Penetration, permeation, and absorption of triamcinolone acetonide in Normal and Psoriatic Skin

Abstract

Penetration studies of radiolabelled Triamcinolone acetonide from ointment or cream preparations revealed that in cases of normal as well as psoriatic skin 70-90% of the applied substance remains on the surface. Normal horny layer stores up to 30% of the steroid. Nevertheless, a rapid penetration into the living layers of the skin is observed, whereby the epidermal concentrations reach levels between 5-10(-6) and 3-10(-5) M (mol per liter of tissue). The excretion in the urine took more than 72 h after removal of the excess of substance from the skin. In psoriatic skin, the epidermal and dermal concentrations were 3-10 times higher than in normal skin. This increase lies in the same range as the one resulting from removal of the horny layer by stripping prior to the application, as reported earlier.

Modelling Dermal Drug Distribution After Topical Application in Human

“…The research effort into understanding the distribution of topically applied solutes in underlying tissues has been relatively modest, confounded by the inability to recreate in-vivo conditions using in-vitro experiments (1) and the invasiveness associated with the collection of such data using biopsy. Most prominent in this regard is the work of Schaefer and colleagues, who obtained human tissue concentration-depth profiles of various drugs in-vivo after topical application (1)(2)(3)(4)(5).…”

“…The model also includes the potential contribution to transport processes by dermal diffusion and vascular wall permeability. We use a combination of human biopsy data generated by Schaefer and colleagues (1)(2)(3)(4)(5) and our own human in-vitro dermis penetration experiments to obtain two critically important parameters of the distributed model: dermis diffusion/dispersion coefficient and dermal blood clearance rate for six solutes: Desoximetasone (Des), Econazole (Ec), Hydrocortisone (Hyd), 8-Methoxypsoralen (Met), Retinoic acid (RA), Triamcinolone acetonide (TA) (molecular weight, solubility and other physicochemical properties of this solutes are presented in Table I). …”

Comparison of the Effects of Chemical Permeation Enhancers on the Lipoidal Pathways of Human Epidermal Membrane and Hairless Mouse Skin and The Mechanism of Enhancer Action

“…Also, the human skin samples are typically obtained from a variety of anatomical sites and under different conditions, which may affect the percutaneous permeability of a drug. [1][2][3] Site-to-site differences within the same donor in percutaneous absorption have been attributed to many factors including variations in stratum corneum (SC) structure, thickness, and lipid content. 1,4,5 Intra-sample variations (differences within a given specimen) have also been reported.…”

Deep Percutaneous Penetration into Muscles and Joints: Update

“…More specifically, they focused on the effect of blood flow, blood protein binding and dermal binding exert on the rate and depth of percutaneous penetration of topical drugs. Unlike Singh and Roberts, and Higaki et al, in applying their model they used the combination of human biopsy data collected by Schaefer and colleagues [23][24][25][26][27] and their own human in-vitro dermis penetration experiments to obtain dermal diffusion/dispersion coefficient, and dermal blood clearance rate of 6 solutes. Schaefer and colleagues collected human tissue concentration-depth profile of drugs in-vivoafter topical application.…”