Reservoir Function of the Stratum corneum: Development of an in vivo Method to Quantitatively Determine the Stratum corneum Reservoir for Topically Applied Substances

Teichmann, A.; Jacobi, U.; Weigmann, H.‐J.; Sterry, Wolfram; Lademann, J.

doi:10.1159/000083707

Cited by 35 publications

(39 citation statements)

References 37 publications

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“…In our work, considering the overall data ( table 1 ), a good in vitro/in vivo correlation was found. In the in vivo study the tape stripping methodology appears as a minimally invasive but powerful approach in obtaining information on the SC reservoir in real conditions [23] . However, the differences revealed in the SC distribution analyses suggest the need for parallel in vitro and in vivo experiments.…”

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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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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“…31,32) Investigations with primaquine demonstrated that both binding to corneocyte keratin as well as the miscibility of the drug with the lipid domains contribute to the horny layer reservoir. 33) Furthermore, a higher amount of GEN retained in the skin could be advantageous to ensure continuous drug levels in skin tissues and/or to reduce frequent administrations. 31) CONCLUSION A simple HPLC bioanalytical method was developed and validated for the precise and accurate determination of genistein in different skin layers, applicable to skin permeation studies.…”

Section: Resultsmentioning

confidence: 99%

Development and Validation of a Simple and Rapid Liquid Chromatography Method for the Determination of Genistein in Skin Permeation Studies

Maione-Silva

Rocha

Oliveira

et al. 2012

Biological & Pharmaceutical Bulletin

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Genistein (GEN) has potential advantages for topical skin delivery, but no literature data are available for its quantitation in different skin layers, such as the stratum corneum (SC). Therefore, a simple, rapid, selective and sensitive bioanalytical method was developed and validated for GEN quantitation in porcine skin samples following in vitro permeation studies. GEN was assayed by HPLC with UV-Vis detection (270 nm) using 0.5% acetic acid in water-n-propanol-acetonitrile (50 : 2 : 48, v/v/v) as mobile phase (flowrate of 1.0 mL/min). Specificity was demonstrated since endogenous skin components did not interfere with GEN peak. Standard analytical curve was linear over the concentration range (0.1-60 µg/mL) and the lower limit of quantitation was determined for different skin layers (100 ng/mL). GEN recovery from skin layers ranged from 95.57 to 97.57%. Permeation studies were carried out using an automated vertical diffusion cell apparatus. No fluctuation on the amount of GEN retained in the SC was observed over time, but increasing amounts of the drug were found in deeper layers of the skin. The method was reliable and reproducible for the quantitation GEN in skin samples enabling the determination of the cutaneous penetration profile of this drug in permeation experiments.Key words genistein; HPLC quantitation; bioanalytical validation; skin layer Genistein (GEN) (Fig. 1) is the main isoflavone found in soybeans with several beneficial effects in cardiovascular diseases, osteoporosis and postmenopausal syndrome. Potential advantages of GEN have been reported in different types of cancer, such as breast and prostate, as well as skin cancer. 1) GEN acts in carcinogenesis through different mechanisms such as induction of differentiation, inhibition of topoisomerase II, protein tyrosine kinase activity and angiogenesis. 1,2)Skin cancer arises predominantly from cells located within the epidermis.3) Thus, to reach skin malignancies and achieve therapeutic benefits, antitumoral drugs, such as GEN, have to penetrate the stratum corneum and reach deeper layers of the epidermis. 4) In general, topical administration is a challenge in pharmaceutics. 5) Regardless, previous studies have demonstrated GEN's viability for topical 6) and transdermal permeation from different kinds of vehicles.7) Thus, with the purpose of conducting percutaneous permeation studies, the quantitative determination of the drug in the skin is necessary in order to evaluate the efficiency of the proposed formulations. 8)Due to the complexity of the skin matrices and the need to quantify low levels of the drug in the epidermis, 9) a highly selective analytical tool is required, since most samples usually contain several endogenous components of the skin. In addition, the analytical method must present enough sensitivity, due to possible very low concentrations of the drug present in each skin layer. 10) Considering the complexity and heterogeneity of the skin tissue, an effective extraction procedure to completely recover the analyte from the ...

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“…The concentration of the chemical UV fi lter 4-methylbenzylidene camphor on the tape strips was analyzed spectroscopically using the modifi ed UV/VIS spectrometer for the determination of the UV absorption [31] .…”

Section: Determination Of the Uv Filter On Each Tape Strip (Study Desmentioning

confidence: 99%

“…The lengths of the bars in the penetration profi le correspond to the concentration of the UV fi lters in the corresponding depth of the SC. Therefore, the penetration profi le can be seen as a cut through the SC [31] .…”

Section: Calculation Of the Penetration Profi Les (Study Designs A Anmentioning

confidence: 99%

Follicular Penetration: Development of a Method to Block the Follicles Selectively against the Penetration of Topically Applied Substances

Teichmann

Otberg

Jacobi

et al. 2006

Skin Pharmacol Physiol

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Investigations into the penetration pathways of topically applied substances through the skin play an important role in dermatological science. Recently, the hair follicles have increasingly been recognized as an important pathway for percutaneous penetration, although the role of the follicles has still not been clarified in detail. Therefore, the aim of the present study was to develop an in vivo method for the analysis of the follicular rate of penetration processes. In order to reach this goal, the follicles were excluded from the penetration process of topically applied substances. Different study designs were evaluated, and we were able to show that the application of nail varnish to each follicular orifice represents an effective method of blocking the follicles selectively against the penetration of topically applied substances. In dermatological science, there is new information on the physiology of skin penetration processes, thus allowing examination of the follicular rate of penetration and improvement of the pharmacokinetics of topically applied substances.

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Reservoir Function of the Stratum corneum: Development of an in vivo Method to Quantitatively Determine the Stratum corneum Reservoir for Topically Applied Substances

Cited by 35 publications

References 37 publications

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

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

Development and Validation of a Simple and Rapid Liquid Chromatography Method for the Determination of Genistein in Skin Permeation Studies

Follicular Penetration: Development of a Method to Block the Follicles Selectively against the Penetration of Topically Applied Substances

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