Abstract：
AIM AND METHODS:Drug development in dermatotherapy and also development of transdermal therapeutic systems (TTS) demand high-predictive in vitro models to estimate drug levels in skin and systemic uptake. Here we compare three ready-to-use models, reconstructed human epidermis, split porcine skin and the perfused porcine forelimb. 17beta-Estradiol (E(2)), which is highly metabolized by skin cells, serves as model drug since E(2) application is of high relevance in hormone replacement therapy while topical E(2) may promote wound healing. E(2) TTS, gel and an ethanolic solution were investigated for cutaneous penetration, permeation and metabolism. RESULTS:E(2) TTS enabled an E(2) uptake of 42.9% of the applied dose accompanied by a high percentage of E(2) metabolism (30% of the penetrated dose) in the perfused porcine forelimb. In Franz cell experiments with reconstructed human epidermis and split porcine skin, the gel allowed an E(2) uptake of 41.7 and 22.9% of the applied dose accompanied by a high E(2) metabolism (42.6 and 28.6% of the penetrated dose). Due to toxic effects of the vehicle, this was not true with an ethanolic solution, then E(2) permeation and metabolism were clearly diminished. Most importantly, the in vitro models proved to be predictive with respect to the E(2)/estrone ratio in female plasma under transdermal hormone replacement therapy. CONCLUSION:In vitro tests should reduce the need for both animal and human studies for cutaneous uptake and metabolism in the future.
journal_name
Skin Pharmacol Physioljournal_title
Skin pharmacology and physiologyauthors
Mahmoud A,Haberland A,Dürrfeld M,Heydeck D,Wagner S,Schafer-Korting Mdoi
10.1159/000081683subject
Has Abstractpub_date
2005-01-01 00:00:00pages
27-35issue
1eissn
1660-5527issn
1660-5535pii
81683journal_volume
18pub_type
杂志文章abstract：:A therapeutic endpoint is a very important tool to evaluate response in clinical trials. In 2005, a consensus statement identified two late endpoints of disease activity in pemphigus: complete remission off therapy and complete remission on therapy, both definitions applying to patients without lesions for at least 2 ...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000430101
更新日期：2015-01-01 00:00:00
abstract：BACKGROUND/AIMS:Wound healing is a complex regeneration process involving the degradation and reassembly of connective tissues and skin layers. Previous studies have shown that pH plays a significant role in both the direct and indirect regulation of cellular processes in the wound, which, in turn, affect the wound heal...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000447016
更新日期：2016-01-01 00:00:00
abstract：:The sirtuins are a family of proteins that comprise class III of the histone deacetylases. These NAD+-dependent proteins have been found to be intricately involved in a variety of important and skin-relevant cellular functions and processes, including aging, UV damage response, oxidative stress, and wound repair. In a...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,评审
doi：10.1159/000477417
更新日期：2017-01-01 00:00:00
abstract：BACKGROUND AND AIM:Since the pharmacological effects of diclofenac (DF) are short-lived because of its short half-life, prolongation of the pharmacological effect in a topical formulation is needed for more appropriate clinical use. For the enhancement of dermal accumulation and prolongation of the pharmacological effe...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000501734
更新日期：2019-01-01 00:00:00
abstract：:Solid lipid nanoparticles (SLNs) can enhance drug penetration into the skin, yet the mechanism of the improved transport is not known in full. To unravel the influence of the drug-particle interaction on penetration enhancement, 3 glucocorticoids (GCs), prednisolone (PD), the diester prednicarbate (PC) and the monoest...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000324053
更新日期：2011-01-01 00:00:00
abstract：:The skin pH is crucial for physiological skin functions. A decline in stratum corneum acidity, as observed in aged or diseased skin, may negatively affect physiological skin functions. Therefore, glycolic acid-containing water-in-oil (W/O) emulsions adjusted to pH 4 were investigated regarding their effect on normal o...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,随机对照试验
doi：10.1159/000439030
更新日期：2015-01-01 00:00:00
abstract：BACKGROUND/AIMS:The aim of the study was to elucidate the effect of sample preparation and microscope configuration on the results of confocal Raman microspectroscopic evaluation of the penetration of a pharmaceutical active into the skin (depth profiling). METHODS:Pig ear skin and a hydrophilic formulation containing...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000444806
更新日期：2016-01-01 00:00:00
abstract：:Brian Barry published over 300 research articles across topics ranging from colloid science, vasoconstriction and the importance of thermodynamics in dermal drug delivery to exploring the structure and organisation of the stratum corneum barrier lipids and numerous strategies for improving topical and transdermal drug...
journal_title：Skin pharmacology and physiology
pub_type： 传,历史文章,杂志文章
doi：10.1159/000351946
更新日期：2013-01-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Evidence suggests the importance of skin biophysical properties in predicting diseases and in developing appropriate skin care. The results to date of studies on skin surface pH, stratum corneum (SC) hydration and sebum content in both genders and at various ages have been inconclusive, which ...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000231524
更新日期：2009-01-01 00:00:00
abstract：:To reduce pruritus and colonization with Staphylococcus aureus, textiles containing silver are increasingly used as therapeutic option for patients with atopic dermatitis (AD). While wearing such textiles, the contained silver is in close contact with the patient's skin. The silver serves two purposes: to reduce bacte...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,随机对照试验
doi：10.1159/000265679
更新日期：2010-01-01 00:00:00
abstract：:The aim of the study was to assess an Ectoin formulation with regard to the antiageing properties. The study was designed as a monocentric, randomized, double-blind application test, in order to ensure the compatibility and the efficacy of Ectoin in comparison to a vehicle emulsion. A total of 104 voluntary healthy fe...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,随机对照试验
doi：10.1159/000103204
更新日期：2007-01-01 00:00:00
abstract：:Histone deacetylase inhibitors (HDACi), a relatively new group of epigenetic agents, are being investigated as powerful chemotherapeutics because of their antiproliferative and prodifferentiation effects both in vitro and in vivo, in various tumor cell lines. Only little is known with respect to their effects on norma...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,评审
doi：10.1159/000351363
更新日期：2014-01-01 00:00:00
abstract：:Despite sensitive skin being highly prevalent, no consensus on the definition and pathomechanism of sensitive skin exists. Here we report the results of a systematic literature review of diagnostic methods for sensitive skin at clinical, histological and biophysical levels. A systematic search revealed 27 out of 1,701...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,评审
doi：10.1159/000363149
更新日期：2015-01-01 00:00:00
abstract：BACKGROUND/AIM:The skin, as the outermost organ, protects against exogenous hazards (outside-in barrier) and prevents the loss of essential parts of the body (inside-out barrier). The epidermal barrier exerts several functions with specific morphological elements. Regional differences in skin functions are well known. ...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000330721
更新日期：2012-01-01 00:00:00
abstract：BACKGROUND:Cetuximab is a member of a new family of antineoplastic agents that inhibit the epidermal growth factor receptor (EGF-R), and which are increasingly being used in the treatment of solid tumors. METHODS:We have observed new secondary side effects. We present here 2 patients with acneiform eruption secondary ...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000106075
更新日期：2007-01-01 00:00:00
abstract：BACKGROUND:The use of antioxidants has become a common practice in the development of antiaging cosmetics. OBJECTIVE:The aim of this study was to evaluate the clinical efficacy of cosmetic formulations containing lycopene and melatonin antioxidants. METHOD:Thirty-six healthy women from 32 to 65 years were enrolled in...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000508673
更新日期：2020-01-01 00:00:00
abstract：BACKGROUND:Reactive oxygen species generated by ultraviolet light result in photocarcinogenic and photoaging changes in the skin. Antioxidants protect the skin from these insults. OBJECTIVE:The aim of this study was to determine the ex vivo ascorbic acid penetration and its degradation in the skin after its topical ap...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000081115
更新日期：2004-11-01 00:00:00
abstract：:The investigation of drug penetration into the stratum corneum (SC) by tape-stripping requires an accurate measure of the amount of SC on each tape-strip in order to determine the depth inside the SC. This study applies infrared densitometry (IR-D) to in vitro tape-stripping using the novel Squame Scan(R) 850A. The de...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000288165
更新日期：2010-01-01 00:00:00
abstract：BACKGROUND:Dry skin induced by rheumatoid arthritis (RA) causes itching, which negatively influences a patient's quality of life. We previously reported that mast cells are related to dry skin in arthritic mice. However, the mechanism of mast cell activation is unclear. In this study, we examined the mechanism underlyi...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000488250
更新日期：2018-01-01 00:00:00
abstract：OBJECTIVE:Epicutaneous application of capsaicin causes a long-lasting analgesic effect by binding to the membrane transient receptor potential vanilloid 1 (TRPV1) on mechanoheat-sensitive C and Aδ fibres, changing axonal integrity and inhibiting neurogenic inflammatory processes. To date, no information is available re...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000362740
更新日期：2015-01-01 00:00:00
abstract：BACKGROUND:Percutaneous penetration of urea in vivo in man has been documented. If urea can penetrate the skin, it may also move laterally. Lateral spreading of topical substances leads to unpredictable penetration dynamics and increased skin surface area exposure. METHODS:The ability of urea, a low molecular-weight h...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000363148
更新日期：2015-01-01 00:00:00
abstract：:Mometasone furoate (MMF) is a modern glucocorticoid of the 4th generation, which has been proven not only for inhalation but also for cutaneous treatment. Due to its lipophilic character, it is mainly used in ointments and creams with an outer lipophilic phase (W/O type). However, this study investigated the cutaneous...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000452743
更新日期：2016-01-01 00:00:00
abstract：:It is preferred that topically administered drugs act either dermally or transdermally. For that reason they have to penetrate into the deeper skin layers or permeate the skin. The outermost layer of the human skin, the stratum corneum, is responsible for its barrier function. Most topically administered drugs do not ...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,评审
doi：10.1159/000091978
更新日期：2006-01-01 00:00:00
abstract：:Along with antibiotics, antihistamines are the most widely used systemic drugs in dermatology. This is attributable to the major role played by histamine in common diseases such as urticaria and atopic eczema. Of the currently recognised four subtypes of G protein-coupled histamine receptors, only the H1 and H2 subtyp...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,评审
doi：10.1159/000086667
更新日期：2005-09-01 00:00:00
abstract：:Bepotastine besilate is an antihistaminic drug of the second generation with superior clinical responses. In this study, we investigated whether bepotastine modulates the production of cytokines/chemokines and the expression of CD54 in human epidermal keratinocytes. The production of IL-1alpha, CXCL10, and CCL17 and t...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000183924
更新日期：2009-01-01 00:00:00
abstract：:The pH of the skin is tightly regulated by endogenous buffering systems. We examined the influence of buffers of different pH and composition on skin barrier repair, pH, inflammation, and epidermal thickness/proliferation/differentiation. After tape-stripping in hairless mice buffers with pH 4-7 were applied in patch ...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000501976
更新日期：2019-01-01 00:00:00
abstract：BACKGROUND:The vitamin D endocrine system, besides multiple other functions, regulates aging in many tissues, including the skin. It protects the skin against the hazardous effects of many skin age-inducing agents, including ultraviolet radiation. Thus, in the present study we aimed to investigate the relationship betw...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000443839
更新日期：2016-01-01 00:00:00
abstract：OBJECTIVES:Retinoic acid (RA) and benzoyl peroxide (BP) were studied, comparing their keratolytic efficacy and water barrier disruption to that of salicylic acid (SA), a well-established keratolytic, under similar conditions. PATIENTS/METHODS:Six volunteers were included in this blinded study. Eleven randomized test s...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章,随机对照试验
doi：10.1159/000093984
更新日期：2006-01-01 00:00:00
abstract：:The aim of the study was to examine the effectiveness of the oxidized form of nicotinamide adenine dinucleotide (NAD(+)), adenosine precursor, in 37 patients suffering from psoriasis. As NAD(+) is known to be relatively unstable, the second goal was to establish the proper conditions for the satisfactory stability of ...
journal_title：Skin pharmacology and physiology
pub_type： 临床试验,杂志文章
doi：10.1159/000096170
更新日期：2007-01-01 00:00:00
abstract：BACKGROUND/AIMS:Extrinsic and intrinsic skin aging is subject to constant remodeling and degradation processes, primarily in components of the extracellular matrix. While collagen fibers thin out during the aging process, the amorphous elastin fibers accumulate. These are essential formative components of the dermis. S...
journal_title：Skin pharmacology and physiology
pub_type： 杂志文章
doi：10.1159/000477854
更新日期：2017-01-01 00:00:00
