Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

Ishii, Hiroshi; Todo, Hiroaki; Sugibayashi, Kenji

doi:10.1248/cpb.58.556

Cited by 31 publications

(21 citation statements)

References 14 publications

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“…We previously reported that the cutaneous disposition of topically applied drugs could be predicted using the difference method based on Fick's 2 nd law of diffusion, and also that the average drug concentration in the stratum corneum and viable epidermis/dermis could be determined separately [19][20][21][22]. However, Fick's law-based approach requires a relatively advanced knowledge of mathematical equations in order to estimate the cutaneous disposition of topically applied drugs.…”

Section: Introductionmentioning

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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Section: Introductionmentioning

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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“…5) Briefly, the silicone membrane was set in a Franz-type diffusion cell with an effective permeation area of 0.38 cm 2 . The test ointments were applied to the donor cell side, and phosphate buffered saline (pH 7.4) (5.0 mL) was applied to the receiver cell side.…”

Section: Methodsmentioning

confidence: 99%

“…Previous studies reported that the vasoconstrictive effect could differ between generic and innovator topical steroids. [1][2][3][4] Because the thermodynamic activity and vehicle solubility of the drug affect its release characteristics from topical formulations, 5,6) drug permeation across the skin might be different between innovator and generic formulations. Therefore, it is necessary to compare the drug release profiles of innovator and generic formulations.…”

mentioning

confidence: 99%

Release Profiles of Dexamethasone Dipropionate from Admixtures of Steroid and Heparinoid Ointments Prepared by Different Mixing Methods

Suzuki

Uchino

Miyazaki

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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Characterization and release profiles of commercial dexamethasone dipropionate (DDP) from an innovator and 2 generic ointments (Methaderm (IM), Promethasone (GP), and Mainvate (GM)) and their admixtures with heparinoid ointment (Hirudoid Soft) were investigated. The admixtures were prepared using 2 mixing methods (slab or rotation/revolution mixer). Microscopic and FT-Raman spectrometric analyses revealed that the ointments, except for IM, contained DDP crystals. A silicone membrane was used for the evaluation of the DDP permeation. The permeated DDP amounts from GP and GM were lower than that from IM, indicating that DDP solubility in the ointment vehicle affected the release of DDP from the ointment. No significant differences were observed in DDP release between IM alone and its admixture prepared using a slab; however, DDP release from the admixture prepared using a rotation/revolution mixer was significantly lower than those from IM alone and its admixture by slab. In the GP system, DDP release from the admixtures by the 2 mixing methods was higher than that from GP alone, whereas no significant difference in DDP release between the 2 mixing methods was observed. No significant differences were observed between the GM and admixtures. The apparent solubility of DDP in the admixtures as determined by the ultracentrifugal separation method indicated that the DDP amount in the liquid phase of admixtures with GP was 6 times higher than that of admixtures with IM or GM. Therefore, the apparent solubility of DDP in the liquid phase in the GP system might influence the DDP release in admixtures.

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“…Therefore, synthetic artificial membranes have been used in permeability evaluations. [3][4][5] Maitani et al…”

Section: 2)mentioning

confidence: 99%

“…Therefore, synthetic artificial membranes have been used in permeability evaluations. [3][4][5] Maitani et al6) evaluated the permeability of diclofenac salts and free diclofenac acid through a silicone membrane to understand the mechanism of percutaneous absorption of ionizable drugs, and the existence of the lipid pathway for diclofenac salts was the same as for diclofenac acid. Strat-M ® is a commercially available multi-layered artificial membrane that is made from polyether sulfonic acid.…”

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confidence: 99%

Effect of Esters on the Permeation of Chemicals with Different Polarities through Synthetic Artificial Membranes Using a High-Throughput Diffusion Cell Array

et al. 2016

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) was measured and correlated with the physicochemical properties of the esters, including their solubility, viscosity, wettability, surface tension, and uptake. The amount of each model compound that permeated through the silicone membrane was not significantly correlated with the solubility of the esters but was significantly correlated with all other measured physical properties of the esters. Similar correlations were observed for the amounts of AMP, BA, and FP that passed through the Strat-M ® membrane. However, the amount of CF that permeated through the Strat-M ® membrane also correlated with the solubility of the esters. There was a highly significant correlation between the amount permeating through the silicone and Strat-M ® membranes because the model compounds had high lipophilicity. These findings demonstrated that to control the permeation of various chemicals through artificial membranes, it is important to consider the uptake of the esters and that the solubility of the esters is also an important consideration when using a more complex membrane.Key words alternative membrane; high-throughput; ester; silicone membrane; Strat-M; physical property In order to develop transdermal drug delivery systems, permeability has been evaluated using Fick's law of diffusion. 1,2)Fick's First Law indicates that the rate of mass transfer across a membrane is proportional to the concentration gradient expressed across the membrane. Synthetic artificial membranes are uniform and are designed to mimic human skin to avoid variability among tissues. They offer a simple and reproducible alternative to human and animal skins and provide key information to help understand the mechanisms of drug permeation by the evaluation of changes in a basic permeation parameter because, theoretically, skin permeation of chemicals can be expressed by physicochemical phenomena of diffusion and partition of compounds. Therefore, synthetic artificial membranes have been used in permeability evaluations. [3][4][5] Maitani et al.6) evaluated the permeability of diclofenac salts and free diclofenac acid through a silicone membrane to understand the mechanism of percutaneous absorption of ionizable drugs, and the existence of the lipid pathway for diclofenac salts was the same as for diclofenac acid. Strat-M ® is a commercially available multi-layered artificial membrane that is made from polyether sulfonic acid. 7) We reported previously also that the permeability coefficients, partition parameters, and diffusion parameters of chemicals through a Strat-M ® membrane were similar to those in human skin, and those in silicone membrane were under-or over-estimation to those in human skin, depending on the lipophilicity of the model compounds. 8,9) In addition, several previous studies have assessed the effects of vehicles on the permeation of chemicals through artificial membranes.10-13) For example, Twist and Zatz 10)evaluated the effect of alcohol on the permeation rate (flux) of methyl-, ethyl-, propyl-, and butyl-parabens. Dias et al. 12)r...

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Effect of Thermodynamic Activity on Skin Permeation and Skin Concentration of Triamcinolone Acetonide

Cited by 31 publications

References 14 publications

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

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

Release Profiles of Dexamethasone Dipropionate from Admixtures of Steroid and Heparinoid Ointments Prepared by Different Mixing Methods

Effect of Esters on the Permeation of Chemicals with Different Polarities through Synthetic Artificial Membranes Using a High-Throughput Diffusion Cell Array

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