Analysis of in Vitro Skin Permeation of 22-Oxacalcitriol Having a Complicated Metabolic Pathway

Abstract

The present analysis made it possible to calculate skin permeation parameters (partitioning, diffusivity, and metabolic rate) of OCT without requiring metabolic information, e.g., quantification of metabolites or identification of metabolic pathways. This would be widely applicable for drugs that are not suitable for conventional methods due to complicated metabolic pathways.

Structure–Permeability Relationship Analysis of the Permeation Barrier Properties of the Stratum Corneum and Viable Epidermis/Dermis of Rat Skin

“…Analysis of skin permeation was carried out according to the method previously reported 16. A two‐layer skin model including metabolic processes was employed to express the in vitro skin permeation of a drug.…”

“…The drug permeation process in skin can be expressed using diffusion models. Using the two‐layer diffusion model for skin permeation analysis,12–16 skin permeation parameters relating to both SC and VED can be estimated. In this study, an in vitro rat skin permeation study was carried out using both hydrophilic and lipophilic compounds as the test compounds.…”

Metabolism of captopril carboxyl ester derivatives for percutaneous absorption

“…The use of homogenised full-thickness skin is perhaps more akin to the in-vivo situation, and as such it may be argued that determination of enzyme concentration and type is not strictly necessary since this information would not be available in vivo, and enzyme localisation may vary depending on skin thickness. [29,30] Porcine skin has often been identified as a good substitute for human skin [31] for use in transdermal diffusion studies, and is known to contain CYP and other non-specific esterases. [8,9] Response (g) regulatory issues pertaining to the use of porcine tissue, therefore it was the most convenient and applicable tissue to use during these investigations.…”

Metabolism of captopril carboxyl ester derivatives for percutaneous absorption

“…The use of homogenised full‐thickness skin is perhaps more akin to the in‐vivo situation, and as such it may be argued that determination of enzyme concentration and type is not strictly necessary since this information would not be available in vivo , and enzyme localisation may vary depending on skin thickness 29,30 . Porcine skin has often been identified as a good substitute for human skin 31 for use in transdermal diffusion studies, and is known to contain CYP and other non‐specific esterases 8,9 .…”