Comparative in Vitro–in Vivo Percutaneous Penetration of the Fungicide ortho-Phenylphenol

Cnubben, N.H.P.; Elliott, Graham R.; Hakkert, Betty C.; Meuling, W.J.A.; Sandt, J.J.M. van de

doi:10.1006/rtph.2001.1530

Cited by 49 publications

(34 citation statements)

References 22 publications

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“…In addition, van de Sandt et al 22) and Cnubben et al 23) reported that the in vitro skin permeation rates of lipofilic compounds (propoxur and ortho-phenylphenol) were overestimated using human epidermal membranes and underestimated using intact human skins, compared with in vivo percutaneous absorption rates in humans. Sato et al 31) and Kawamata and Tojo.…”

Section: Discussionmentioning

confidence: 99%

“…20,21) In addition, several investigators have reported that the in vitro skin permeation rates of lipophilic compounds were overestimated using epidermal membranes and were underestimated using intact skins, compared with in vivo perctaneous absorption rates in humans. 22,23) Their findings indicate that VED acts as an important permeation barrier as well as stratum corneum. Therefore, we suggested that in vitro skin permeation studies should be performed, ideally using split skin with various thicknesses.…”

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confidence: 99%

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Influence of Skin Thickness on the in Vitro Permeabilities of Drugs through Sprague-Dawley Rat or Yucatan Micropig Skin

Takeuchi

Ishida

Furuya

et al. 2012

Biological & Pharmaceutical Bulletin

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The purpose of this study was to clarify the influence of skin thickness on the in vitro permeabilities of 3 model drugs with different physicochemical properties (nicorandil (NR), isosorbide dinitrate (ISDN) and flurbiprofen (FP)) through Sprague-Dawley rat (rat) or Yucatan micropig (YMP) skin. Intact, dermis-split, stratum corneum-stripped or stratum corneum-stripped and dermis-split rat or YMP skin (rat skin thickness: approximately 0.4, 0.9 or 1.2 mm; YMP skin thickness: approximately 0.4, 0.9, 1.8 or 2.8 mm) were set in Franz-type diffusion cells to determine the permeation rate, lag time and resistance ratio of the viable epidermis and dermis against whole skin (R ved /R tot ) of the drugs. The YMP skin permeabilities of the drugs decreased with an increase in the skin thickness, and significant differences were observed in the permeation rates and lag times between intact and dermis-split (0.4 mm) YMP skins. The decreases in the permeabilities of the drugs through the YMP skin were larger than those through the rat skin. The influence of resistances of ISDN and FP through the dermis-split rat or YMP skin was greater at 0.9 mm skin thickness than 0.4 mm skin thickness. The R ved /R tot values for the YMP skins were relatively large for lipophilic drugs (ISDN and FP), and these ratios increased with an increase in the dermis thickness. These results suggest that in vitro skin permeation studies must be done using dermis-split (0.4 mm) skin with the thinnest dermis for predicting in vivo human percutaneous absorption rate.Key words Yucatan micropig; intact skin; stripped skin; split skin; skin permeabilityIn vitro skin permeation studies have been broadly used in the development of transdermal formulations. Animal skins are frequently used as an alternative to human skin in percutaneous absorption studies, because human skin is not always available and the use of human tissues and organs creates ethical problems.1-10) Numerous animal models, including primate, porcine, mouse, rat, guinea pig and pig, have been utilized for skin permeability studies. 1,3,4,[11][12][13] Animal skins with minimal variations in skin permeability may be much better than human skin for determining or estimating the skin permeabilities of drugs and for developing transdermal formulations. 1,14,15) In our previous studies, the in vitro permeation of 3 model drugs was investigated through Sprague-Dawley rat (rat), Yucatan micropig (YMP) and human skin. 16,17) The 3 model drugs were selected because of their different log K o/w values (the logarithm of the octanol/water partition coefficient at 37°C; Table 1). 18) Nicorandil (NR), isosorbide dinitrate (ISDN) and flurbiprofen (FP) were used as hydrophilic, lipophilic and highly lipophilic drugs, respectively. The inter-individual variations in rat and YMP skin permeabilities for the 3 drugs were smaller than the human skin permeability. 16,17) In addition, in vitro permeation studies using rat and YMP skin were particularly useful for evaluating differences in the skin permeabilities o...

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Influence of Skin Thickness on the in Vitro Permeabilities of Drugs through Sprague-Dawley Rat or Yucatan Micropig Skin

Takeuchi

Ishida

Furuya

et al. 2012

Biological & Pharmaceutical Bulletin

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“…A good correlation between in vitro skin levels and in vivo total systemic absorption was reported for cathecol [20] . In addition a comparative in vitro/in vivo percutaneous absorption study of orthophenylphenol [21] and oxybenzone [22] showed a good correlation with in vivo data. In our work, considering the overall data ( table 1 ), a good in vitro/in vivo correlation was found.…”

Section: Discussionmentioning

confidence: 99%

In vitro Percutaneous Absorption and in vivo Stratum Corneum Distribution of an Organic and a Mineral Sunscreen

Mavon

Miquel

Lejeune

et al. 2006

Skin Pharmacol Physiol

179

114

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Sunscreens, whose main function is to protect the skin against the harmful effects of solar irradiation, should remain at the skin surface or impregnate the first layers of the stratum corneum only and not penetrate into the underlying living tissue. The goal of this work was to assess the penetration of titanium dioxide (TiO₂) and methylene bis-benzotriazoyl tetramethylbutylphenol (MBBT), included in a broad-spectrum sunscreen formulation, into human skin in vivo, using the tape stripping method, and in vitro, using a compartmental approach. An additional objective was to propose an easy and minimally invasive approach to determining the percutaneous uptake of sunscreens following topical application. TiO₂ and MBBT were quantified using colorimetric assay and HPLC analysis, respectively. The transmission electron microscopy and particle-induced X-ray emission techniques were used to localize the TiO₂ in skin sections.More than 90% of both sunscreens was recovered in the first 15 tape strippings. In addition we have shown that the remaining 10% did not penetrate the viable tissue, but was localized in the furrows and in the opened infundibulum. Less than 0.1% of MBBT was detected in the receptor medium, and no TiO₂ was detected in the follicle, viable epidermis or dermis. Thus, this in vivo and in vitro penetration study showed an absence of TiO₂ penetration into the viable skin layers through either transcorneal or transfollicular pathways and negligible transcutaneous absorption of MBBT. However, differences in distribution within the stratum corneum reinforced the need for a complementary approach, using minimally invasive in vivo methodology and in vitro compartmental analysis.This combination represents a well-adapted method for testing the safety of topically applied sunscreen formulations in real-life conditions.

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“…Some of the studies contained only in vivo [2-4, 10-12, 14, 23, 26, 31] or in vitro [5, 8, 13, 17, 19-21, 24, 29] data, whereas others contained both sets of data [6,7,9,15,16,18,22,25,27,28,30] .…”

Section: Resultsmentioning

confidence: 99%

Percutaneous Absorption in Man: In vitro-in vivo Correlation

Lehman¹,

Raney²,

Franz³

2011

Skin Pharmacol Physiol

112

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Aims: To examine the existing literature to determine the degree to which percutaneous absorption data obtained using the excised human skin model match those obtained from living man. Methods: The scientific literature was reviewed to collect data on compounds whose percutaneous absorption through human skin had been measured under both in vitro and in vivo conditions. The in vitro-in vivo (IVIV) correlation was evaluated by computing the in vitro/in vivo ratio using total absorption (percent of applied dose) as the metric for comparison. Results: A total of 92 data sets were collected from 30 published studies. The average IVIV ratio across all values was 1.6, though for any single data set there could be a nearly 20-fold difference between the in vitro and in vivo values. In 85% of the cases, however, the difference was less than 3-fold. The correlation was significantly improved when data were excluded from studies in which the protocols for both studies were not fully harmonized. For harmonized data sets the average IVIV ratio was 0.96 and there was a less than 2-fold difference between the in vitro and in vivo results for any one compound, with IVIV ratios ranging from 0.58 to 1.28. The dominant factors leading to exclusion of data were the use of skin from different anatomical sites and vehicles of differing composition. Conclusions: Percutaneous absorption data obtained from the excised human skin model closely approximate those obtained from living man when the two study protocols are appropriately matched.

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Comparative in Vitro–in Vivo Percutaneous Penetration of the Fungicide ortho-Phenylphenol

Cited by 49 publications

References 22 publications

Influence of Skin Thickness on the in Vitro Permeabilities of Drugs through Sprague-Dawley Rat or Yucatan Micropig Skin

Influence of Skin Thickness on the in Vitro Permeabilities of Drugs through Sprague-Dawley Rat or Yucatan Micropig Skin

In vitro Percutaneous Absorption and in vivo Stratum Corneum Distribution of an Organic and a Mineral Sunscreen

Percutaneous Absorption in Man: In vitro-in vivo Correlation

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