Follicles Play an Important Role in Percutaneous Absorption

Illel, Brigitte; Schaefer, Hans; Wépierre, J.; Doucet, Olivier

doi:10.1002/jps.2600800505

Cited by 140 publications

(61 citation statements)

References 9 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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“…However, researchers reported that the skin penetration was influenced by the existence of hair follicles. [15][16][17] The steady-state penetration rate of model drugs through appendage-free skin of hairless rat was two to four times larger than that of normal skin. 15) Aim of our research isn't to indicate the importance of appendage but is to show the correlation between the penetration parameters through LabCyte and HLM skin.…”

Section: Resultsmentioning

confidence: 96%

Prediction of Percutaneous Absorption in Human Using Three-Dimensional Human Cultured Epidermis LabCyte EPI-MODEL

Hikima

Kaneda

Matsuo

et al. 2012

Biological & Pharmaceutical Bulletin

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The objective of this study is to establish a relationship of the skin penetration parameters between the three-dimensional cultured human epidermis LabCyte EPI-MODEL (LabCyte) and hairless mouse (HLM) skin penetration in vitro and to predict the skin penetration and plasma concentration profile in human. The skin penetration experiments through LabCyte and HLM skin were investigated using 19 drugs that have a different molecular weight and lipophilicity. The penetration flux for LabCyte reached 30 times larger at maximum than that for HLM skin. The human data can be estimated from the in silico approach with the diffusion coefficient (D), the partition coefficient (K) and the skin surface concentration (C) of drugs by assuming the bi-layer skin model for both LabCyte and HLM skin. The human skin penetration of β-estradiol, prednisolone, testosterone and ethynylestradiol was well agreed between the simulated profiles and in vitro experimental data. Plasma concentration profiles of β-estradiol in human were also simulated and well agreed with the clinical data. The present alternative method may decrease human or animal skin experiment for in vitro skin penetration.Key words in silico correlation; reconstructed epidermis; LabCyte EPI-MODEL; hairless mouse Human skin permeability of drugs in vivo can be estimated from in vitro experiment using human skin. However, some researchers have ethical and cultural difficulty to get human skins. Thus, animal skins have been widely used for pharmaceutical, toxicological and cosmetic R&D although the skins have a species difference between human. Recently, the 7th Amendment of the EC Cosmetic Directive prohibits the sale of cosmetics and ingredients validated their safety by animal testing with an alternative method. 1) Thus, researchers utilize reconstructed human skin instead of animal skin. The experiments used reconstructed epidermis is approved by the European Centre for the Validation of Alternative Methods (ECVAM) as the scientifically validated methods for skin corrosion and irritation. 2,3) Permeability studies with Episkin ® , EpiDerm TM and SkinEthic ® comparison to human and animal skin were investigated and the authors reported that the penetration flux through the reconstructed skin was higher than that of skin. [4][5][6] The OECD regulations accepted the results from the reconstructed skin 7) but don't approve it as an alternative method for in vitro human skin penetration experiment yet.Skin penetration is widely expressed by the mathematical models on the basis of the process of diffusion and dissolution. Penetration parameters, diffusion coefficient D [cm 2 /s] and partition coefficient K [-], through stratum corneum (SC) and viable skin (VS) of hairless mouse skin are found to well agree with that of human skin. 8) Not only the skin penetration profile but the blood concentration profile in human is well simulated using the penetration parameters determined from hairless mouse skin, the thickness of human SC and VS, the skin enzymatic parameters (first-ord...

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“…In vivo tests are usually conducted on human, rodent, and pig skin, which is the best approximation of human skin. Sometimes monkey skin is also used [2,[14][15][16][17][18].…”

Section: Percutaneous Absorption Assaymentioning

confidence: 99%

Mass transport model through the skin by microencapsulation system

Carreras

Alonso

Martı́

et al. 2015

Journal of Microencapsulation

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Skin drug delivery can be subdivided into topical and transdermal. In a topical administration, the drug is intended to act at skin level, this is indicated for the treatment of skin diseases such as follicle-related disorders (for example, acne and alopecias). The aim of transdermal administration is getting a systemic release, and in this case the skin represents a barrier and not a target. Transdermal administration can take advantage of chemical and physical strategies that can improve skin permeability and can allow to drug penetration.In this study the development of the skin penetration profile have carried out by in vitro technique for a microencapsulated system of Ibuprofen and was determined using pig skin. The release experiments are performed using absorption percutaneous test with Franz cells apparatus in order to know the evolution of the amount of the principle present in each of the different skin compartments (stratum corneum, epidermis and dermis) as well as in the receptor fluid, as a function of time by HPLC analysis. It has achieved a general kinetic model by a microencapsulated system as mass transport system through the skin. This modelization could serve to predict penetration in human skin of encapsulated substances from biofunctional textiles and the estimation of the dosification profile of the active principle.

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Follicles Play an Important Role in Percutaneous Absorption

Cited by 140 publications

References 9 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

Prediction of Percutaneous Absorption in Human Using Three-Dimensional Human Cultured Epidermis LabCyte EPI-MODEL

Mass transport model through the skin by microencapsulation system

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