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

Takeuchi, Hiroyuki; Ishida, Masahiro; Furuya, Atsushi; Todo, Hiroaki; Urano, Hidetoshi; Sugibayashi, Kenji

doi:10.1248/bpb.35.192

Cited by 50 publications

(32 citation statements)

References 31 publications

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“…YMP skin were prepared as described by Takeuchi, et al [11]. The full-thickness pig skin which is stored in a freezer at −80 °C advance, thawed slowly at about 4 °C, subcutaneous fat was removed using scissors.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of formulation properties and skin penetration in the same additive-containing formulation

Inoue

Suzuki

Maeda

et al. 2014

Results in Pharma Sciences

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The aim of this study is to examine the physicochemical properties of the external preparation, the effect on the skin permeability and the human senses. Miconazole nitrate cream formulation (MCZ-A: bland name and MCZ-B, −C, −D: generics) to measure the physicochemical properties, was performed by the skin permeation test and human sensory test. The flattening, viscoelasticity, and water content of each cream were measured and each cream was subjected to near-infrared (NIR) absorption spectroscopy and human sensory testing. The yield value was calculated based on measured flattening and was 734.8 dynes/cm2 for MCZ-A, 1198.9 dynes/cm2 for MCZ-B, 461.3 dynes/cm2 for MCZ-C and 3112.3 dynes/cm2 for MCZ-D. Measurement of viscoelasticity and viscosity revealed that MCZ-C had a smaller tanδ than the other 3 creams at 25 °C. NIR absorption spectroscopy revealed that MCZ-A had the highest absorption peak due to hydroxyl groups, followed by MCZ-C, −B, and then −D. Measurement of water content revealed that MCZ-A had a water content of 65.9%, MCZ-B, −C, and −D had a water content of around 56.3%. Human sensory testing revealed differences between MCZ-A and MCZ-C and between MCZ-B and MCZ-D in terms of spreadability and feel. These findings indicate that differences in water and oil content and emulsification resulted in the creams having different physical properties, such as flattening, internal structure, and dynamic viscoelasticity. NIR absorption spectroscopy, which allows non-destructive measurement of a sample’s physicochemical properties, and measurement of viscoelasticity and viscosity, which allows measurement of a sample’s dynamic viscoelasticity, revealed differences in the physical properties of creams. The skin permeation test, skin MCZ amount was 7.48 µg/cm2 for MCZ-A, 5.11 µg/cm2 for MCZ-B, 12.08 µg/cm2 for MCZ-C and 3.75 µg/cm2 for MCZ-D. In addition, since the drug spread is good about the skin migration, spreadability is affecting the potential dermal transfer.

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Section: Methodsmentioning

confidence: 99%

Evaluation of formulation properties and skin penetration in the same additive-containing formulation

Inoue

Suzuki

Maeda

et al. 2014

Results in Pharma Sciences

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“…One thousand-micrometer-thick stripped pig ear skin slices were prepared using a dermatome (Acculan 3Ti Dermatome, Aesculap-a B. Braun Company, Melsungen, Hessen, Germany) to separate the upper epidermis from the dermis and subcutaneous tissues [28].…”

Section: Skin Extraction and Pretreatmentmentioning

confidence: 99%

Potential of imaging analysis in establishing skin concentration-distance profiles for topically applied FITC-dextran 4 kDa

Kijima¹,

Masaki²,

Kadhum³

et al. 2015

ADMET DMPK

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Quantitatively determining the skin concentration-distance profiles of topically applied drugs is important for evaluating their safety and efficacy. The aim of the present study was to quantitatively visualize the distribution of hydrophilic drugs through the skin using confocal laser scanning microscopy (CLSM) in order to obtain skin concentration-distance profiles. FITC-dextran with a molecular weight of approximately 4 kDa (FD-4) was selected as the model fluorescent drug in the present study, and excised pig ear skin was used. The skin concentration of FD-4 at each depth of a skin section was assessed by imaging analysis of the intensity of fluorescence. The FD-4 skin concentration-distance profile obtained was analyzed usingFick's second law of diffusion, and was markedly similar to that using skin permeation parameters in the skin permeation study. These results suggest that the present CLSM method may be a promising tool for quantitatively visualizing the concentration-distance profiles of drugs through the skin.

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“…In addition, the thicknesses of the stratum corneum, epidermis and dermis of YMP skin are similar to those of human skin. Besides these similarities to human skin, because of the reproducibility of the Flux of drugs through the YMP skin, YMP skin has been used as an in vitro model of animal skin [15] [16]. In this study, the superior skin permeability profile, including the favorable values of Q, Flux and lag time, of SFP as compared to FP in the YMP skin indicates the favorable physiological properties of SFP for percutaneous absorption.…”

Section: Discussionmentioning

confidence: 92%

S(+)-Flurbiprofen Shows Potent PGE2 Inhibitory Activity in Inflammatory Cells, Superior Cell Transport Activity and Skin Permeability

Toda¹,

Sugimoto²,

Endo³

et al. 2016

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We developed a novel topical non-steroidal anti-inflammatory drug (NSAID)patch, S(+)-flurbiprofen plaster, (SFPP), containing S(+)-flurbiprofen (SFP), an enantiomer of flurbiprofen (FP).In a previous study conducted in an animal model, we showed good skin absorption and potent analgesic efficacy of SFPP. In this study, to examine the superior features, as an NSAID patch, of SFP as compared to FP and R(−)-flurbiprofen (RFP), we tested the stereospecificity of SFP actions on Prostaglandin E2 (PGE2) inhibition in rat inflammatory leukocytes and in the binding activity of the drug to cells, and also the in vitro skin permeability of the drug in the Yucatan micropig (YMP). SFP showed potent inhibitory activity on PGE2 production from peritoneal leukocytes stimulated with a bacterial suspension, as compared to RFP and FP. The half maximal (50%) inhibitory concentration (IC50) values were 14 nM for SFP, 52 nM for FP, and 17,000 nM for RFP. In the cell binding study, significant and rapid increase of SFP binding to polymorphonuclear leucocytes (PMNs) was observed at 5 min after incubation, eventually reaching a steady state. SFP showed significantly higher binding activity for the inflammatory leucocytes as compared to RFP, suggesting its superior transfer potency. The skin permeability profile of SFP, RFP and FP in the YMP model showed that the rank order of the cumulative amount of permeated compounds in the * Corresponding author. Y. Toda et al. 306skin was SFP > RFP > FP. The steady-state permeation rate (Flux) of SFP was significantly higher than that of FP (4.89 and 1.55 mg/cm 2 /h, respectively, p = 0.0068), indicating the remarkably superior skin permeability of SFP. SFP exerted potent inhibitory activity on PGE2 production and superior binding activity to the PMNs and skin permeability, as compared to FP and RFP. These results suggest that SFP possesses favorable characteristics for use as an active ingredient in the NSAID patch.

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

Cited by 50 publications

References 31 publications

Evaluation of formulation properties and skin penetration in the same additive-containing formulation

Evaluation of formulation properties and skin penetration in the same additive-containing formulation

Potential of imaging analysis in establishing skin concentration-distance profiles for topically applied FITC-dextran 4 kDa

S(+)-Flurbiprofen Shows Potent PGE2 Inhibitory Activity in Inflammatory Cells, Superior Cell Transport Activity and Skin Permeability

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