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Supersaturation: Enhancement of Skin Penetration and Permeation of a Lipophilic Drug

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Titel: Supersaturation: Enhancement of Skin Penetration and Permeation of a Lipophilic Drug
Autoren: Moser, Katrin, Kriwet, K, Froehlich, C, Kalia, Yogeshvar, Guy, Richard H.
Quelle: Pharmaceutical Research, Vol. 18, No 7 (2001) pp. 1006-11
Verlagsinformationen: Springer Science and Business Media LLC, 2001.
Publikationsjahr: 2001
Schlagwörter: ddc:615, Lipids/administration & dosage/pharmacokinetics, Swine, Skin Absorption, Lipids, Propylene Glycol, Permeability, Drug Delivery Systems, Drug Delivery Systems/methods, Animals, Propylene Glycol/administration & dosage/pharmacokinetics, Skin Absorption/physiology, Pharmaceutical Vehicles/administration & dosage/pharmacokinetics, Epidermis, Pharmaceutical Vehicles, Epidermis/metabolism
Beschreibung: To increase the dermal delivery of a lipophilic model compound (LAP), and to deduce the underlying mechanism of enhanced absorption.Penetration of LAP from mixtures of up to four degrees of saturation into the stratum corneum was evaluated using a tape-stripping method; epidermal permeation of the drug was measured in Franz diffusion cells. The relative diffusion and stratum corneum-vehicle partition coefficients of LAP were determined by fitting the results to the appropriate solutions to Fick's second law of diffusion.Both the skin permeation rate and the amount of LAP in the stratum corneum increased linearly with increasing degree of saturation. The apparent diffusivity and its partition coefficient deduced from the penetration experiments were independent of the degree of saturation of the drug in the applied formulation, and consistent with corresponding parameters derived from the permeation experiments.Supersaturation can increase the skin penetration and permeation of lipophilic drugs. The diffusion and partition parameters deduced for LAP indicate that supersaturation acts exclusively via increased thermodynamic activity without apparent effect on the barrier function of the skin per se.
Publikationsart: Article
Dateibeschreibung: application/pdf
Sprache: English
ISSN: 1573-904X
0724-8741
DOI: 10.1023/a:1010948630296
Zugangs-URL: https://pubmed.ncbi.nlm.nih.gov/11496937
https://pubmed.ncbi.nlm.nih.gov/11496937/
https://archive-ouverte.unige.ch/unige:21958
https://researchportal.bath.ac.uk/en/publications/supersaturation-enhancement-of-skin-penetration-and-permeation-of
https://www.ncbi.nlm.nih.gov/pubmed/11496937
https://link.springer.com/article/10.1023/A%3A1010948630296
https://archive-ouverte.unige.ch/unige:21958
Rights: Springer Nature TDM
Dokumentencode: edsair.doi.dedup.....57a5cd81d9968d6631bd5cba108bda7e
Datenbank: OpenAIRE
Beschreibung
Abstract:To increase the dermal delivery of a lipophilic model compound (LAP), and to deduce the underlying mechanism of enhanced absorption.Penetration of LAP from mixtures of up to four degrees of saturation into the stratum corneum was evaluated using a tape-stripping method; epidermal permeation of the drug was measured in Franz diffusion cells. The relative diffusion and stratum corneum-vehicle partition coefficients of LAP were determined by fitting the results to the appropriate solutions to Fick's second law of diffusion.Both the skin permeation rate and the amount of LAP in the stratum corneum increased linearly with increasing degree of saturation. The apparent diffusivity and its partition coefficient deduced from the penetration experiments were independent of the degree of saturation of the drug in the applied formulation, and consistent with corresponding parameters derived from the permeation experiments.Supersaturation can increase the skin penetration and permeation of lipophilic drugs. The diffusion and partition parameters deduced for LAP indicate that supersaturation acts exclusively via increased thermodynamic activity without apparent effect on the barrier function of the skin per se.
ISSN:1573904X
07248741
DOI:10.1023/a:1010948630296