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Shah, Vinod P.; Flynn, Gordon L.; Yacobi, Avraham; Maibach, Howard I.; Bon, Charles; Fleischer, Nicholas M.; Franz, Thomas; Kaplan, Stanley A.; Kawamoto, Jeff; Lesko, Lawrence J.; Marty, Jean‐Paul; Pershing, Lynn K.; Schaefer, H.; Sequeira, Joel; Shrivastava, S. P.; Wilkin, Jonathan K.; Williams, Roger L.

doi:10.1023/a:1011941929495

Cited by 141 publications

(27 citation statements)

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“…Furthermore, these methods cannot provide a visual observation of drug disposition from the surface to deeper regions of the skin, which is necessary for further understanding of the dermatopharmacokinetics of topically applied drugs. The tape-stripping method [8][9][10][11][12] has been used to measure drug concentrations at each depth of the skin, but only in the stratum corneum. A clearer understanding of drug disposition through the whole skin will be helpful for evaluating their safety and efficacy by specifying the skin tissue targeted by these 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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“…An emulsion with 10% water instead of DGME served as control formulation. The penetration of quercetin into human skin was studied in vivo using the tape stripping technique, based on the progressive removal of the stratum corneum outer layers by sequential stripping with adhesive tapes [29,30,36]. The amount of quercetin transferred to the individual tape strips following topical application of the tested formulations was quantified to provide the in vivo stratum corneum penetration profile of the flavonoid.…”

Section: Resultsmentioning

confidence: 99%

“…This is a disadvantage since in vivo studies in humans provide the most direct, realistic and therefore conclusive information on skin penetration. In fact, although in vitro testing represents a useful and simple model for the prediction of percutaneous absorption, it may produce responses different from the in vivo situation due to modifications of the barrier organization as well as of the functional properties of the isolated stratum corneum or full-thickness skin [28,29]. Moreover, animal skin used in in vivo experiments exhibits different permeability than human skin [29,39], and hence the relevance of the observed effects to realistic conditions is limited.…”

Section: Discussionmentioning

confidence: 99%

“…The tapes were applied to the skin with a constant pressure by a 500 g stainless steel roller (30 mm diameter). The first stripped tape was added to the cotton swab for the assay of the unabsorbed quercetin [29,36]. The successive 14 tape strips were collected separately in 4 groups (group 1: strips 2–4; group 2: strips 5–7; group 3: strips 8–11; group 4: strips 12–15).…”

Section: Methodsmentioning

confidence: 99%

“…In order to overcome this problem, in this study the skin penetration of the flavonoid was assessed in vivo on human volunteers using a noninvasive procedure, namely the tape-stripping technique, based on the progressive removal of the outer stratum corneum layers with adhesive tapes [29,30]. The effect of different topical vehicles on the in vivo percutaneous permeation of quercetin was investigated.…”

Section: Introductionmentioning

confidence: 99%

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Comparative Evaluation of the Effect of Permeation Enhancers, Lipid Nanoparticles and Colloidal Silica on in vivo Human Skin Penetration of Quercetin

Scalia

Franceschinis

Bertelli

et al. 2012

Skin Pharmacol Physiol

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Background/Aim: The aim of this study was to evaluate emulsions containing a penetration enhancer, lipid nanoparticles (LNs) or colloidal silica as systems to improve the topical delivery of the flavonoid quercetin. Methods: The skin penetration of quercetin was investigated in vivo on human volunteers by tape stripping. Quercetin-loaded LNs were prepared using hot high-pressure homogenization and characterized by means of dynamic light scattering and release studies. The location of the silica nanoparticles in the skin was determined by inductively coupled plasma mass spectrometry assay of silicon in the stratum corneum strips. Results and Conclusions: The penetration enhancer diethylene glycol monoethyl ether did not produce any significant increase in the fraction of the applied quercetin dose permeated in vivo into human stratum corneum (17.1 ± 3.2%) compared to the control emulsion (18.1 ± 2.3%). A greater but statistically nonsignificant accumulation of the flavonoid in the human horny layer (21.2 ± 2.9% of the applied dose) was measured following topical application of quercetin-loaded LNs (mean particle size: 527 nm). On the other hand, the addition of colloidal silica (average particle diameter: 486 nm) to the emulsion (2%, w/w) significantly increased the in vivo uptake of quercetin by the human stratum corneum to 26.7 ± 4.1% of the applied dose, the enhancing effect on permeation being more marked in the deepest horny layer strips. The measured in vivo skin penetration profile of colloidal silica showed that silica particles diffused down to the intermediate region of the human horny layer and hence could act as carrier for quercetin.

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Semisolid Dosages: Ointments, Creams, and Gels

Ravichandran

Jasti

2010

Pharmaceutical Sciences Encyclopedia

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Semisolid dosage forms are traditionally used for treating topical ailments. Various categories of drugs such as antibacterials, antifungals, and antivirals are incorporated into these products, which show their activity on the surface layers of tissues or penetrate into internal layers to reach the site of action. This article focuses on the formulation, evaluation, and regulatory features of ointments, creams, and gels.

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Cited by 141 publications

References 0 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

Comparative Evaluation of the Effect of Permeation Enhancers, Lipid Nanoparticles and Colloidal Silica on in vivo Human Skin Penetration of Quercetin

Semisolid Dosages: Ointments, Creams, and Gels

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