The critical role of the vehicle to therapeutic efficacy and patient compliance.
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Administration, Topical↗
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Results for “Skin Absorption”
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Effect of saline iontophoresis on skin barrier function and cutaneous irritation in four ethnic groups.
The effect of saline iontophoresis on skin barrier function and irritation was investigated in four ethnic groups (Caucasians, Hispanics, Blacks and Asians). Forty healthy human volunteers were recruited according to specific entry criteria. Ten subjects, five males and five females, were assigned to each ethnic group. Skin barrier function was examined after 4 hours of saline iontophoresis at a current density of 0.2 mA/cm(2) on a 6.5 cm(2) area in terms of the measured responses: transepidermal water loss (TEWL), skin capacitance, skin temperature and visual scores. There were significant differences in TEWL among the ethnic groups prior to patch application. TEWL at baseline in ethnic groups was in the rank order: Caucasian>Asian>Hispanic>Black. Iontophoresis was generally well tolerated, and skin barrier function was not irreversibly affected by iontophoresis in any group. There was no significant skin temperature change, compared to baseline, in any ethnic groups at any observation point. Edema was not observed. At patch removal, the erythema score was elevated in comparison to baseline in all ethnic groups; erythema resolved within 24 hours. Thus, saline iontophoresis produced reversible changes in skin barrier function and irritation in healthy human subjects.
Adolescent↗
Gasoline contact burns.
In the past four years, four cases of gasoline contact burns have been treated at the Detroit General Hospital Emergency Department. Signs are erythema and blister formation within 24 hours. Treatment is removal of contaminated clothing and washing the surface with soap and water plus open exposure of the wounds. Renal failure is not caused by skin absorption but may develop following inhalation.
Accidents, Traffic↗
Dermal exposure to aqueous solutions of N-methyl pyrrolidone.
N-methyl pyrrolidone (NMP) is a substance widely used for its strong and selective solvent capacity. The strong potential NMP has for skin absorption makes biological monitoring ideal for exposure assessment. This study looked at brief exposures to NMP in aqueous solutions over a range of concentrations. Two volunteers placed one hand in NMP solutions ranging from 5 to 25% for as long as 15 min followed by urine collection for 48 h. The analyte of interest (analysed by GC-MS) was the NMP metabolite 5-hydroxy-N-methyl pyrrolidone (5-HNMP). Excretion of 5-HNMP was plotted against time and this showed that urine concentrations were at a maximum after about 10 h and 5-HNMP excretion continued for 48 h after exposure. The half-life of excretion was found to be approximately 11 h. The mean correlation between exposure (as a measure of exposure duration and solution concentration) and total 5-HNMP excreted was 0.9297.
Administration, Cutaneous↗
Simulation of skin permeability in chitosan membranes.
To provide an alternative means of evaluating transdermal drug delivery systems, membranes of chitosan were developed. The membranes were prepared by cast-drying method. The effects of chitosan concentration, sodium tripolyphosphate (NaTPP) concentration and crosslinking (CL) time on flux and lag time were studied using central composite design. It was observed that chitosan membrane at a particular composition simulated the permeation of diclofenac sodium through rat skin The mathematical model developed in the present study can be used to simulate the permeation of drugs through different species of animal skins.
Analysis of Variance↗
Skin, the final frontier.
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Administration, Cutaneous↗
Skin permeation enhancement effect and skin irritation of saturated fatty alcohols.
Though the skin permeation enhancement effect of chemical penetration enhancers has been studied extensively, their skin irritation potential has not been adequately investigated. The objective of this study was to evaluate the skin permeation enhancement effect and skin irritation of saturated fatty alcohols using melatonin as a model compound. A saturated solution of melatonin in a mixture of water and ethanol (40:60) containing 5% w/v of saturated fatty alcohol was used in the skin permeation studies using Franz diffusion cells. For skin irritation studies, 230 microl of fatty alcohol solution was applied on the dorsal surface of the hairless rats using Hill top chamber. The skin irritation was evaluated by visual scoring method and bioengineering methods such as measurement of transepidermal water loss (TEWL) and skin blood flow. The flux of melatonin across hairless rat skin was found to be dependent on the carbon chain length of the fatty alcohols, with decanol showing the maximum permeation of melatonin. All fatty alcohols increased the TEWL and skin blood flow significantly compared with the vehicle. The fatty alcohols (decanol, undecanol and lauryl alcohol), which showed greater permeation of melatonin, also produced greater TEWL, skin blood flow and erythema. Tridecanol and myristyl alcohol showed lower permeation enhancement effect but caused greater skin irritation. Octanol and nonanol may be the most useful enhancers for the transdermal delivery of melatonin considering their lower skin irritation and a reasonably good permeation enhancement effect. However, further studies are needed to ascertain their safety as skin penetration enhancers. Skin permeation and skin irritation in experimental animals such as rats are generally higher compared with human skin. Further studies in human volunteers using fatty alcohols at the concentrations of 5% or lower may provide useful information on the utility of these fatty alcohols as permeation enhancers.
Administration, Cutaneous↗
Ultrasound-enhanced diffusion into coupling gel during phonophoresis of 5-fluorouracil.
PURPOSE: To investigate the competitive transport across skin and back-diffusion of 5-fluorouracil into coupling gel under the influence of ultrasound, heat-alone and Azone enhancement. METHODS: The ultrasound effect on 5-fluorouracil penetration through whole rat skin was investigated in modified diffusion cells using a commercial ultrasound generator which was calibrated with a bilaminar membrane hydrophone. RESULTS: Ultrasonic dosimetry measurements demonstrated that the skin membrane was subjected to a complex and unpredictable standing wave field which induced physiologically acceptable heating of the tissue. Surprisingly, ultrasonication produced a decrease in percutaneous drug penetration. Quantification studies indicated that this effect was due to the diffusive loss of the hydrophilic substance 5-fluorouracil from the skin surface into the overlying volume of coupling gel. This phenomenon could be duplicated by the application of conductive heating, indicating that the thermal effects of ultrasound were probably responsible for accelerated 5-fluorouracil diffusion through the gel. CONCLUSION: This study acutely demonstrates how formulation design of the donor vehicle/coupling gel may radically affect therapeutic efficacy in phonophoretic systems.
Animals↗
Transdermal drug delivery. Clinical aspects.
The delivery of drugs into and through the skin is a recognized and effective means of therapy for dermatologic, regional, and systemic disease. The selection of drug candidates and the rational design of suitable formulations depends upon the biological make-up of the skin's barrier, and the physiochemical interactions between the membrane, the delivery system technology, and the active agent. This article summarizes the state of the art and examines more recent developments that are the subject of considerable research at this time. In addition, the potential to use the skin as a portal for noninvasive clinical chemistry (e.g., for glucose monitoring in diabetics) is discussed.
Administration, Cutaneous↗
The skin barrier and use of moisturizers in atopic dermatitis.
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Administration, Topical↗
The effect of dryness on the skin.
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Body Water↗
Effect of L-fucose and fucose-rich oligo- and polysaccharides (FROP-s) on skin aging: penetration, skin tissue production and fibrillogenesis.
Skin thickness is decreasing with age. This loss concerns both dermis and epidermis, cells and extracellular matrix. We could show here that percutaneous application of an L-fucose-containing preparation produced an increase of skin thickness and a densification of collagen bundles. We also could show that 3H-L-fucose penetrates in the dermis, a prerequisite for the above mentioned favorable pharmacological activities. These results, together with the previous favorable activities on the downregulation of matrix-degrading enzymes, free radical scavenging and increased cell proliferation confirm the favorable action of fucose and fucose-rich polysaccharides (FROP-s) on the skin by slowing down its aging.
Administration, Topical↗
Capsaicin and nonivamide as novel skin permeation enhancers for indomethacin.
The study was conducted in vitro to investigate the changes of indomethacin transdermal permeation pretreated by capsaicin and nonivamide, two compounds chemically similar to Azone. The combined effect of low frequency ultrasound (20 kHz) and enhancers on the indomethacin permeation was also evaluated. The experimental data demonstrated that capsaicin and nonivamide significantly enhanced the flux of indomethacin across nude mouse skin. Enhancement effects of both analogues were very similar and depended predominantly on the concentration tested. Histological examination coupled with visual scores indicated the safety of capsaicin and nonivamide on skin structure. Simultaneous application of ultrasound and enhancers significantly increased skin permeation of indomethacin compared with either ultrasound or enhancers alone. Better effect was obtained by the combination with capsaicin than nonivamide.
Animals↗
Random sampling or 'random' model in skin flux measurements? [Commentary on "Investigation of the mechanism of flux across human skin in vitro by quantitative structure-permeability relationships"].
Transdermal therapy receives increasing attention as an attractive alternative to traditional drug delivery. Unfortunately the exact algorithm of transdermal permeation that could guide medicinal chemists towards delivery optimization at an early stage of the drug design process still remains to be decoded. This paper discusses some major hurdles on the way to full understanding of Quantitative Structure-Activity Relationships (QSAR) of skin permeation. From the statistical perspective, a recently published combined data set is found to be inappropriate with respect to the distribution of major molecular descriptors, and therefore should be approached cautiously as a source for QSAR model training and in modelling of occupational and environmental skin exposures.
Cell Membrane Permeability↗
Development of sesquiterpenes from Alpinia oxyphylla as novel skin permeation enhancers.
To improve the drug permeation into and/or across the skin, essential oils extracted from Alpinia oxyphylla (AO) were evaluated using in vitro and in vivo permeation techniques with Wistar rats as the animal model. Hydrocarbons and oxygenated sesquiterpenes were the major components in the lower-polarity fraction (AO-1) and higher-polarity fraction (AO-2), respectively. Permeation of indomethacin was significantly enhanced after treatment with AO-1 and AO-2 in the in vitro and in vivo studies. AO-2 generally showed a higher ability to promote drug permeation compared to AO-1. The increment of skin/vehicle partitioning may be the predominant mechanism for this enhancing activity. Both transepidermal water loss (TEWL) and colorimetric evaluation showed limited irritation to skin by AO essential oils at the macroscopic level. Human skin fibroblasts were used to investigate the in vitro screening of skin toxicity. AO-1 slightly increased prostaglandin E(2) (PGE(2)) formation from skin fibroblasts. A striking result was observed with AO-2, which greatly inhibited the release of PGE(2). Moreover, both AO essential oils had no statistically significant effect on PGE(2) release by human lung epithelial cells. The results of this study indicate that skin disruption and inflammation do not necessary correspond to the enhancing efficiency of the enhancers tested.
Alpinia↗
Comparative permeation studies for delta-aminolevulinic acid and its n-butylester through stratum corneum and artificial skin constructs.
The improvement of the permeation properties through excised human stratum corneum and artificial skin constructs (ASC) of delta-aminolevulinic-n-butylester (ABE) compared with delta-aminolevulinic acid (ALA) was investigated. For this purpose the permeated amounts of each substance were determined depending on time in a Franz diffusion cell experiment with stratum corneum and ASC, respectively. Furthermore the barrier properties of ASC were compared with those of stratum corneum. Detection of both substances was performed by high-performance liquid chromatography (HPLC) analysis. For the determination of ABE a new HPLC method was developed. ABE could be determined with the new HPLC method with sufficient sensitivity (detection limit: 0.1 microg/ml) after derivatisation with o-phthalaldehyde (OPA). Stratum corneum and ASC were more permeable for ABE than for ALA. The permeation coefficient P of ABE through stratum corneum was nearly ten-fold higher than that of ALA. Using ASC as permeation barrier the permeation coefficient of ABE was about 22-fold higher than that of ALA. ABE and ALA permeated 142-fold and 64-fold, respectively, faster through ASC than through stratum corneum.
Aminolevulinic Acid↗
In vitro percutaneous penetration through hairless rat skin: influence of temperature, vehicle and penetration enhancers.
Theoretically, a positive relation is expected between skin temperature and the percutaneous penetration of topically applied substances. The aim of the present study was to evaluate the influence of the temperature on the in vitro percutaneous penetration of dihydrotestosterone. Hairless rat skin was mounted in static diffusion cells placed in a water bath at different temperatures (28.6, 35.1 and 38.2 degrees C, respectively). Different vehicles were tested as well as the addition of penetration promoting molecules such as oleic acid and limonene. A saline buffer was used as the receptor phase. Penetration through the skin was evaluated by means of scintillation counting of the radiolabelled dihydrotestosterone. Experiments were followed for a period of 29 h. The total amount of penetrant, dihydrotestosterone, as well as the flux, were calculated from these kinetics. Our results demonstrate a temperature effect with the highest penetration at 38.2 degrees C. The vehicle was also found to influence the penetration of dihydrotestosterone in a significant way. Furthermore, limonene presented better penetration promoting properties compared with oleic acid.
Administration, Topical↗
The transdermal revolution.
Historically, developments in transdermal drug delivery have been incremental, focusing on overcoming problems associated with the barrier properties of the skin, reducing skin irritation rates and improving the aesthetics associated with passive patch systems. More-recent advances have concentrated on the development of non-passive systems to aid delivery of larger drug molecules, such as proteins and nucleotides, as the trend for discovering and designing biopharmaceuticals continues. Fundamentally, improvements in transdermal delivery will remain incremental until there is wider acceptance of this route of administration within the pharmaceutical industry. Only then will the transdermal revolution live up to its true potential.
Administration, Cutaneous↗