate and the co-administration of Azone (AZ) and surfactant (HCO-60) were used to promote the absorption of CF. We have also studied the injury of skin tissue by the absorption promoters. The fluorescence photographic image of rat skin, after the co-administration of SDS and MER and after the co-administration of AZ and HCO-60 were similar to the image with the stratum corneum removed from the skin. These absorption promoters did not affect the histological nature of the rat skin tissue and the recovery experiment showed no injurious effect by these absorption promoters to the skin tissue.

Topics: Animals; Azepines; Electrophoresis, Polyacrylamide Gel; Fluoresceins; Histocytochemistry; In Vitro Techniques; Keratins; Male; Rats; Rats, Inbred Strains; Skin; Skin Absorption; Sulfhydryl Compounds; Surface-Active Agents