Role of Transepidermal and Transfollicular Routes in Percutaneous Absorption of Hydrocortisone and Testosterone: In vivo Study in the Hairless Rat

Hueber, Frédérique; Wépierre, J.; Schaefer, Hans

doi:10.1159/000211026

Cited by 87 publications

(50 citation statements)

References 12 publications

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“…In the literature, a major contribution of hair follicles to the skin permeation of steroids has already been reported. [16][17][18] Next, the hairless rat skin surface was observed in a SEM after application of a TA suspended solution at a concentration of 1000 mg/ml. As shown in the two pictures in Fig.…”

Section: Resultsmentioning

confidence: 99%

Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

2010

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Studies on topical formulations containing steroidal drugs were started in 1952 by Goldman et al.,1) who firstly used topical formulations containing a steroid, cortisone acetate, to treat skin diseases. Dumas and Scholtz reported typical concentration dependence of steroidal drugs on the pharmacological effect against psoriasis.2) The effect of topical steroids is closely related to the steroidal concentration at the skin disease site. The skin concentration is usually determined by partition and diffusivity of the steroid into and through the skin. The calculated concentration is sometimes more useful than the directly observed skin concentration.3) The partition and diffusion properties are affected by the thermodynamic activity and state (solution/suspension) of steroids, as well as the barrier function of the skin. Generally, the thermodynamic activity of drugs shows their escaping tendencies from formulations. 4) Skin permeation is a transport phenomenon from a high activity-site to a low activitysite, indicating that skin permeation occurs due to an activity difference. 5) Thermodynamic activity of drugs must be considered when designing topical [6][7][8] and cosmetic formulations. 9) Most studies on steroidal drugs focused on their pharmacological effects, 1,2,10,11) but not on steroid disposition in the skin. 11,12) There are very few studies, however, on the effect of thermodynamic activity and state (solution/suspension) of steroids in topical formulations on skin permeation and skin disposition.A medium strength steroid, triamcinolone acetonide (TA), was selected as a model drug in the present study. The effects of thermodynamic activity and TA state were evaluated for the TA concentration in the stratum corneum and viable epidermis and dermis. One-layered and two layered models were used to analyze the membrane permeation and concentration of TA by Fick's law of diffusion. Distilled water was used as a formulation vehicle to simplify evaluate the effect of thermodynamic activity and TA state. ExperimentalMaterials and Experimental Animals A powder of triamcinolone acetonide (TA) (MW; 434.5, mp; 290°C, Log P; 2.53, solubility in water at 32°C; 22.05Ϯ0.05 mg/ml, and solubility parameter; 9.45 (cal/cm 3 ) 1/2 ) was purchased from Wako Pure Chemical Industries, Ltd. (Chuo, Osaka, Japan). A disposable syringe filter unit (DISMIC ® -13HP 0.20 mm) was purchased from Toyo Roshi Kaisha, Ltd. (Bunkyo, Tokyo, Japan). Other chemicals and solvents were of reagent grade or HPLC grade and used without further purification. A silicone membrane (LTC-S1-75, thickness of 75 mm) was a kind gift from Lintec Co., Ltd. (Itabashi, Tokyo, Japan). A three-dimensional cultured human skin model (LSE-high: TMLSE-003) was purchased from Toyobo Co., Ltd. (Kita, Osaka, Japan). Male hairless rats (WBM/ILA-Ht, 8-9 weeks-old, body weight: 230-260 g) were obtained from the Life Science Research Center, Josai University (Sakado, Saitama, Japan) or Ishikawa Experimental Animals (Fukaya, Saitama, Japan). The animal feeding and experiment...

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Section: Resultsmentioning

confidence: 99%

Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

2010

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“…for multiple topically applied lipophilic compounds, e.g., for steroid hormones (76) or photosensitizers (77), etc., arguing that the CBD doses tested here are translationally absolutely relevant.…”

Section: Discussionmentioning

confidence: 99%

Cannabidiol exerts sebostatic and antiinflammatory effects on human sebocytes

Oláh¹,

Tóth²,

Borbíró³

et al. 2014

J. Clin. Invest.

236

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“…Nonetheless, for several compounds (e.g., caffeine, hydrocortisone, testosterone [68][69][70] ) the follicular route seems to promote permeability at the beginning of skin absorption while it is overruled by the other higher capacity pathways at later times in the transport process. 68 In the context of the absorption of nanoparticles the follicles have received much higher attention.…”

Section: Follicular Penetrationmentioning

confidence: 99%

Nanoparticles and their interactions with the dermal barrier

Schneider

Stracke

Hansen

et al. 2009

Dermato-Endocrinology

383

193

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The dermal application of drugs is promising due to the ease of application. In this context nano-scale carrier systems were already evaluated in several studies with respect to the skin interaction and the impact on drug penetration. At the same time the upcoming production of engineered nano-scale materials requires a thorough safety evaluation. Drug delivery as well as risk assessment depends crucially on the ability of such carriers to overcome the skin barrier and reach deeper tissue layers. Therefore, the interaction of nanoparticles with skin and especially skin models is an intriguing field. However, the data obtained do not show a clear image on the effect of nano-carriers. Especially the penetration of such particles is an open and controversially discussed topic. The literature reports different results mainly on pig or murine skin showing strong penetration (pig and mouse) or the opposite. Looking only at the sizes of the particles also no conclusive picture can be obtained. Nevertheless, size is regarded to play an important role for skin penetration. Furthermore, the state of the skin influences penetration (hydration) and the mechanical stress is of outmost importance. IntroductionAny kind of organism always faced nanoscale environmental compounds interacting with their exterior barrier but a significant interest in these interactions came up not until the broad ascent of artificial nanoparticulate compounds. 1 The great potential for future advanced applications in areas such as energy, electronics, automotive, chemistry and life sciences led to a rapidly growing number of nanoparticulate systems, with respect to material composition, size, shape and formulation. Nanomedicines, incorporating drug delivery, diagnostics, implants, cancer therapy, to name just a few, pose an important and appealing area for beneficial application. Regarding final applicability it is essential to investigate the various biological aspects of nanoparticle exposure to the human organism. On one hand health hazards are to be identified and assessed, on the other hand medical and pharmaceutical potentials may be discovered and exploited. The behavior of nanoparticulate substances in biosystems and their physiological effects can, up to now, neither be extrapolated straightforwardly from bulk properties nor can they be predicted from molecular properties of the constituents. The first step of any interaction between an organism and any compound is the uptake of the compound from the environment. Several pathways of absorption exist for human (and most animal) organisms of which the skin is the most obvious and easiest to reach.The present review focus on skin and its barrier as well as sink function to artificial nanoparticulate compounds. Different classes of nanoparticulate material were studied to gain knowledge on the interaction and possible impact on skin covering bio-resistant particles (e.g., metal oxide, carbon-based) and biodegradable particles (e.g., liposomes, polymeric particles). Furthermore, mainly healthy ...

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Role of Transepidermal and Transfollicular Routes in Percutaneous Absorption of Hydrocortisone and Testosterone: In vivo Study in the Hairless Rat

Cited by 87 publications

References 12 publications

Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

Cannabidiol exerts sebostatic and antiinflammatory effects on human sebocytes

Nanoparticles and their interactions with the dermal barrier

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