Distribution of salicylic acid in human stratum corneum following topical application in vivo: a comparison of six different formulations

Tsai, Jui Chen; Chuang, Shan An; Hsu, May Ying; Sheu, Hamm Ming

doi:10.1016/s0378-5173(99)00217-3

Cited by 48 publications

(19 citation statements)

References 11 publications

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“…This finding has been also observed in other drugs (e.g. BFZ, 25) sertaconazole, 26) flutrimazole, 27) and salicylic acid 28) ). Ingredients of TCZ solution formulation are easy to volatilize, and the majority of TCZ in solution formulation is distributed over the surface of the stratum corneum soon after the applications.…”

Section: Discussionsupporting

confidence: 69%

Difference in Percutaneous Absorption and Intracutaneous Distribution in Guinea Pigs among Topical Antifungal Drugs (Tioconazole Solution, Tioconazole Cream, Miconazole Nitrate Solution and Bifonazole Solution)

Sobue

Sekiguchi

2004

Biological & Pharmaceutical Bulletin

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Tioconazole (TCZ) is an imidazole antifungal agent with broad spectrum activity in vitro against dermatophytes and yeasts, as well as against some chlamydia, trichomonads and Gram-positive bacteria.1,2) Its in vitro antifungal activity against dermatophytes, yeasts and bacteria is equal or stronger in comparison with those of the known imidazoles, miconazole nitrate (MCZ), bifonazole (BFZ) and clotrimazole. [3][4][5] TCZ has a dual mechanism of antifungal action that is inhibition of sterol biosynthesis and direct cell membrane damage. [6][7][8] In growing cultures, TCZ exerts a potent killing action. The extent and rapidity of this fungicidal effect of TCZ are greater than those of MCZ and clotrimazole. 9,10) This activity is paralleled by good topical efficacy in a guinea pig dermatomycosis model. 2,9) At the beginning, TCZ was been used as a cream formulation. Clinical trials for treating superficial dermatophyte or yeast infections of the skin have clearly demonstrated once to three times a day topical applications of TCZ cream were at least as effective as alternative imidazole antifungal drugs, and in a few trials significantly greater efficacy has been reported for TCZ cream, compared with MCZ, clotrimazole, and econazole. 1,[11][12][13][14] After that TCZ solution was developed as over-the-counter drug. The efficacy and safety of twice or three times a day topical preparations of TCZ solution appear to be similar to those of TCZ cream and clotrimazole solution. [15][16][17][18] Pharmacokinetic studies in rats have demonstrated minimal systemic exposure following dermal application of TCZ cream.2) After a single application of TCZ cream about 16% of the applied radioactivity penetrates into rat skin and the percutaneous penetration into swine skin is considerably higher than that of clotrimazole cream.19) BFZ also penetrates far better into human skin than clotrimazole. 20) Clinical trials have clearly demonstrated the efficacy and safety of various formulations of BFZ applied once a daily in the treatment of superficial fungal infections of the skin.4) The skin retention time of MCZ in effective therapeutic concentrations is longer than that of BFZ. MCZ formulations are also recommended for once a daily application. 21) In the present study, in order to support the usefulness of once a daily applications of TCZ solution and cream, the percutaneous absorption and intracutaneous distribution of TCZ solution were investigated and compared with those of TCZ cream, MCZ solution and BFZ solution following a single topical application to abdominal skin of guinea pigs. (Tokyo, Japan). Itraconazole, IS for BFZ, was extracted from commercial preparations purchased from Janssen Kyowa Co., Ltd. (Tokyo, Japan). All other chemicals used were of reagent grade. MATERIALS AND METHODS MaterialsAnimals Guinea pigs of the Hartley strain (Japan SLC, Shizuoka, Japan) weighing approximately 400 g were used in the study. The animals were kept in an animal room main- Tioconazole (TCZ) is an imidazole antifungal agent with broa...

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Section: Discussionsupporting

confidence: 69%

Difference in Percutaneous Absorption and Intracutaneous Distribution in Guinea Pigs among Topical Antifungal Drugs (Tioconazole Solution, Tioconazole Cream, Miconazole Nitrate Solution and Bifonazole Solution)

Sobue

Sekiguchi

2004

Biological & Pharmaceutical Bulletin

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“…To estimate the distribution of the model parameters and to test the hypothesis of KP-SLN gel superiority, a one-sided permutation test was performed (Tsai et al, 1999). The residuals defined as the deviation between calculated and model-predicted responses, were permuted and added to the predicted values, thus creating a new dataset.…”

Section: In Vivo Activity and Pharmacodynamics Modelingmentioning

confidence: 99%

“…It is well known that topical formulations determine bioavailability and clinical efficacy of NSAIDs through impacting their release and skin penetration (Tsai & Chuang, 1999). Therefore, understanding the complex relationship between formulation process parameters and physicochemical/biological responses is imperative for designing effective formulations.…”

Section: Ann Modelingmentioning

confidence: 99%

Topical ketoprofen nanogel: artificial neural network optimization, clustered bootstrap validation, and in vivo activity evaluation based on longitudinal dose response modeling

et al. 2016

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Objectives: This work aimed at investigating the potential of solid lipid nanoparticles (SLN) as carriers for topical delivery of Ketoprofen (KP); evaluating a novel technique incorporating Artificial Neural Network (ANN) and clustered bootstrap for optimization of KP-loaded SLN (KP-SLN); and demonstrating a longitudinal dose response (LDR) modeling-based approach to compare the activity of topical non-steroidal anti-inflammatory drug formulations. Methods: KP-SLN was fabricated by a modified emulsion/solvent evaporation method. BoxBehnken design was implemented to study the influence of glycerylpalmitostearate-to-KP ratio, Tween 80, and lecithin concentrations on particle size, entrapment efficiency, and amount of drug permeated through rat skin in 24 hours. Following clustered bootstrap ANN optimization, the optimized KP-SLN was incorporated into an aqueous gel and evaluated for rheology, in vitro release, permeability, skin irritation and in vivo activity using carrageenan-induced rat paw edema model and LDR mathematical model to analyze the time course of anti-inflammatory effect at various application durations. Results: Lipid-to-drug ratio of 7.85 ], Tween 80 of 1.27% [bootstrap 95%CI: 0.601-2.40%], and Lecithin of 0.263% [bootstrap 95%CI: 0.263-0.328%] were predicted to produce optimal characteristics. Compared with profenid Õ gel, the optimized KP-SLN gel exhibited slower release, faster permeability, better texture properties, greater efficacy, and similar potency. Conclusions: SLNs are safe and effective permeation enhancers. ANN coupled with clustered bootstrap is a useful method for finding optimal solutions and estimating uncertainty associated with them. LDR models allow mechanistic understanding of comparative in vivo performances of different topical formulations, and help design efficient dermatological bioequivalence assessment methods.

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“…Tape stripping (TS) has been investigated as a surrogate measure for bioavailability and bioequivalence assessment of topical products (8)(9)(10). It uses the concept of determining drug permeation through the stratum corneum (SC) following application to the skin of human subjects.…”

Section: Introductionmentioning

confidence: 99%

Comparison of tape stripping with the human skin blanching assay for the bioequivalence assessment of topical clobetasol propionate formulations.

Skinner

Kanfer

2010

J Pharm Pharm Sci

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-Purpose: A draft guidance on tape stripping for assessing the bioavailability/bioequivalence of topical formulations was issued by the United States Food and Drug Administration in 1998 but has since been withdrawn. This was due to problems associated with the method and also inconsistencies and variability in the resulting data. The purpose of this study was to re-visit the tape stripping technique, incorporate refinements to reduce variability and validate the method using bioequivalence data obtained from the assessment of a topical corticosteroid cream containing 0.05% clobetasol propionate using the human skin blanching assay. Methods: A pilot tape stripping study was conducted to establish the variability of the formulations.The bioequivalence of two different commercially available clobetasol propionate cream formulations and a clobetasol propionate ointment formulation were subsequently investigated using the tape stripping method. Results: The data from the pilot tape stripping study correlated well with data from the human skin blanching assay. A subsequent pivotal tape stripping study confirmed bioequivalence between the two cream formulations whereas bio-inequivalence was demonstrated between the cream and ointment formulations. Conclusions: These studies show that the results from tape stripping concur with data from the human skin blanching assay and demonstrate the potential of a well-controlled tape stripping study as an option for the assessment of bioequivalence of topical corticosteroid formulations. _______________________________________________________________________________________

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Distribution of salicylic acid in human stratum corneum following topical application in vivo: a comparison of six different formulations

Cited by 48 publications

References 11 publications

Difference in Percutaneous Absorption and Intracutaneous Distribution in Guinea Pigs among Topical Antifungal Drugs (Tioconazole Solution, Tioconazole Cream, Miconazole Nitrate Solution and Bifonazole Solution)

Difference in Percutaneous Absorption and Intracutaneous Distribution in Guinea Pigs among Topical Antifungal Drugs (Tioconazole Solution, Tioconazole Cream, Miconazole Nitrate Solution and Bifonazole Solution)

Topical ketoprofen nanogel: artificial neural network optimization, clustered bootstrap validation, and in vivo activity evaluation based on longitudinal dose response modeling

Comparison of tape stripping with the human skin blanching assay for the bioequivalence assessment of topical clobetasol propionate formulations.

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