Physical model approach to understanding finite dose transport and uptake of hydrocortisone in hairless guinea-pig skin

Seta, Yasuo; Ghanem, Abdel‐Halim; Higuchi, William I.; Borsadia, S.; Behl, Christian; Malick, A. Waseem

doi:10.1016/0378-5173(92)90046-5

Cited by 13 publications

(5 citation statements)

References 10 publications

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“…This, however, requires that the distribution factor f sc is known, e.g. by previous autoradiography experiments or by layerwise retention measurements in the skin as described by Seta et al [12]. In Neelissen et al [1] it was stated that the distribution factor can also be used to illustrate the effect of donor type on the distribution of 3 H-estradiol in the skin.…”

Section: Estimation Of Autoradiography Exposure Timementioning

confidence: 99%

Validation of Freeze-Drying to Visualize Percutaneous <sup>3</sup>H-Estradiol Transport: The Influence of Skin Hydration on the Efficacy of the Method

Neelissen¹,

Arth

Schrijvers

et al. 1998

Skin Pharmacol Physiol

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A study was made of the validity of freeze-drying to visualize the distribution of ³H-estradiol in human stratum corneum after topical application of a dry dose, a patch or a buffer solution. Each of these donor formulations was applied to human dermatomed skin for 24 h using Franz permeation cells. Subsequently, small pieces of skin were subjected to cryofixation, freeze-drying, osmium tetroxide vapor fixation, Spurr resin embedding and electron microscopic autoradiography. Stratum corneum from dry dose and patch application experiments was well preserved by freeze-drying, allowing an accurate localization of ³H-estradiol. In contrast, stratum corneum from buffer solution experiments suffered from cryofixation artifacts due to excessive hydration of the skin. The corresponding autoradiographs showed strong redistribution of ³H-estradiol. Thus, the visualization method under investigation has its limitations regarding the hydration level of the skin.

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Section: Estimation Of Autoradiography Exposure Timementioning

confidence: 99%

Validation of Freeze-Drying to Visualize Percutaneous <sup>3</sup>H-Estradiol Transport: The Influence of Skin Hydration on the Efficacy of the Method

Neelissen¹,

Arth

Schrijvers

et al. 1998

Skin Pharmacol Physiol

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“…In contrast to Seta et al [35], the experimental resolution of the epidermis is divided in lipophilic (SC) and hydrophilic parts (viable epidermis), which is more reasonable from a physiological point of view in our opinion. The same holds true for the works by Kasting et al [24,34] which focused on volatile compounds and thus did only supply mass balance information about the skin as a whole tissue [36,37] and, in a further study, about the epidermis and dermis [38].…”

Section: Discussionmentioning

confidence: 87%

“…After a successful description of the experimental setup a detailed diffusion model (MICRO) driven by input parameters gathered from infinite dose experiments was applied. It has been shown, that this is reasonable even for finite dose kinetics [7,35], whereas estimation from finite dose experiments may show great intra-individual variability [40]. In contrast to one-dimensional models cited above, the work at hand relies on a microscopic two-dimensional geometry.…”

Section: Discussionmentioning

confidence: 95%

Finite dose skin mass balance including the lateral part: Comparison between experiment, pharmacokinetic modeling and diffusion models

Selzer

Hahn

Naegel

et al. 2013

Journal of Controlled Release

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“…Many in vitro predictions aimed to envisage the cumulative amount penetrated, since determination of the amount of permeant in the skin is difficult and usually involves destruction of the barrier. Thus, Seta et al [ 41 ] simulated the concentration−time course in hairless guinea pig skin and the receptor in vitro, and Krüse [ 42 ] and Frasch and Barbero [ 43 ] extrapolated the time course of a permeant for finite dosing from parameters derived from infinite dose studies, and they found an overprediction of accumulated mass. Buist et al [ 44 ] also obtained an overestimation of the tested drug absorption.…”

Section: Discussionmentioning

confidence: 99%

Assessment of Finite and Infinite Dose In Vitro Experiments in Transdermal Drug Delivery

et al. 2021

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Penetration, usually with finite dosing, provides data about the total active amount in the skin and permeation, being the most used methodology, usually with infinite dosing, leads to data about pharmacokinetic parameters. The main objective of this work is to assess if results from permeation, most of them at finite dose, may be equivalent to those from penetration usually at infinite dose. The transdermal behavior of four drugs with different physicochemical properties (diclofenac sodium, ibuprofen, lidocaine, and caffeine) was studied using penetration/finite and kinetic permeation/infinite dose systems using vertical Franz diffusion cells to determine the relationships between permeation and penetration profiles. Good correlation of these two in vitro assays is difficult to find; the influence of their dosage and the proportion of different ionized/unionized compounds due to the pH of the skin layers was demonstrated. Finite and infinite dose regimens have different applications in transdermal delivery. Each approach presents its own advantages and challenges. Pharmaceutical industries are not always clear about the method and the dose to use to determine transdermal drug delivery. Being aware that this study presents results for four actives with different physicochemical properties, it can be concluded that the permeation/infinite results could not be always extrapolated to those of penetration/finite. Differences in hydrophilicity and ionization of drugs can significantly influence the lack of equivalence between the two methodologies. Further investigations in this field are still needed to study the correlation of the two methodologies and the main properties of the drugs that should be taken into account.

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Physical model approach to understanding finite dose transport and uptake of hydrocortisone in hairless guinea-pig skin

Cited by 13 publications

References 10 publications

Validation of Freeze-Drying to Visualize Percutaneous <sup>3</sup>H-Estradiol Transport: The Influence of Skin Hydration on the Efficacy of the Method

Validation of Freeze-Drying to Visualize Percutaneous <sup>3</sup>H-Estradiol Transport: The Influence of Skin Hydration on the Efficacy of the Method

Finite dose skin mass balance including the lateral part: Comparison between experiment, pharmacokinetic modeling and diffusion models

Assessment of Finite and Infinite Dose In Vitro Experiments in Transdermal Drug Delivery

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